Search Result
Results for "
blood
" in MCE Product Catalog:
26
Biochemical Assay Reagents
115
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
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- HY-N10509
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- HY-W145690
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- HY-N10510
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Blood group A antigen tetraose type 5
A-Tetrasaccharide
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Others
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Others
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Blood group A antigen tetraose type 5 (A-Tetrasaccharide) is a tetrasaccharide and a blood group specific oligosaccharide, inhibits the binding of anti-A antibody to blood group A substance. Blood group A antigen tetraose type 5 can be isolated from polar bear milk samples.
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- HY-W145682
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- HY-118870
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- HY-P99769
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Omfiloctocog alfa
SCT-800
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Factor VIII
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Metabolic Disease
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Omfiloctocog alfa (SCT-800) is a recombinant factor VIII (FVIII). FVIII is an essential blood coagulation protein and a key component of the fluid phase blood coagulation system. Omfiloctocog alfa can be used for the research of Hemophilia A.
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- HY-130003
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- HY-B0202
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Irbesartan
SR-47436; BMS-186295
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Angiotensin Receptor
Apoptosis
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Cardiovascular Disease
Endocrinology
|
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Irbesartan (SR-47436) is an orally active Ang II type 1 (AT1) receptor blocker (ARB). Irbesartan can relax the blood vessels, low blood pressure and increase the supply of blood and oxygen to the heart. Irbesartan can be used for the research of high blood pressure, heart failure, and diabetic kidney disease.
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- HY-B0202A
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Irbesartan hydrochloride
SR-47436 hydrochloride; BMS-186295 hydrochloride
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Angiotensin Receptor
Apoptosis
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Metabolic Disease
Neurological Disease
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Irbesartan (SR-47436) hydrochloride is an orally active Ang II type 1 (AT1) receptor blocker (ARB). Irbesartan hydrochloride can relax the blood vessels, low blood pressure and increase the supply of blood and oxygen to the heart. Irbesartan hydrochloride can be used for the research of high blood pressure, heart failure, and diabetic kidney disease.
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- HY-106093
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Eltenac
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COX
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Inflammation/Immunology
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Eltenac, a non-steroidal anti-inflammatory drug (NSAID), is a COX inhibitor. Eltenac shows IC50 of 0.03 μM for both COX-1 and COX-2 in isolated human whole blood.
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- HY-135375
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- HY-W088068
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Wright's stain
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Fluorescent Dye
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Others
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Wright's stain is a hematologic stain that facilitates the differentiation of blood cell types. Wright's stain is classically a mixture of eosin (red) and methylene blue dyes. It is used primarily to stain peripheral blood smears, urine samples, and bone marrow aspirates. Wright's stain provides a manual or automated stain for bone marrow and peripheral blood smears.
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- HY-107398
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1-(2,3-Dichlorophenyl)ethanamine hydrochloride
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Others
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Cardiovascular Disease
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1-(2,3-Dichlorophenyl)ethanamine hydrochloride is a phenylethanolamine N-methyltransferase (PNMT) inhibitor. 1-(2,3-Dichlorophenyl)ethanamine hydrochloride effectively reduces blood pressure of spontaneously hypertensive. 1-(2,3-Dichlorophenyl)ethanamine hydrochloride can be used for the research of blood pressure.
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- HY-136346
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- HY-121354
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- HY-W233505
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Iophenoxic acid
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Others
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Others
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Iophenoxic acid is a systemic blood marker for assessment of bait acceptance by stoats (Mustela erminea) and weasels (Mustela nivalis).
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- HY-B0309
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Felodipine
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Calcium Channel
Autophagy
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Cardiovascular Disease
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Felodipine, a dihydropyridine, is a potent, vasoselective calcium channel antagonist. Felodipine lowers blood pressure (BP) by selective action on vascular smooth muscle, especially in the resistance vessels. Felodipine, an anti-hypertensive agent, induces autophagy. Felodipine can cross the blood-brain barrier.
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- HY-N10817
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- HY-N3009
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- HY-12515A
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- HY-B0946
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Sulfamonomethoxine
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Bacterial
Antibiotic
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Infection
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Sulfamonomethoxine is a long acting sulfonamide antibacterial agent, used in blood kinetic studies,and blocks the synthesis of folic acid by inhibiting synthetase of dihydropteroate.
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- HY-123563
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- HY-A0184
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Remikiren
Ro 42-5892; Ro 42-5892/001
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Renin
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Cardiovascular Disease
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Remikiren (Ro 42-5892) is an orally active and highly specific renin inhibitor. Remikiren specifically inhibits human reninand human plasma renin with IC50 values of 0.7 and 0.8 nM, respectively. Remikiren also reduces mean arterial blood pressure in sodium-depleted marmosets and squirrel monkeys. Remikiren can be used in study of hypertension.
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- HY-137892
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GSK620
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Epigenetic Reader Domain
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Inflammation/Immunology
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GSK620 is a potent and orally active pan-BD2 inhibitor with excellent broad selectivity, developability and in vivo oral pharmacokinetics. GSK620 is highly selective for the BET-BD2 family of proteins, with >200-fold selectivity over all other bromodomains. GSK620 shows an anti-inflammatory phenotype in human whole blood.
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- HY-135363
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- HY-12515
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Nicardipine
YC-93 free base
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Calcium Channel
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Neurological Disease
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Nicardipine (YC-93 free base) is a calcium channel blocker with an IC50 of 1 μM for blocking cardiac calcium channels. Nicardipine acts as an agent for chronic stable angina and for controlling blood pressure.
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- HY-121565
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- HY-147323
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- HY-N0252B
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Catharanthine Sulfate
(+)-3,4-Didehydrocoronaridine Sulfate
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Calcium Channel
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Cancer
Cardiovascular Disease
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Catharanthine Sulfate ((+)-3,4-Didehydrocoronaridine Sulfate) is an alkaloid isolated from Madagascar periwinkle, inhibits voltage-operated L-type Ca 2+ channel, with anti-cancer and blood pressure-lowering activities.
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- HY-B0371
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Terazosin
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Adrenergic Receptor
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Metabolic Disease
Endocrinology
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Terazosin is a quinazoline derivative and a competitive and orally active α1-adrenoceptor antagonist. Terazosin works by relaxing blood vessels and the opening of the bladder. Terazosin has the potential for benign prostatic hyperplasia (BPH) and high blood pressure treatment.
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- HY-B0371F
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Terazosin hydrochloride
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Adrenergic Receptor
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Endocrinology
Metabolic Disease
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Terazosin hydrochloride is a quinazoline derivative and a competitive and orally active α1-adrenoceptor antagonist. Terazosin hydrochloride works by relaxing blood vessels and the opening of the bladder. Terazosin hydrochloride has the potential for benign prostatic hyperplasia (BPH) and high blood pressure treatment.
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- HY-P3976
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- HY-135151
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Difluoro atorvastatin
Fluoroatorvastatin
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Drug Metabolite
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Cardiovascular Disease
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Difluoro atorvastatin (Fluoroatorvastatin) is an impurity of Atorvastatin. Atorvastatin is an orally active HMG-CoA reductase inhibitor, has the ability to effectively decrease blood lipids. Atorvastatin inhibits human SV-SMC proliferation and invasion with IC50s of 0.39 μM and 2.39 μM, respectively.
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- HY-148575
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α-Glucosidase-IN-23
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Glucosidase
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Metabolic Disease
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α-Glucosidase-IN-23 is an orally active α-Glucosidase inhibitor. α-Glucosidase-IN-23 decreases blood glucose by a-glucosidase inhibition with an IC50 value of 4.48 μM. α-Glucosidase-IN-23 can be used for the research of diabetes.
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- HY-B0371A
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Terazosin hydrochloride dihydrate
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Adrenergic Receptor
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Endocrinology
Metabolic Disease
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Terazosin hydrochloride dihydrate is a quinazoline derivative and a competitive and orally active α1-adrenoceptor antagonist. Terazosin hydrochloride dihydrate works by relaxing blood vessels and the opening of the bladder. Terazosin hydrochloride dihydrate has the potential for benign prostatic hyperplasia (BPH) and high blood pressure treatment.
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- HY-108299
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Perfluamine
Perfluorotripropylamine; FTPA; Tris(perfluoropropyl)amine
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Biochemical Assay Reagents
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Others
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Perfluamine (Perfluorotripropylamine), a hydrophobic carrier fluid, is used in the surface modification of droplet polymeric microfluidic devices. Perfluamine has a role as a blood substitute.
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- HY-148617
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- HY-B1815
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Xanthinol Nicotinate
Xanthinol Niacinate
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Others
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Cardiovascular Disease
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Xanthinol Nicotinate (Xanthinol Niacinate), a vasodilator, can act directly on the smooth muscle of small arteries and capillaries. Xanthinol Nicotinate expands blood vessels, improves blood rheology and reduces peripheral vascular resistance.
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- HY-114782
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- HY-12515AS
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Nicardipine-d3 hydrochloride
YC-93-d3
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Calcium Channel
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Neurological Disease
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Nicardipine-d3 (hydrochloride) (YC-93 D3) is the deuterium labeled Nicardipine hydrochloride. Nicardipine hydrochloride is a calcium channel blocker with an IC50 of 1 μM for blocking cardiac calcium channels. Nicardipine hydrochloride acts as an agent for chronic stable angina and for controlling blood pressure[1].
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- HY-P2273
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- HY-12611
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Sergliflozin etabonate
GW-869682X
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SGLT
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Metabolic Disease
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Sergliflozin etabonate (GW-869682X) is a potent and orally active sodium glucose cotransporter (SGLT2) inhibitor. Sergliflozin etabonate shows antidiabetic and antihyperglycemic effects. Sergliflozin etabonate significantly reduces non-fasting blood glucose levels in diabetic mice. Sergliflozin etabonate has the potential for the research of diabetes.
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- HY-18204
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- HY-N10885
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- HY-B0946S
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Sulfamonomethoxine-d4
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Bacterial
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Infection
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Sulfamonomethoxine-d4 is a deuterium labeled Sulfamonomethoxine. Sulfamonomethoxine is a long acting sulfonamide antibacterial agent, used in blood kinetic studies,and blocks the synthesis of folic acid by inhibiting synthetase of dihydropteroate[1].
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- HY-114794
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- HY-141892A
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DSPE-PEG Carboxylic acid sodium (MW 2000)
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Liposome
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Others
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DSPE-PEG Carboxylic acid sodium (MW 2000) is a PEG-lipid that can be used to form micelles as nanoparticles for drug delivery. DSPE-PEG Carboxylic acid sodium (MW 2000) increases the blood circulation time of liposomes.
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- HY-147299
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- HY-143226
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DK1
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Estrogen Receptor/ERR
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Metabolic Disease
|
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DK1 is a potent modulator of estrogen related receptor. DK1 has an ability in reducing blood glucose, and impacts the activity of ERRα receptor. DK1 has the potential for the research of diabetes.
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- HY-P1685
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- HY-148144
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- HY-W005288
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4-Vinylphenol
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Apoptosis
Endogenous Metabolite
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Cancer
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4-Vinylphenol is found in the medicinal herb Hedyotis diffusa Willd, wild rice and is also the metabolite of p-coumaric and ferulic acid by lactic acid bacteria in wine. 4-Vinylphenol induces apoptosis and inhibits blood vessels formation and suppresses invasive breast tumor growth in vivo.
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- HY-141510
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myo-Inositol trispyrophosphate hexasodium
ITPP hexasodium
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Others
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Cancer
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myo-Inositol trispyrophosphate (ITPP) hexasodium, a modifier of haemoglobin, is an allosteric effector that reduces the oxygen‐binding affinity of haemoglobin and facilitates the release of oxygen by red blood cells. myo-Inositol trispyrophosphate can reverse hypoxia, control tumor growth and improve chemotherapy response.
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- HY-150560
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α-Glucosidase-IN-11
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Glucosidase
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Metabolic Disease
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α-Glucosidase-IN-11 is a highly permeable competitive α-glucosidase inhibitor with the IC50 value of 0.56 μM. α-Glucosidase-IN-11 binds to Trp residues in α-glucosidase and regulates protein folding. α-Glucosidase-IN-11 can be used to regulate blood glucose levels.
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- HY-139385A
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MPEG-2000-DSPE sodium
|
Liposome
Parasite
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Cancer
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MPEG-2000-DSPE sodium is a phospholipid PEG conjugate, has both hydrophilicity and hydrophobility. MPEG-2000-DSPE sodium is used in the synthesis of liposomes, increases the hydrophilicity on the surface of liposomes, consequently increasing the longevity of liposomes in the blood circulation for the study of anticancer and antimalarial agents.
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- HY-139385
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MPEG-2000-DSPE
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Liposome
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Cancer
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MPEG-2000-DSPE is a phospholipid PEG conjugate, has both hydrophilicity and hydrophobility. MPEG-2000-DSPE is used in the synthesis of liposomes, increases the hydrophilicity on the surface of liposomes, consequently increasing the longevity of liposomes in the blood circulation for the study of anticancer and antimalarial agents[1][2].
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- HY-109058
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Firibastat
QGC001; RB150
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Aminopeptidase
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Cardiovascular Disease
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Firibastat (QGC001), an orally active brain penetrating proagent of EC33, is a first-in-class brain aminopeptidase A (APA) inhibitor (Ki=200 nM). Firibastat selectively and specifically inhibits conversion of brain angiotensin-II into angiotensin-III and decreases blood pressure in hypertensive rats.
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- HY-W014394
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Vanillyl butyl ether
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Others
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Cardiovascular Disease
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Vanillyl butyl ether is a major contributor to the characteristic flavor and fragrance of vanilla. Vanillyl butyl ether is one of the eco-friendly and nontoxic substances. Vanillyl butyl ether has been proposed as a mild warming agent providing a warming sensation and enhancing the blood circulation.
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- HY-B0259
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Indapamide
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Potassium Channel
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Cardiovascular Disease
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Indapamide is an orally active sulphonamide diuretic agent, that can reduce blood pressure by decreasing vascular reactivity and peripheral vascular resistance. Indapamide is also can reduce left ventricular hypertrophy.
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- HY-136185
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- HY-106991A
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Amustaline dihydrochloride
S-303 dihydrochloride
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HIV
Bacterial
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Infection
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Amustaline (S-303) dihydrochloride, a nucleic acid-targeted alkylator, is an efficient pathogen inactivation agent for blood components containing red blood cells. Amustaline dihydrochloride has three components: an acridine anchor (an intercalator that targets nucleic acids non-covalently), an effector (a bis-alkylator group that reacts with nucleophiles), and a linker (a small flexible carbon chain containing a labile ester bond that hydrolyzes at neutral pH to yield non-reactive breakdown products).
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- HY-135674
-
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SR-318
|
p38 MAPK
TNF Receptor
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Cancer
Inflammation/Immunology
|
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SR-318 is a potent and highly selective p38 MAPK inhibitor with IC50s of 5 nM, 32 nM and 6.11 μM for p38α, p38β and p38α/β, respectively. SR-318 potently inhibits the TNF-α release in whole blood with an IC50 of 283 nM. SR-318 has anti-cancer and anti-inflammatory activity.
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- HY-W015007
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Metyrosine
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COX
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Cardiovascular Disease
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Metyrosine is a selective tyrosine hydroxylase enzyme inhibitor. Metyrosine exerts anti-inflammatory and anti-ulcerative effects. Metyrosine significantly inhibits high COX-2 activity. Metyrosine is a very effective agent for blood pressure control.
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- HY-122613
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YM543 free base
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SGLT
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Metabolic Disease
|
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YM543 free base is a potent and orally active sodium-glucose cotransporter (SGLT) 2 inhibitor. YM543 free base reduces blood glucose levels. YM543 free base can be used in research of diabetes.
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- HY-12724A
-
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Guanabenz hydrochloride
|
Parasite
Adrenergic Receptor
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Cardiovascular Disease
|
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Guanabenz hydrochloride is an orally active α-2-adrenoceptor agonist. Guanabenz hydrochloride has antihypertensive effect and antiparasitic activity. Guanabenz hydrochloride interferes ER stress-signalling and has protective effects in cardiac myocytes. Guanabenz hydrochloride also is used for the research of high blood pressure.
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- HY-103433
-
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K579
|
Dipeptidyl Peptidase
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Metabolic Disease
|
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K579 is a potent and orally active dipeptidyl peptidase IV inhibitor. K579 inhibits the blood glucose elevation. K579 increases the plasma insulin and active forms of glucagon-like peptide-1 (GLP-1). K579 has the potential for the research of diabetic.
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- HY-12724
-
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Guanabenz
|
Adrenergic Receptor
Parasite
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Cardiovascular Disease
|
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Guanabenz is an orally active α-2-adrenoceptor agonist. Guanabenz has antihypertensive effect and antiparasitic activity. Guanabenz interferes ER stress-signalling and has protective effects in cardiac myocytes. Guanabenz also is used for the research of high blood pressure.
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- HY-12912
-
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KDU691
|
PI4K
Parasite
|
Infection
|
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KDU691, an imidazopyrazine with potent anti-parasitic activity against blood stage schizonts, gametocytes and liver stages, is a Plasmodium PI4K inhibitor. KDU691 selectively inhibits dihydroartemisinin-pretreated Plasmodium falciparum ring-stage parasites.
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- HY-A0115
-
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- HY-14860A
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- HY-14860
-
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1-Deoxynojirimycin
Duvoglustat
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Glucosidase
PI3K
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Metabolic Disease
|
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1-Deoxynojirimycin (Duvoglustat) is a potent and orally active α-glucosidase inhibitor. 1-Deoxynojirimycin suppresses postprandial blood glucose and is widely used for diabetes mellitus. 1-Deoxynojirimycin possesses antihyperglycemic, anti-obesity, and antiviral features.
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- HY-12378
-
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BQ-123
|
Endothelin Receptor
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Cardiovascular Disease
|
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BQ-123 is a potent and selective endothelin A (ETA) receptor antagonist with an IC50 of 7.3 nM and a Ki of 25 nM. BQ-123 inhibits endothelin-1-mediated proliferation of human pulmonary artery smooth muscle cells and lowers blood pressure in different rat models of hypertension.
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- HY-148189
-
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Aldometanib
LXY-05-029
|
AMPK
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Metabolic Disease
|
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Aldometanib (LXY-05-029) is an orally active aldolase inhibitor. Aldometanib can activate lysosomal adenosine monophosphate-activated protein kinase (AMPK) and decreases blood glucose. Aldometanib can be used for the research of metabolic homeostasis.
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- HY-15344
-
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(R,R)-BD-AcAc 2
(R,R)-Ketone Ester
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Others
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Metabolic Disease
Neurological Disease
|
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(R,R)-BD-AcAc 2 ((R,R)-Ketone Ester), a ketone monoester, can be used as a source of oral nutritional ketones. (R,R)-BD-AcAc 2 can elevate plasma levels of β-hydroxybutyrate and acetoacetate, blood glucose, blood Na + levels and blood creatinine levels after oral administration in mice. (R,R)-BD-AcAc 2 can partly prevent muscle weakness in septic mice. (R,R)-BD-AcAc 2 has potential to improve exercise performance and endurance in animal body. (R,R)-BD-AcAc 2 can also be used to research Parkinson’s disease or diabetes.
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- HY-32018
-
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Cot inhibitor-2
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MAP3K
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Cancer
|
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Cot inhibitor-2 is a potent, selective and orally active cot (Tpl2/MAP3K8) inhibitor with an IC50 of 1.6 nM. Cot inhibitor-2 inhibts TNF-α production in LPS-stimulated human whole blood with an IC50 of 0.3 μM.
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- HY-12378A
-
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BQ-123 TFA
|
Endothelin Receptor
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Cardiovascular Disease
|
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BQ-123 TFA is a potent and selective endothelin A (ETA) receptor antagonist with an IC50 of 7.3 nM and a Ki of 25 nM. BQ-123 TFA inhibits endothelin-1-mediated proliferation of human pulmonary artery smooth muscle cells and lowers blood pressure in different rat models of hypertension.
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- HY-147873
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NMDAR/HDAC-IN-1
|
iGluR
HDAC
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Neurological Disease
|
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NMDAR/HDAC-IN-1 (Compound 9d) is a dual NMDAR and HDAC inhibitor with a Ki of 0.59 μM for NMDAR and IC50 values of 2.67, 8.00, 2.21, 0.18 and 0.62 μM for HDAC1, HDAC2, HDAC3, HDAC6 and HDAC8, respectively. NMDAR/HDAC-IN-1 efficiently penetrates the blood brain barrier.
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- HY-W011297
-
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Methyl arachidonate
Arachidonic acid methyl ester
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Others
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Metabolic Disease
|
|
Methyl arachidonate (Arachidonic acid methyl ester) is a fatty acid methyl ester resulting from the formal condensation of the carboxy group of arachidonic acid with methanol. Methyl arachidonate has activity of human blood serum metabolite.
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- HY-135795
-
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1-Cyclohexyl-3-dodecyl urea
CDU; N-Cyclohexyl-N-dodecyl urea; NCND
|
Epoxide Hydrolase
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Metabolic Disease
Cardiovascular Disease
|
|
1-Cyclohexyl-3-dodecyl urea (CDU; N-Cyclohexyl-N-dodecyl urea; NCND) is a highly selective soluble epoxide hydrolase (sEH) inhibitor. 1-Cyclohexyl-3-dodecyl urea (CDU; N-Cyclohexyl-N-dodecyl urea; NCND) increases epoxyeicosatrienoic acids (EETs) levels and lowers blood pressure in angiotensin II (Ang II) hypertension.
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- HY-148136
-
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sEH inhibitor-7
|
Epoxide Hydrolase
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Inflammation/Immunology
|
|
sEH inhibitor-7 (compound c-2) is an inhibitor of soluble epoxide hydrolase (sEH) with IC50s of 0.15 μM (mouse sEH) and 6.2 μM (human sEH), respectively. soluble epoxide hydrolase (sEH) plays an important role in the metabolism of endogenous chemical mediators involved in the regulation of blood pressure and inflammation.
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- HY-13458
-
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Droxidopa
L-DOPS; DOPS; SM5688
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Adrenergic Receptor
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Neurological Disease
|
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Droxidopa(L-DOPS) is a potent, orally active norepinephrine precursor. Droxidopa increases standing blood pressure, ameliorates symptoms of orthostatic hypotension and improves standing ability. Droxidopa has the potential for the research of neurogenic orthostatic hypotension (nOH) and alternative ADHD (attention deficit hyperactivity disorder).
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- HY-121693
-
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DIDS
|
RAD51
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Cancer
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DIDS is a potent RAD51 inhibitor. DIDS inhibits the RAD51-mediated homologous pairing and strand-exchange reactions. DIDS inhibits anion exchange and binding to the red blood cell membrane.
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- HY-136886
-
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IR-820
New Indocyanine Green
|
Fluorescent Dye
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Cancer
|
|
IR-820 (New Indocyanine Green) is an infrared blood pool contrast agent. IR-820 also is normally used as a laser and near-infrared dye to detect and quantify diseased tissue in live animals.
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- HY-13458A
-
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Droxidopa hydrochloride
L-DOPS hydrochloride; DOPS hydrochloride; SM5688 hydrochloride
|
Adrenergic Receptor
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Neurological Disease
|
|
Droxidopa (L-DOPS) hydrochloride is a potent, orally active norepinephrine precursor. Droxidopa hydrochloride increases standing blood pressure, ameliorates symptoms of orthostatic hypotension and improves standing ability. Droxidopa hydrochloride has the potential for the research of neurogenic orthostatic hypotension (nOH) and alternative ADHD (attention deficit hyperactivity disorder).
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- HY-N11335
-
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Bitis Parviocula Venom
Ethiopian Mountain Adder Venom
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Others
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Cardiovascular Disease
|
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Bitis Parviocula Venom (Ethiopian Mountain Adder Venom) is a venom that can be obtained from the Ethiopian endemic snake of the species Bitis parviocula. Bitis Parviocula Venom contains vasoactive compounds that have a direct effect on blood vessels.
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- HY-14275
-
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Verapamil
(±)-Verapamil; CP-16533-1
|
Calcium Channel
P-glycoprotein
Cytochrome P450
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Metabolic Disease
|
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Verapamil ((±)-Verapamil) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil also inhibits CYP3A4. Verapamil has the potential for high blood pressure, heart arrhythmias and angina research.
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- HY-A0064
-
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Verapamil hydrochloride
(±)-Verapamil hydrochloride; CP-16533-1 hydrochloride
|
Calcium Channel
P-glycoprotein
Cytochrome P450
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Cardiovascular Disease
|
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Verapamil hydrochloride ((±)-Verapamil hydrochloride) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil hydrochloride also inhibits CYP3A4. Verapamil hydrochloride has the potential for high blood pressure, heart arrhythmias and angina research.
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- HY-N0293
-
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Paeoniflorin
Peoniflorin
|
HSP
|
Cancer
Infection
Neurological Disease
|
|
Paeoniflorin is a heat shock protein-inducing compound and commonly exists in the plants of Paeoniaceae family, with various biological activities, including anticancer activity, anti-inflammatory activity, enhancing cognition and attenuating learning impairment, anti-oxidative stress, antiplatelet aggregation, expansion of blood vessels, and reducing blood viscosity.
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- HY-105276
-
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Enalkiren
A-64662
|
Renin
|
Cardiovascular Disease
|
|
Enalkiren (A-64662) is a potent dipeptide renin inhibitor with an IC50 of 0.78 nM in a purified renal renin-angiotensinogen system (pH=6.0). Enalkiren suppresses renin activity, and also reduces systolic and diastolic blood pressure. Enalkiren can be used to research essential hypertension.
|
-
- HY-101059
-
|
FGIN 1-27
|
Others
|
Neurological Disease
|
|
FGIN 1-27, an indoleacetamide, is a specific peripheral benzodiazepine receptor (PBR) ligand with a Ki of 5.0 nM. FGIN 1-27 can penetrate the blood brain barrier (BBB). FGIN 1-27 inhibits the onset of Isoniazid-induced convulsions.
|
-
- HY-144446
-
|
BuChE-IN-1
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
BuChE-IN-1 (Compound 23) is a potent inhibitor of butyrylcholinesterase (BuChE). Butyrylcholinesterase (BuChE) is recently regarded as a biomarker in progressed Alzheimer’s disease (AD). BuChE-IN-1 shows low cytotoxicity and high blood brain barrier (BBB) permeability. BuChE-IN-1 is a promising BuChE inhibitor for the research of AD.
|
-
- HY-151368
-
|
AChE/BChE-IN-10
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
AChE/BChE-IN-10 (Compound 7b) is a potent dual AChE and BChE inhibitor with IC50 values of 0.176, and 0.47 μM, respectively. AChE/BChE-IN-10 shows good blood brain barrier permeability. AChE/BChE-IN-10 can inhibit Aβ-aggregation and be used in Alzheimer’s disease (AD) research.
|
-
- HY-103697
-
|
Gardiquimod
|
Toll-like Receptor (TLR)
HIV
|
Cancer
Infection
|
|
Gardiquimod, an imidazoquinoline analog, is a TLR7/8 agonist. Gardiquimod could inhibit HIV-1 infection of macrophages and activated peripheral blood mononuclear cells (PBMCs). Gardiquimod specifically activates TLR7 when used at concentrations below 10 μM.
|
-
- HY-B0475
-
-
- HY-123983
-
|
HS56
|
Pim
DAPK
|
Cardiovascular Disease
|
|
HS56 is an ATP-competitive dual Pim/DAPK3 inhibitor with Ki values of 0.26, 0.208, 2.94, and ＞100 μM for DAPK3, Pim-3, Pim-1, and Pim-2, respectively. HS56 inhibits LC20 phosphorylation and smooth muscle contraction. HS56 decreases blood pressure in spontaneously hypertensive mice. HS56 can be used in research of hypertension.
|
-
- HY-B0228
-
-
- HY-B0804
-
|
Nadolol
SQ-11725
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Nadolol (SQ-11725) is a non-selective and orally active β-adrenergic receptors blocker and is a substrate of organic anion transporting polypeptide 1A2 (OATP1A2). Nadolol has the the potential for high blood pressure, angina pectoris and vascular headaches research.
|
-
- HY-102064
-
|
SR 57227A
|
5-HT Receptor
|
Neurological Disease
|
|
SR 57227A is a potent, orally active and selective 5-HT3 receptor agonist, with ability to cross the blood brain barrier. SR 57227A has affinities (IC50) varying between 2.8 and 250 nM for 5-HT3 receptor binding sites in rat cortical membranes and on whole NG 108-15 cells or their membranes. Anti-depressant effects.
|
-
- HY-103697A
-
|
Gardiquimod diTFA
|
Toll-like Receptor (TLR)
HIV
|
Cancer
Infection
|
|
Gardiquimod diTFA, an imidazoquinoline analog, is a TLR7/8 agonist. Gardiquimod diTFA could inhibit HIV-1 infection of macrophages and activated peripheral blood mononuclear cells (PBMCs). Gardiquimod diTFA specifically activates TLR7 when used at concentrations below 10 μM.
|
-
- HY-108482
-
-
- HY-P1323
-
-
- HY-118284
-
|
Vicagrel
|
P2Y Receptor
|
Cardiovascular Disease
|
|
Vicagrel is a potent, safe and orally active antiplatelet agent, which works by irreversibly inhibiting P2Y12 receptor. Vicagrel can be used for the research of blood clots in coronary artery disease, peripheral vascular disease, and cerebrovascular disease.
|
-
- HY-103210
-
|
DSP-4 hydrochloride
Neurotoxin DSP 4 hydrochloride
|
Others
|
Neurological Disease
|
|
DSP-4 hydrochloride is a highly and selective adrenergic neurotoxin. DSP-4 hydrochloride can cross the blood brain barrier. DSP-4 hydrochloride can be used for the temporary selective degradation of the central and peripheral noradrenergic neurons.
|
-
- HY-P1271
-
|
Catestatin
|
nAChR
|
Cardiovascular Disease
|
|
Catestatin is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin is an endogenous peptide that regulates cardiac function and blood pressure. Catestatin is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release.
|
-
- HY-P1323A
-
-
- HY-17459
-
|
Clopidogrel hydrogen sulfate
(S)-(+)-Clopidogrel bisulfate; (S)-(+)-Clopidogrel hydrogen sulfate
|
Cytochrome P450
P2Y Receptor
|
Cardiovascular Disease
Cancer
|
|
Clopidogrel hydrogen sulfate is an antiplatelet agent to prevent blood clots. Clopidogrel hydrogen sulfate inhibits CYP2B6 and CYP2C19 with IC50s of 18.2 nM and 524 nM, respectively. Clopidogrel hydrogen sulfate is a potent antithrombotic agent that inhibits ADP-induced platelet aggregation．Clopidogrel hydrogen sulfate also is an orally active P2Y(12) inhibitor.
|
-
- HY-120295
-
|
A-192621
|
Endothelin Receptor
Apoptosis
|
Endocrinology
Cardiovascular Disease
|
|
A-192621 is a potent, nonpeptide, orally active and selective endothelin B (ETB) receptor antagonist with an IC50 of 4.5 nM and a Ki of 8.8 nM. The selectivity of A-192621 is 636-fold higher than ETA (IC50 of 4280 nM and Ki of 5600 nM). A-192621 promotes apoptosis in PASMCs. A-192621 alos causes elevation of arterial blood pressure and an elevation in the plasma ET-1 level.
|
-
- HY-118941
-
|
BAY 73-1449
|
Prostaglandin Receptor
|
Cardiovascular Disease
|
|
BAY 73-1449 is a selective antagonist of prostacyclin receptor (IP), with high potency (IC50 of less than 0.1 nM) in cAMP assays in Human HEL cells and rat DRG. BAY 73-1449 can be used in the research of lowering blood pressure.
|
-
- HY-P1271A
-
|
Catestatin TFA
|
nAChR
|
Cardiovascular Disease
|
|
Catestatin TFA is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin TFA is an endogenous peptide that regulates cardiac function and blood pressure. Catestatin TFA is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release.
|
-
- HY-B0007
-
|
Baclofen
|
GABA Receptor
|
Neurological Disease
|
|
Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABAB receptor (GABABR) agonist. Baclofen mimics the action of GABA and produces slow presynaptic inhibition through the GABAB receptor. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research.
|
-
- HY-B0007C
-
|
Baclofen hydrochloride
|
GABA Receptor
|
Neurological Disease
|
|
Baclofen hydrochloride, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABAB receptor (GABABR) agonist. Baclofen hydrochloride mimics the action of GABA and produces slow presynaptic inhibition through the GABAB receptor. Baclofen hydrochloride has high blood brain barrier penetrance. Baclofen hydrochloride has the potential for muscle spasticity research.
|
-
- HY-151138
-
-
- HY-N0148
-
|
Rutin
Rutoside; Quercetin 3-O-rutinoside
|
Amyloid-β
Autophagy
Apoptosis
Endogenous Metabolite
|
Inflammation/Immunology
Cancer
|
|
Rutin (Rutoside) is a flavonoid found in many plants and shows a wide range of biological activities including anti-inflammatory, antidiabetic, antioxidant, neuroprotective, nephroprotective, hepatoprotective and reducing Aβ oligomer activities. Rutin can cross the blood brain barrier. Rutin attenuates vancomycin-induced renal tubular cell apoptosis via suppression of apoptosis, mitochondrial dysfunction, and oxidative stress.
|
-
- HY-N0148A
-
|
Rutin hydrate
Rutoside hydrate; Quercetin 3-O-rutinoside hydrate
|
Amyloid-β
Autophagy
Apoptosis
Endogenous Metabolite
|
Cancer
Neurological Disease
|
|
Rutin (Rutoside) hydrate is a flavonoid found in many plants and shows a wide range of biological activities including anti-inflammatory, antidiabetic, antioxidant, neuroprotective, nephroprotective, hepatoprotective and reducing Aβ oligomer activities. Rutin hydrate can cross the blood brain barrier. Rutin hydrate attenuates vancomycin-induced renal tubular cell apoptosis via suppression of apoptosis, mitochondrial dysfunction, and oxidative stress.
|
-
- HY-123410
-
|
KM-233
|
Cannabinoid Receptor
|
Cancer
|
|
KM-233 is a classical cannabinoid with good blood brain barrier penetration. KM-233 possesses a selective affinity for the CB2 receptors relative to THC. KM-233 is effective at reducing U87 glioma tumor burden, and can be used for glioma research.
|
-
- HY-N1050
-
|
Zederone
|
mTOR
|
Cancer
|
|
Zederone, a germacrane-type sesquiterpene, has potently cytotoxic against human white blood cancer cells and human prostate cancer cells. Zederone significantly inhibits the proliferation and downregulates the protein expressions of mTOR, and phosphorylated p70 S6 kinase (p-p70s6K) in SKOV3 cells.
|
-
- HY-136910
-
|
USP7-IN-7
|
Deubiquitinase
|
Cancer
|
|
USP7-IN-7 (compound 124) is a USP7 inhibitor with an IC50 value ＜10 nM. USP7-IN-7 shows cytotoxicity against p53-mutant cancer cell lines, p53 wild-type blood cancer and neuroblastoma cell lines with low nanomolar values. USP7-IN-7 can be used for cancer research.
|
-
- HY-W033577
-
|
Tricarbonyldichlororuthenium(II) dimer
CORM-2
|
Others
|
Inflammation/Immunology
|
|
Tricarbonyldichlororuthenium(II) dimer is a pharmacological donor of CO releasing. CO releases from Tricarbonyldichlororuthenium(II) dimer prevents gastric mucosal oxidative damage induced by ischemia/reperfusion (I/R) improving gastric blood flow (GBF), decreasing DNA oxidation and inflammatory response on systemic level.
|
-
- HY-B0007S
-
|
Baclofen-d4
|
GABA Receptor
|
Neurological Disease
|
|
Baclofen-d4 is the deuterium labeled Baclofen. Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABAB receptor (GABABR) agonist. Baclofen mimics the action of GABA and produces slow presynaptic inhibition through the GABAB receptor. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research[1][2][3].
|
-
- HY-103190
-
|
MRS1220
|
Adenosine Receptor
|
Cancer
Neurological Disease
|
|
MRS1220, a highly potent and selective human A3 adenosine receptor (hA3AR) antagonist with a Ki of 0.59 nM, has therapeutic potential for the research of diseases of the central nervous system. MRS1220 reduces glioblastoma tumor size and blood vessel formation in vivo.
|
-
- HY-118250
-
|
GSK2245035
|
Toll-like Receptor (TLR)
IFNAR
TNF Receptor
|
Inflammation/Immunology
|
|
GSK2245035 is a highly potent and selective intranasal Toll-Like receptor 7 (TLR7) agonist with preferential Type-1 interferon (IFN)-stimulating properties. GSK2245035 has pEC50s of 9.3 and 6.5 for IFNα and TFNα. GSK2245035 effectively suppresses allergen-induced Th2 cytokine production in human peripheral blood cell cultures. GSK2245035 is used for asthma.
|
-
- HY-B0824
-
|
Bifenthrin
|
Sodium Channel
|
Neurological Disease
|
|
Bifenthrin is a synthetic pyrethroid insecticide. Bifenthrin prolongs the opening time of Nav1.8 sodium channels, leading to membrane depolarization and conductance block in the insect nervous system, thereby disrupting neural function. Bifenthrin was effective in inhibiting A. gambiae (LD50=0.15 ng/mg) and C. quinquefasciatus (LD50=0.16 ng/mg). Bifenthrin has good lethality against susceptible and resistant mosquitoes and is very effective in inhibiting blood sucking and can be developed as a mosquito-removal netting material.
|
-
- HY-B0362A
-
|
Phentolamine mesylate
Phentolamine methanesulfonate
|
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Phentolamine mesylate (Phentolamine methanesulfonate) is a reversible, non-selective, and orally active blocker of α1 and α2 adrenergic receptor that expands blood vessels to reduce peripheral vascular resistance. Phentolamine mesylate can be used for the research of pheochromocytoma-related hypertension, heart failure and erectile dysfunction.
|
-
- HY-N8189
-
-
- HY-139781
-
|
PD-L1-IN-1
|
PD-1/PD-L1
|
Cancer
|
|
PD-L1-IN-1 is a potent PD-L1 inhibitor with an IC50 of 115 nM. PD-L1-IN-1 strongly binds with the PD-L1 protein and challenged it in a co-culture of PD-L1 expressing cancer cells (PC9 and HCC827 cells) and peripheral blood mononuclear cells enhanced antitumor immune activity of the latter. PD-L1-IN-1 significantly increased interferon γ release and apoptotic induction of cancer cells, with low cytotoxicity in healthy cells.
|
-
- HY-15306
-
|
Eltrombopag
SB-497115
|
Thrombopoietin Receptor
Bacterial
Apoptosis
|
Cancer
Infection
Cardiovascular Disease
|
|
Eltrombopag (SB-497115) is an orally active thrombopoietin receptor nonpeptide agonist. Eltrombopag owns thrombopoietic activity, and has been used to research low blood platelet counts with chronic immune thrombocytopenia. Eltrombopag can be used for the research of cardiovascular. Eltrombopag also has highly inhibitory effects against multidrug resistant Staphylococcus aureus. Eltrombopag can induce apoptosis in hepatocellular carcinomab (HCC) as well.
|
-
- HY-123348
-
-
- HY-15306A
-
|
Eltrombopag Olamine
Eltrombopag diethanolamine salt; SB-497115GR
|
Thrombopoietin Receptor
Bacterial
Apoptosis
|
Cancer
Infection
Cardiovascular Disease
|
|
Eltrombopag Olamine (Eltrombopag diethanolamine salt) is an orally active thrombopoietin receptor nonpeptide agonist. Eltrombopag Olamine owns thrombopoietic activity, and has been used to research low blood platelet counts with chronic immune thrombocytopenia. Eltrombopag Olamine can be used for the research of cardiovascular. Eltrombopag Olamine also has highly inhibitory effects against multidrug resistant Staphylococcus aureus. Eltrombopag Olamine can induce apoptosis in hepatocellular carcinomab (HCC) as well.
|
-
- HY-120878
-
|
CXCR2-IN-2
|
CXCR
|
Inflammation/Immunology
|
|
CXCR2-IN-2 is a selective, brain penetrant, and orally bioavailable CXCR2 antagonist (IC50=5.2 nM/1 nM in β-arrestin assay/CXCR2 Tango assay, respectively). CXCR2-IN-2 displays ~730-fold selectivity over CXCR1 and >1900-fold selectivity over all other chemokine receptors. CXCR2-IN-2 inhibits human whole blood Gro-α induced CD11b expression with an IC50 of 0.04 μM.
|
-
- HY-U00147
-
-
- HY-13779
-
|
J-147
|
Monoamine Oxidase
Dopamine Transporter
|
Neurological Disease
|
|
J-147 is an exceptionally potent, orally active, neuroprotective agent for cognitive enhancement. J-147 can readily pass the blood brain barrier (BBB). J-147 can inhibit monoamine oxidase B (MAO B) and the dopamine transporter with EC50 values of 1.88 μM and 0.649 μM, respectively. J-147 has potential for the treatment of Alzheimer’s disease (AD).
|
-
- HY-P3624
-
|
Cenderitide
|
Guanylate Cyclase
|
Cardiovascular Disease
|
|
Cenderitide is a potent agonist of particulate guanylyl cyclase receptor (pGC). Cenderitide is a natriuretic peptide (NP) composed of C-type natriuretic peptide (CNP) fused to the C-terminus of Dendroaspis natriuretic peptide (DNP). Cenderitide activates both pGC-A and pGC-B, activates the second messenger cGMP, suppresses aldosterone, and preserves GFR without reducing blood pressure. Cenderitide can be used for heart failure research.
|
-
- HY-109556
-
|
Insulin Detemir
|
Akt
ERK
|
Metabolic Disease
|
|
Insulin Detemir is an artificial insulin, shows effect on controlling blood sugar levels. Insulin Detemir stimulates GLP-1 secretion as a consequence of enhanced Gcg expression by a mechanism involving activation of Akt- and/or extracellular signal-regulated kinase (ERK)-dependent-cat and CREB signaling pathways. Insulin Detemir can be used for type 2 diabetes research.
|
-
- HY-16276A
-
|
Osilodrostat phosphate
LCI699 phosphate
|
Mineralocorticoid Receptor
|
Cancer
|
|
Osilodrostat (LCI699) phosphate is a potent, orally active11β-hydroxylase (CYP11B1) inhibitor with an IC50 value of 35 nM. Osilodrostat phosphate is a potent, orally aldosterone synthase (CYP11B2) inhibitor with IC50 values of 0.7 nM and 160 nM for human aldosterone synthase and rat aldosterone synthase, respectively. Osilodrostat phosphate inhibits aldosterone and corticosterone synthesis. Osilodrostat phosphate has blood pressure lowering ability. Osilodrostat phosphate can be used for research of Cushing syndrome (CS).
|
-
- HY-16276
-
|
Osilodrostat
LCI699
|
Mineralocorticoid Receptor
|
Cancer
Inflammation/Immunology
|
|
Osilodrostat (LCI699) is a potent, orally active11β-hydroxylase (CYP11B1) inhibitor with an IC50 value of 35 nM. Osilodrostat is a potent, orally aldosterone synthase (CYP11B2) inhibitor with IC50 values of 0.7 nM and 160 nM for human aldosterone synthase and rat aldosterone synthase, respectively. Osilodrostat inhibits aldosterone and corticosterone synthesis. Osilodrostat has blood pressure lowering ability. Osilodrostat can be used for research of Cushing syndrome (CS).
|
-
- HY-145552
-
|
Azilsartan mepixetil
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
Azilsartan mepixetil is the antagonist of angiotensin II receptor. Azilsartan mepixetil has stronger and longer blood pressure effect, more abvious and longer lasting heart rate lowering effect and high safety. Azilsartan mepixetil achieves ideal protective effect for heart and kidney functions. Azilsartan mepixetil has the potential for the research of hypertension, chronic heart failure and diabetic nephropathy (extracted from patent CN107400122A).
|
-
- HY-105559A
-
-
- HY-105559
-
-
- HY-B0665
-
|
Fibrin
|
Others
|
Cardiovascular Disease
Cancer
|
|
Fibrin, isolated from bovine blood, is an insoluble protein produced in response to bleeding. Fibrin is the major component of the blood clot and is used for coagulation.
|
-
- HY-B0202S2
-
|
Irbesartan-d6-1
|
Apoptosis
Angiotensin Receptor
|
|
|
Irbesartan-d6-1 is the deuterium labeled Irbesartan[1]. Irbesartan (SR-47436) is an orally active Ang II type 1 (AT1) receptor blocker (ARB). Irbesartan can relax the blood vessels, low blood pressure and increase the supply of blood and oxygen to the heart. Irbesartan can be used for the research of high blood pressure, heart failure, and diabetic kidney disease[2].
|
-
- HY-126233
-
-
- HY-B0315
-
-
- HY-B0642
-
-
- HY-108844
-
|
Rasburicase
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Rasburicase is a recombinant urate oxidase and a hyperuricemia inhibitor. Rasburicase converts uric acid into allantoin, making it easier to be cleared by the kidneys and improving the elevated level of uric acid in the blood.
|
-
- HY-148322
-
|
Sirtuin modulator 5
|
Sirtuin
|
Cancer
Infection
Metabolic Disease
Inflammation/Immunology
Neurological Disease
|
|
Sirtuin modulator 5 is a sirtuin modulating agent. Sirtuin modulator 5 can activate SIRT1 with a DC50 value of <50 μM. Sirtuin modulator 5 can be used for increasing the lifespan of a cell and used for the research of variety of diseases including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benfit from increased mitochondrial activity.
|
-
- HY-N0298
-
-
- HY-107863
-
-
- HY-N7971
-
-
- HY-B0315A
-
-
- HY-N10896
-
-
- HY-B0193A
-
|
Prazosin hydrochloride
|
Adrenergic Receptor
Autophagy
|
Cardiovascular Disease
Endocrinology
Cancer
|
|
Prazosin hydrochloride is a well-tolerated, CNS-active α1-adrenergic receptor antagonist for the research of high blood pressure and alcohol use disorders. Prazosin hydrochloride potently inhibits Norepinephrine (NE)-stimulated 45Ca efflux with an IC50 of 0.15 nM.Prazosin hydrochloride inhibits organic cation transporters OCT-1 and OCT-3 with IC50s of 1.8, and 13 μM, respectively.
|
-
- HY-B0523B
-
|
Anagrelide hydrochloride monohydrate
|
Phosphodiesterase (PDE)
|
Others
|
|
Anagrelide hydrochloride monohydrate is a imidazoquinazoline agent. Anagrelide hydrochloride monohydrate decreases the level of platelets in blood, prevents blood clots formation. Anagrelide hydrochloride monohydrate can be used for research of essential thrombocythaemia (ET) and thrombocythaemia associated with polycythaemia vera (PV).
|
-
- HY-101952
-
-
- HY-113098
-
-
- HY-101701
-
-
- HY-W011552
-
-
- HY-B1226
-
-
- HY-D0954
-
|
Jenner's Stain
|
Fluorescent Dye
|
Others
|
|
Jenner's Stain is a dye that is used in microscopy for staining blood smears. Jenner's Stain can be used for the chromosome stain by C-banding technique. Jenner's Stain can be used for the stain for routine blood examinations and malarial staining.
|
-
- HY-15874A
-
|
Fiboflapon sodium
GSK2190915 sodium salt; AM-803 sodium
|
FLAP
Leukotriene Receptor
|
Inflammation/Immunology
|
|
Fiboflapon sodium (GSK2190915; AM-803) is a potent and orally bioavailable 5-lipoxygenase-activating protein (FLAP) inhibitor with a potency of 2.9 nM in FLAP binding, an IC50 of 76 nM for inhibition of LTB4 in human blood.
|
-
- HY-15874
-
|
Fiboflapon
GSK2190915; AM-803
|
FLAP
Leukotriene Receptor
|
Inflammation/Immunology
|
|
Fiboflapon (GSK2190915; AM-803) is a potent and orally bioavailable 5-lipoxygenase-activating protein (FLAP) inhibitor with a potency of 2.9 nM in FLAP binding, an IC50 of 76 nM for inhibition of LTB4 in human blood.
|
-
- HY-113236
-
-
- HY-B2158
-
-
- HY-B1209
-
|
Etofylline
7-(β-Hydroxyethyl)theophylline
|
Others
|
Cardiovascular Disease
|
|
Etofylline (7-(β-Hydroxyethyl)theophylline) is a N-7-substituted derivative of Theophylline. Etofylline is a bronchodilator which can be used for the research of asthma. Etofylline is also an anticholesteremic and reduces total cholesterol level in the blood.
|
-
- HY-B1231
-
-
- HY-B1236
-
-
- HY-B1448
-
-
- HY-128757
-
|
Remibrutinib
|
Btk
|
Inflammation/Immunology
|
|
Remibrutinib, is a potent and orally active bruton tyrosine kinase (BTK) inhibitor with an IC50 value of 1 nM. Remibrutinib inhibits BTK activity with an IC50 value of 0.023 μM in blood. Remibrutinib has the potential for Chronic urticaria (CU) treatment.
|
-
- HY-B0315S
-
-
- HY-148529
-
|
Midaglizole
(±)-DG5128 free base; DG5128 free base
|
Adrenergic Receptor
|
Metabolic Disease
|
|
Midaglizole ((±)-DG5128 free base, DG5128 free base) is a potent α2-adrenoceptor antagonist. Midaglizole is a hypoglycemic agent. Midaglizole increases blood pressure and reduces blood glucose levels in vivo.
|
-
- HY-146286
-
|
Anticancer agent 44
|
Apoptosis
|
Cancer
|
|
Anticancer agent 44 (compound 2a) is a potent anticancer agent. Anticancer agent 44 shows cytotoxicity activity in cancer cells. Anticancer agent 44 induces apoptosis. Anticancer agent 44 shows low toxicity towards activated lymphocytes of human blood.
|
-
- HY-113094
-
-
- HY-B1206
-
-
- HY-B0920
-
-
- HY-B0564
-
-
- HY-147409
-
|
Ulecaciclib
|
CDK
|
Cancer
|
|
Ulecaciclib is an orally activitive inhibitor of cyclin-dependent kinase (CDK), with Ki values of 0.62 μM (CDK2/Cyclin A), 0.2 nM (CDK4/Cyclin D1), 3 nM (CDK6/Cyclin D3), and 0.63 μM (CDK7/Cyclin H), respectively. Ulecaciclib can cross blood brain barrier and has good pharmacokinetic characteristics.
|
-
- HY-N2101
-
|
Benzoyloxypaeoniflorin
|
Tyrosinase
NF-κB
|
Inflammation/Immunology
|
|
Benzoyloxypaeoniflorin, isolated from the root of Paeonia suffruticosa, is a tyrosinase inhibitor against mushroom tyrosinase with IC50 of 0.453 mM. Benzoyloxypaeoniflorin is NF-κB Inhibitor and contributes to improving blood circulation through its inhibitory effect on both platelet aggregation and blood coagulation.
|
-
- HY-146290
-
|
Anticancer agent 45
|
Apoptosis
|
Cancer
|
|
Anticancer agent 46 (compound 2b) is a potent and selective anticancer agent. Anticancer agent 46 shows cytotoxicity activity in cancer cells. Anticancer agent 46 induces apoptosis. Anticancer agent 46 shows low toxicity towards activated lymphocytes of human blood.
|
-
- HY-B0093
-
-
- HY-B1108
-
-
- HY-N0684
-
-
- HY-B0093A
-
-
- HY-N7004
-
-
- HY-103293
-
-
- HY-B2158S
-
|
Chlorotrianisene-d9
|
Estrogen Receptor/ERR
COX
|
Endocrinology
Cardiovascular Disease
|
|
Chlorotrianisene-d9 is the deuterium labeled Chlorotrianisene. Chlorotrianisene is a long-acting non-steroidal estrogen and an orally active estrogen receptor modulator. Chlorotrianisene exhibits antiestrogenic activity. Chlorotrianisene potently inhibits the enzyme COX-1 and inhibits platelet aggregation in whole blood[1][2][3].
|
-
- HY-B0266
-
-
- HY-101109
-
-
- HY-110281
-
-
- HY-N1505
-
-
- HY-18738
-
-
- HY-B0612ES
-
-
- HY-D1479
-
-
- HY-148145
-
-
- HY-106416
-
-
- HY-A0168
-
|
Regadenoson
CVT-3146
|
Adenosine Receptor
|
Cardiovascular Disease
|
|
Regadenoson (CVT-3146) is a selective A2A adenosine receptor agonist and vasodilator that increases coronary blood flow, can be used in study of myocardial perfusion imaging. Regadenoson also increases the permeability of the blood-brain barrier (BBB) in rodents, can be used to study increased delivery of agents to the human CNS.
|
-
- HY-119624
-
|
MOMIPP
|
PIKfyve
|
Cancer
|
|
MOMIPP, a macropinocytosis inducer, is a PIKfyve inhibitor. MOMIPP penetrates the blood-brain barrier (BBB).
|
-
- HY-B1435
-
-
- HY-W010031
-
-
- HY-B0209
-
-
- HY-101952S1
-
-
- HY-B0309S1
-
|
Felodipine-d5
|
Calcium Channel
Autophagy
|
Cardiovascular Disease
|
|
Felodipine-d5 is deuterium labeled Felodipine. Felodipine, a dihydropyridine, is a potent, vasoselective calcium channel antagonist. Felodipine lowers blood pressure (BP) by selective action on vascular smooth muscle, especially in the resistance vessels. Felodipine, an anti-hypertensive agent, induces autophagy. Felodipine can cross the blood-brain barrier[1][2][3].
|
-
- HY-B0371S
-
|
Terazosin-d8
|
Adrenergic Receptor
|
Metabolic Disease
Endocrinology
|
|
Terazosin-d8 is deuterium labeled Terazosin. Terazosin is a quinazoline derivative and a competitive and orally active α1-adrenoceptor antagonist. Terazosin works by relaxing blood vessels and the opening of the bladder. Terazosin has the potential for benign prostatic hyperplasia (BPH) and high blood pressure treatment[1][2][3].
|
-
- HY-B0309S2
-
|
Felodipine-d3
|
Calcium Channel
Autophagy
|
Cardiovascular Disease
|
|
Felodipine-d3 is the deuterium labeled Felodipine. Felodipine, a dihydropyridine, is a potent, vasoselective calcium channel antagonist. Felodipine lowers blood pressure (BP) by selective action on vascular smooth muscle, especially in the resistance vessels. Felodipine, an anti-hypertensive agent, induces autophagy. Felodipine can cross the blood-brain barrier[1][2][3].
|
-
- HY-101952S
-
-
- HY-B0787
-
-
- HY-133608
-
-
- HY-B1508
-
-
- HY-144007
-
|
Chol-PEG
|
Liposome
|
Others
|
|
Chol-PEG is a nonionic surfactant vesicles and can be used for a blood-persistent drug delivery system.
|
-
- HY-N1503
-
-
- HY-N1449
-
|
Neonuezhenide
|
Others
|
Others
|
|
Neonuezhenide exhibits strong antioxidant effect against hemolysis of red blood cells induced by free radicals.
|
-
- HY-W016823
-
-
- HY-125437
-
-
- HY-W007606
-
-
- HY-13344A
-
-
- HY-N0318
-
-
- HY-17591
-
-
- HY-122489
-
-
- HY-B0193
-
-
- HY-13344
-
-
- HY-N0640
-
|
Kuromanin chloride
Chrysontemin; Cyanidin 3-O-glucoside chloride
|
Others
|
Metabolic Disease
|
|
Kuromanin (chloride), extracted from mulberry leaves, has been shown to improve blood glucose concentrations and lipid homeostasis and to reduce obesity.
|
-
- HY-110256
-
-
- HY-107663
-
|
MIF-1
Pro-Leu-Gly-NH2; Melanostatin
|
Dopamine Receptor
|
Neurological Disease
|
|
MIF-1 (Melanostatin), an endogenous brain peptide, is a potent dopamine receptor allosteric modulator. MIF-1 inhibits melanin formation. MIF-1 blocks the effects of opioid receptor activation to modulate the analgesic effects. MIF-1 accesses from the blood to the CNS by directly crossing the blood-brain barrier (BBB).
|
-
- HY-15321S2
-
|
Etoricoxib-d3
MK-0663-d3; L-791456-d3
|
COX
|
|
|
Etoricoxib-d3 is the deuterium labeled Etoricoxib[1]. Etoricoxib (MK-0663) is a non steroidal anti-inflammatory agent, acting as a selective and orally active COX-2 inhibitor, with IC50s of 1.1 μM and 116 μM for COX-2 and COX-1 in human whole blood[2][3][4].
|
-
- HY-11054
-
|
TH-237A
meso-GS 164
|
Others
|
Neurological Disease
|
|
TH-237A(meso-GS 164) is a novel neuroprotective agent exhibiting favorable permeation across the blood brain barrier.
|
-
- HY-P4191
-
|
Met-RANTES (human)
MSPYSSDTTPCCFAYIARPLPRAHIKEYFYTSGKCSN
|
CCR
|
Others
|
|
Met-RANTES (human) is a partial antagonist of CCR5. Met-RANTES (human) reduces the infiltration of blood monocytes into the liver.
|
-
- HY-100244
-
-
- HY-B2172
-
-
- HY-B1028
-
|
Pantethine
D-Pantethine; LBF disulfide
|
Endogenous Metabolite
|
Others
|
|
Pantethine is a dimeric form of pantothenic acid, is an intermediate in the production of Coenzyme A, is available as a dietary supplement, and is used to treat acne and improve the blood-cholesterol profile.
|
-
- HY-113313S
-
-
- HY-113293
-
-
- HY-132670S
-
|
(R)-(-)-Felodipine-d5
|
Calcium Channel
Autophagy
|
Cardiovascular Disease
|
|
(R)-(-)-Felodipine-d5 is the deuterium labeled (R)-(-)-Felodipine. (R)-(-)-Felodipine is the S enantiomer of Felodipine. Felodipine, a dihydropyridine, is a potent, vasoselective calcium channel antagonist. Felodipine lowers blood pressure (BP) by selective action on vascular smooth muscle, especially in the resistance vessels. Felodipine, an anti-hypertensive agent, induces autophagy. Felodipine can cross the blood-brain barrier[1][2][3].
|
-
- HY-P0005
-
|
Glucagon (Human)
Glukagon; Hyperglycemic-glycogenolytic factor
|
Others
|
Metabolic Disease
|
|
Glucagon exhibits marked effects on protein and amino acid metabolism. Glucagon inhibits the incorporation of amino acids into protein of liver, muscle, and pancreas, to increase excretion of nitrogen, to promote hepatic urea synthesis, and to increase the concentration of hepatic transaminases and urea cycle enzymes. Glucagon can promote the hepatic uptake of amino acids, to enhance their incorporation into liver glycogen, and to depress the concentration of amino acids in blood.
|
-
- HY-150012
-
-
- HY-12763
-
|
GNE-317
|
PI3K
mTOR
|
Cancer
|
|
GNE-317 is a PI3K/mTOR inhibitor, is able to cross the blood-brain barrier (BBB).
|
-
- HY-113318
-
-
- HY-113434
-
-
- HY-N0483
-
|
Phillygenin
Phillygenol; Epipinoresinol methyl ether; (+)-Phillygenin
|
Reactive Oxygen Species
|
Others
|
|
Phillygenin (Phillygenol) is an active ingredient from Forsythia with many medicinal properties, such as antioxidant, reducing blood lipid, inhibition of low density lipoprotein oxidation.
|
-
- HY-N7148A
-
-
- HY-151143
-
-
- HY-120401
-
-
- HY-120797
-
|
CRT0273750
|
LPL Receptor
|
Cancer
|
|
CRT0273750 is an autotaxin (ATX) inhibitor and modulates LPA levels in plasm (IC50 = 0.014 μM). CRT0273750 can be used in ATX/LPA-dependent models of cancer.
|
-
- HY-P3608
-
|
[Des-His1,Glu9] Glucagon
|
GCGR
|
Metabolic Disease
|
|
[Des-His1,Glu9] Glucagon is a potent glucagon receptor system peptide antagonist. [Des-His1,Glu9] Glucagon enhances the glucose-stimulated release of insulin from pancreatic islet cells. [Des-His1,Glu9] Glucagon can be used to research diabetes.
|
-
- HY-17447
-
-
- HY-151145
-
-
- HY-151144
-
-
- HY-101446
-
|
HIOC
|
Trk Receptor
ERK
Apoptosis
|
Neurological Disease
|
|
HIOC is a potent and selective activator of TrkB (tropomyosin related kinase B) receptor. HIOC can pass the blood-brain and blood-retinal barriers.HIOC activates TrkB/ERK pathway and decreases neuronal cell apoptosis. HIOC attenuates early brain injury after SAH (subarachnoid hemorrhage). HIOC shows protective activity in an animal model for light-induced retinal degeneration.
|
-
- HY-101448
-
|
TMI-1
WAY-171318
|
MMP
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
TMI-1 is a potent inhibitor of disintegrin metalloenzyme 17 (ADAM17) and other MMPs. TMI-1 inhibits LPS-induced TNF-α secretion in human primary monocytes, and human whole blood. TMI-1 selectively induces caspase-dependent apoptosis in triple negative (TN) and ERBB2-overexpressing breast tumor cell lines.
|
-
- HY-106004
-
|
Zamicastat
BIA 5-1058
|
Dopamine β-hydroxylase
P-glycoprotein
BCRP
|
Cancer
Cardiovascular Disease
|
|
Zamicastat (BIA 5-1058) is a dopamine β-hydroxylase (DBH) inhibitor and can cross the blood-brain barrier (BBB) to cause central as well as peripheral effects. Zamicastat is also a concentration-dependent dual P-gp and BCRP inhibitor with IC50 values of 73.8 μM and 17.0 μM, respectively. Zamicastat reduces high blood pressure.
|
-
- HY-107663A
-
|
MIF-1 TFA
Pro-Leu-Gly-NH2 TFA; Melanostatin TFA
|
Dopamine Receptor
|
Neurological Disease
|
|
MIF-1 TFA (Melanostatin), an endogenous brain peptide, is a potent dopamine receptor allosteric modulator. MIF-1 TFA inhibits melanin formation. MIF-1 TFA blocks the effects of opioid receptor activation to modulate the analgesic effects. MIF-1 TFA accesses from the blood to the CNS by directly crossing the blood-brain barrier (BBB).
|
-
- HY-126899
-
|
TPI-287
|
Microtubule/Tubulin
|
Cancer
|
|
TPI-287, a blood-brain barrier-permeable microtubule stabilizer, can significantly reduce metastatic colonization of breast cancer in the brain.
|
-
- HY-B1090
-
-
- HY-B1251
-
|
Guanethidine
|
Others
|
|
|
Guanethidine sulphate was synthesized in 1959. Guanethidine is thought to lowing blood pressure by interfering with the metabolism of chemical transmitter substances in post-ganglionic sympathetic nerve fibres.
|
-
- HY-113317
-
-
- HY-17004
-
-
- HY-137441
-
-
- HY-N6685
-
-
- HY-129953A
-
-
- HY-N0766
-
|
Isorhynchophylline
|
Others
|
Others
|
|
Isorhynchophylline (IRN), an alkaloid isolated from Uncaria rhynchophylla, possesses the effects of lowered blood pressure, vasodilatation and protection against ischemia-induced neuronal damage.
|
-
- HY-147151
-
|
AMCPy
|
Others
|
Others
|
|
AMCPy is a potent electron paramagnetic resonance (EPR) brain imaging agent, possessing excellent lipophilicity for blood−brain barrier (BBB) penetration.
|
-
- HY-113024
-
-
- HY-U00340
-
|
PPAR agonist 1
|
PPAR
|
Metabolic Disease
|
|
PPAR agonist 1 is an agonist of PPAR α and PPAR γ, used for reducing blood glucose, lipid levels, lowering cholesterol and reducing body weight.
|
-
- HY-14165A
-
|
(S)-Veliflapon
(S)-BAY X 1005; (S)-DG-031
|
Leukotriene Receptor
FLAP
|
Inflammation/Immunology
|
|
(S)-Veliflapon ((S)-BAY X 1005) is an orally active inhibitor of leukotriene biosynthesis and 5-lipoxygenase activating protein (FLAP). (S)-Veliflapon inhibits the formation of leukotriene B4 (LTB4) in rat, mouse and human leukocytes with IC50 values of 0.026 µM, 0.039 µM and 0.22 µM respectively. (S)-Veliflapon showes enantioselectivity in human whole blood.
|
-
- HY-B0130A
-
-
- HY-121660
-
|
Hexyl nicotinate
|
Others
|
Others
|
|
Hexyl nicotinate, a nicotinic acid ester with vasodilatory effect. Hexyl nicotinate improves blood circulation, usually serves as an active ingredient in topical preparations, such as creams and lotions.
|
-
- HY-111431
-
-
- HY-D0300
-
|
Leucomalachite green
|
Fluorescent Dye
|
Others
|
|
Leucomalachite green is a triphenylmethane dye used to detect blood. Leucomalachite green, a major metabolite of malachite green, is a potential carcinogen, teratogen and mutagen.
|
-
- HY-19657
-
-
- HY-B0130
-
-
- HY-17004S
-
|
Olmesartan-d4
RNH-6270-d4
|
Angiotensin Receptor
|
Others
|
|
Olmesartan-d4 is the deuterium labeled Olmesartan. Olmesartan is an angiotensin II receptor (AT1R) antagonist used to treat high blood pressure.
|
-
- HY-139573
-
-
- HY-N1480
-
|
(-)-Fucose
6-Desoxygalactose; L-(-)-Fucose; L-Galactomethylose
|
Endogenous Metabolite
Parasite
|
Infection
Metabolic Disease
|
|
(-)-Fucose is classified as a member of the hexoses, plays a role in A and B blood group antigen substructure determination, selectin-mediated leukocyte-endothelial adhesion, and host-microbe interactions.
|
-
- HY-A0245
-
|
Dihydrotachysterol
|
VD/VDR
|
Metabolic Disease
|
|
Dihydrotachysterol is a synthetic analog of vitamin D. Dihydrotachysterol can be used to for the research of hypocalcemia (lack of calcium in the blood) and hypoparathyroidism (lack of parathyroid hormone in the body) .
|
-
- HY-14503
-
|
MDR-1339
DWK-1339
|
Amyloid-β
|
Neurological Disease
|
|
MDR-1339 (DWK-1339) is an orally active and blood-brain-barrier-permeable Aβ-aggregation inhibitor, used in the research of Alzheimer's disease.
|
-
- HY-107275
-
-
- HY-112305
-
|
AZ32
|
ATM/ATR
|
Cancer
|
|
AZ32 is an orally bioavailable and blood-brain barrier-penetrating ATM inhibitor with an IC50 of <6.2 nM for ATM enzyme, and an IC50 of 0.31 μM for ATM in cell.
|
-
- HY-113208
-
-
- HY-103253
-
|
LY231617
|
Others
|
Neurological Disease
|
|
LY231617 is a potent and blood-brain barrier penetrable antioxidant. LY231617 is a neuroprotective agent in brain, it can be used for the research of nervous disease.
|
-
- HY-107929
-
|
Calcium polystyrene sulfonate
Poly(styrenesulfonic acid) calcium salt
|
Others
|
Cardiovascular Disease
|
|
Calcium polystyrene sulfonate is an ion-exchange resin used for reducing blood levels of potassium. Calcium polystyrene sulfonate is used to treat hyperkalemia in patients with chronic kidney disease (CKD).
|
-
- HY-B0209S
-
-
- HY-131277
-
-
- HY-153354
-
-
- HY-12614
-
|
AMG-1694
|
Glucokinase
|
Metabolic Disease
|
|
AMG-1694 is a potent glucokinase–glucokinase regulatory protein (GK-GKRP) disruptors and promotes the dissociation of the GK-GKRP complex with an IC50 of 7 nM, indirectly increasing GK enzymatic activity. AMG-1694 potently reverses the inhibitory effect of GKRP on GK activity and promotes GK translocation. AMG-1694 normalizes blood glucose levels in several rodent models of diabetes and lowes blood glucose restricted to diabetic and not normoglycaemic animals.
|
-
- HY-134820
-
|
MLT-943
|
MALT1
|
Inflammation/Immunology
|
|
MLT-943 is a potent, selective and orally active MALT1 protease inhibitor. MLT-943 inhibits stimulated-IL-2 secretion in PBMC or in whole blood with a similar IC50 across species (0.07-0.09 μM in PBMC, 0.6-0.8 μM in whole blood). MLT-943 has anti-inflammatory activities and can be used for FcgR-mediated inflammation research.
|
-
- HY-100740
-
|
Lanabecestat
AZD3293; LY3314814
|
Beta-secretase
|
Neurological Disease
|
|
Lanabecestat (AZD3293) is a potent, orally active and blood-brain barrier penetrating BACE1 inhibitor with a Ki of 0.4 nM. Lanabecestat is used for the research of Alzheimer's disease.
|
-
- HY-N9343
-
-
- HY-12219B
-
|
MSI-1701
|
Others
|
Metabolic Disease
|
|
MSI-1701 is an analogue of MSI-1436 which can control weight gain and blood glucose level extracted from patent US 7410959 B1.
|
-
- HY-117501
-
-
- HY-U00170
-
-
- HY-18204S
-
-
- HY-B0318
-
-
- HY-113347
-
-
- HY-N7692
-
|
Polyporusterone A
|
Others
|
Others
|
|
Polyporusterone A is a triterpene carboxylic acid isolated from Polyporus umbellatus Fries. Polyporusterone A has inhibitory effect on free radical-induced lysis of red blood cells (hemolysis).
|
-
- HY-103240
-
|
Methoxy-X04
|
Amyloid-β
|
Others
|
|
Methoxy-X04 is a fluorescent dye that crosses the blood-brain barrier and selectively binds to beta-pleated sheets found in dense core amyloid Aβ plaques.
|
-
- HY-N0252
-
-
- HY-107781
-
-
- HY-131276
-
-
- HY-109549
-
|
Desirudin
CGP 39393; Revasc
|
Thrombin
|
Cardiovascular Disease
|
|
Desirudin (CGP 39393) is a thrombin inhibitor. Desirudin can inhibit the formation of blood clots and venous stasis thrombosis, which is used for the research of thrombocytopenia or platelet dysfunction.
|
-
- HY-B0439
-
|
Sulfadoxine
Sulphadoxine
|
Parasite
HIV
Antibiotic
Endogenous Metabolite
|
Infection
|
|
Sulfadoxine(Sulphadoxine) is a long acting sulfonamide that is used, usually in combination with other agents, for respiratory, urinary tract and malarial infections. Sulfadoxine inhibits HIV replication in peripheral blood mononuclear cells.
|
-
- HY-130012
-
-
- HY-B0946S1
-
|
Sulfamonomethoxine-d3
|
Bacterial
Antibiotic
|
Infection
|
|
Sulfamonomethoxine-d3 is the deuterium labeled Sulfamonomethoxine. Sulfamonomethoxine is a long acting sulfonamide antibacterial agent, used in blood kinetic studies,and blocks the synthesis of folic acid by inhibiting synthetase of dihydropteroate.
|
-
- HY-135381
-
-
- HY-111827
-
-
- HY-N0252A
-
-
- HY-120332
-
-
- HY-W250151
-
|
Leishman's stain
|
Fluorescent Dye
|
Others
|
|
Leishman's stain is an essential staining tool for for staining of the peripheral blood and bone marrow smears (displayed pale bluish-grey to deep blue under oil-immersion lens).
|
-
- HY-153175
-
|
BT44
|
RET
|
Neurological Disease
|
|
BT44 is a selective RET activator. BT44 can penetrate through the blood-brain barrier and can be used for the research of neurodegenerative disorders and diabetes mellitus.
|
-
- HY-D0711
-
|
Indocyanine green
Foxgreen; IC Green; Cardiogreen
|
Fluorescent Dye
|
Others
|
|
Indocyanine green (Foxgreen) is a low toxicic fluorescent agent that has been widely used in medical diagnostics, such as determining cardiac output, hepatic function, and liver blood flow, and for ophthalmic angiography.
|
-
- HY-Y1787
-
|
Dimethyl malonate
|
Apoptosis
|
Neurological Disease
|
|
Dimethyl malonate is a competitive inhibitor of succinate dehydrogenase (SDH). Dimethyl malonate is able to cross the blood-brain barrier and hydrolyse to malonate. Dimethyl malonate reduces neuronal apoptosis.
|
-
- HY-B0193S
-
-
- HY-146676
-
|
UR-MB108
|
BCRP
|
Cancer
|
|
UR-MB108 (Compound 57) is a potent, selective ABCG2 (BCRP) inhibitor with an IC50 of 79 nM. UR-MB108 is stable in blood plasma.
|
-
- HY-N0518
-
|
Toddalolactone
|
PAI-1
|
Cardiovascular Disease
|
|
Toddalolactone, a main component of Toddalia asiatica, inhibits the activity of recombinant human plasminogen activator inhibitor-1 (PAI-1), with an IC50 value of 37.31 μM.
|
-
- HY-128923
-
|
SKF-34288 hydrochloride
3-Mercaptopicolinic acid hydrochloride; 3-MPA hydrochloride
|
PEPCK
|
Metabolic Disease
|
|
SKF-34288 (3-Mercaptopicolinic acid) hydrochloride is an orally active phosphoenolpyruvate carboxykinase (PEPCK) inhibitor (Ki: 2-9 μM). SKF-34288 hydrochloride is a potent hypoglycemic agent by inhibiting glucose synthesis. SKF-34288 hydrochloride also inhibits Asn metabolism and increases amino acids and amides.
|
-
- HY-W013075
-
|
Rutin trihydrate
Rutoside trihydrate; Quercetin 3-O-rutinoside trihydrate
|
Apoptosis
Endogenous Metabolite
|
Neurological Disease
Cancer
|
|
Rutin (Rutoside) trihydrate is a multifunctional natural flavonoid glycoside. Rutin trihydrate has been demonstrating excellent antioxidant, anti-inflammatory, anti-diabetic, and anti-carcinogenic properties. Cardioprotective and neuroprotective activities .
|
-
- HY-13956B
-
|
Pioglitazone potassium
U 72107 potassium
|
PPAR
Ferroptosis
|
Cancer
Metabolic Disease
|
|
Pioglitazone (U 72107) potassium is an orally active and selective PPARγ (peroxisome proliferator-activated receptor) agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 μM and 0.99 μM for human and mouse PPARγ, respectively. Pioglitazone potassium can be used in diabetes research.
|
-
- HY-120559
-
-
- HY-13956
-
|
Pioglitazone
U 72107
|
PPAR
Ferroptosis
|
Metabolic Disease
Cancer
|
|
Pioglitazone (U 72107) is an orally active and selective PPARγ (peroxisome proliferator-activated receptor) agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively. Pioglitazone can be used in diabetes research.
|
-
- HY-128868D
-
|
FITC-Dextran (MW 40000)
|
Fluorescent Dye
|
Others
|
|
FITC-Dextran (MW 40000) is a fluorescent probe for fluorescein isothiocyanate (FITC) dextran (Ex=495 nm; Em=525 nm). FITC-Dextran (MW 40000) can be used as a marker to reveal heat shock-induced cell damage and to study the early and late stages of apoptosis. FITC-Dextran (MW 40000) can also be used for cell permeability studies, such as blood-brain barrier permeability and determination of the extent of blood-brain barrier disruption. Storage: protect from light.
|
-
- HY-128868H
-
|
FITC-Dextran (MW 500000)
|
Biochemical Assay Reagents
|
Others
|
|
FITC-Dextran (MW 500000) is a fluorescent probe for fluorescein isothiocyanate (FITC) dextran (Ex=495 nm; Em=525 nm). FITC-Dextran (MW 500000) can be used as a marker to reveal heat shock-induced cell damage and to study the early and late stages of apoptosis. FITC-Dextran (MW 500000) can also be used for cell permeability studies, such as blood-brain barrier permeability and determination of the extent of blood-brain barrier disruption. Storage: protect from light.
|
-
- HY-128868
-
|
FITC-Dextran (MW 10000)
|
Fluorescent Dye
|
Others
|
|
FITC-Dextran (MW 10000) is a fluorescent probe for fluorescein isothiocyanate (FITC) dextran (Ex=495 nm; Em=525 nm). FITC-Dextran (MW 10000) can be used as a marker to reveal heat shock-induced cell damage and to study the early and late stages of apoptosis. FITC-Dextran (MW 10000) can also be used for cell permeability studies, such as blood-brain barrier permeability and determination of the extent of blood-brain barrier disruption. Storage: protect from light.
|
-
- HY-128868G
-
|
FITC-Dextran (MW 150000)
|
Fluorescent Dye
|
Others
|
|
FITC-Dextran (MW 150000) is a fluorescent probe for fluorescein isothiocyanate (FITC) dextran (Ex=495 nm; Em=525 nm). FITC-Dextran (MW 150000) can be used as a marker to reveal heat shock-induced cell damage and to study the early and late stages of apoptosis. FITC-Dextran (MW 150000) can also be used for cell permeability studies, such as blood-brain barrier permeability and determination of the extent of blood-brain barrier disruption. Storage: protect from light.
|
-
- HY-128868I
-
|
FITC-Dextran (MW 2000000)
|
Biochemical Assay Reagents
|
Others
|
|
FITC-Dextran (MW 2000000) is a fluorescent probe for fluorescein isothiocyanate (FITC) dextran (Ex=495 nm; Em=525 nm). FITC-Dextran (MW 2000000) can be used as a marker to reveal heat shock-induced cell damage and to study the early and late stages of apoptosis. FITC-Dextran (MW 2000000) can also be used for cell permeability studies, such as blood-brain barrier permeability and determination of the extent of blood-brain barrier disruption. Storage: protect from light.
|
-
- HY-128868A
-
|
FITC-Dextran (MW 4000)
|
Fluorescent Dye
|
Others
|
|
FITC-Dextran (MW 4000) is a fluorescent probe for fluorescein isothiocyanate (FITC) dextran (Ex=495 nm; Em=525 nm). FITC-Dextran (MW 4000) can be used as a marker to reveal heat shock-induced cell damage and to study the early and late stages of apoptosis. FITC-Dextran (MW 4000) can also be used for cell permeability studies, such as blood-brain barrier permeability and determination of the extent of blood-brain barrier disruption. Storage: protect from light.
|
-
- HY-128868F
-
|
FITC-Dextran (MW 110000)
|
Biochemical Assay Reagents
|
Others
|
|
FITC-Dextran (MW 110000) is a fluorescent probe for fluorescein isothiocyanate (FITC) dextran (Ex=495 nm; Em=525 nm). FITC-Dextran (MW 110000) can be used as a marker to reveal heat shock-induced cell damage and to study the early and late stages of apoptosis. FITC-Dextran (MW 110000) can also be used for cell permeability studies, such as blood-brain barrier permeability and determination of the extent of blood-brain barrier disruption. Storage: protect from light.
|
-
- HY-N2118
-
|
Bilobetin
|
PPAR
PKA
|
Metabolic Disease
|
|
Bilobetin, an active component of Ginkgo biloba, can reduce blood lipids and improve the effects of insulin. Bilobetin ameliorated insulin resistance, increased the hepatic uptake and oxidation of lipids, reduced very-low-density lipoprotein triglyceride secretion and blood triglyceride levels, enhanced the expression and activity of enzymes involved in β-oxidation and attenuated the accumulation of triglycerides and their metabolites in tissues. Bilobetin also increased the phosphorylation, nuclear translocation and activity of PPARα accompanied by elevated cAMP level and PKA activity.
|
-
- HY-128868E
-
|
FITC-Dextran (MW 70000)
|
Biochemical Assay Reagents
|
Others
|
|
FITC-Dextran (MW 70000) is a fluorescent probe for fluorescein isothiocyanate (FITC) dextran (Ex=495 nm; Em=525 nm). FITC-Dextran (MW 70000) can be used as a marker to reveal heat shock-induced cell damage and to study the early and late stages of apoptosis. FITC-Dextran (MW 70000) can also be used for cell permeability studies, such as blood-brain barrier permeability and determination of the extent of blood-brain barrier disruption. Storage: protect from light.
|
-
- HY-128868C
-
|
FITC-Dextran (MW 20000)
|
Biochemical Assay Reagents
|
Others
|
|
FITC-Dextran (MW 20000) is a fluorescent probe for fluorescein isothiocyanate (FITC) dextran (Ex=495 nm; Em=525 nm). FITC-Dextran (MW 20000) can be used as a marker to reveal heat shock-induced cell damage and to study the early and late stages of apoptosis. FITC-Dextran (MW 20000) can also be used for cell permeability studies, such as blood-brain barrier permeability and determination of the extent of blood-brain barrier disruption. Storage: protect from light.
|
-
- HY-124475
-
|
Antalarmin
|
CRFR
|
Neurological Disease
|
|
Antalarmin is a selective nonpeptide corticotropin-releasing factor receptor 1 (CRHR1) antagonist with a Ki of 2.7 nM. Antalarmin can pass through the blood–brain barrier.
|
-
- HY-146154
-
|
EGFR-IN-58
|
EGFR
|
Cancer
|
|
EGFR-IN-58 (Compound 4a) is a potent, ATP-competitive, and selective EGFR inhibitor. EGFR-IN-58 shows potent cytotoxicity against melanoma, colon, and blood cancers.
|
-
- HY-A0167
-
|
Gadopentetate dimeglumine
SH-L-451A; Gadopentetic acid dimeglumine salt
|
Others
|
Cancer
|
|
Gadopentetate dimeglumine (SH-L-451A) is used in combination with magnetic resonance imaging (MRI) to allow blood vessels, organs, and other non-bony tissues to be seen more clearly on the MRI.
|
-
- HY-145964
-
|
INE963
|
Parasite
|
Infection
|
|
INE963 is a potent and fast-acting blood-stage antimalarial agent, with an EC50s of 3-6 nM. INE963 is potential for single-dose cures in uncomplicated malaria.
|
-
- HY-12599
-
-
- HY-121599
-
|
CGP 36742
SGS-742
|
GABA Receptor
|
Neurological Disease
|
|
CGP 36742 is a selective GABAB receptor antagonist that can penetrate the blood–brain barrier after peripheral administration, with an IC50 of 32 μM. CGP 36742 is useful in treatment of depression.
|
-
- HY-113335
-
-
- HY-W016823S
-
-
- HY-B0303A
-
-
- HY-135380
-
-
- HY-15283
-
|
Clopidogrel
|
P2Y Receptor
|
Cardiovascular Disease
|
|
Clopidogrel is an orally active platelet inhibitor that targets P2Y12 receptor. Clopidogrel is used to inhibit blood clots in coronary artery disease, peripheral vascular disease, and cerebrovascular disease.
|
-
- HY-114164
-
|
Thrombin (MW 37kDa)
|
Thrombin
|
Neurological Disease
|
|
Thrombin (MW 37kDa) is a Na +-activated, allosteric serine protease that plays opposing functional roles in blood coagulation. Thrombin recognition sequence and can be used to digest GST-tagged proteins.
|
-
- HY-N0026
-
|
2'-Acetylacteoside
2'-AA
|
Others
|
Others
|
|
2'-Acetylacteoside is a phenylethanoid glycoside isolated from Brandisia hancei, inhibits free radical-induced hemolysis of red blood cells and exhibits free radical scavenging activity.
|
-
- HY-106147
-
|
Frakefamide
|
Opioid Receptor
|
Neurological Disease
|
|
Frakefamide is a potent analgesic that acts as a peripheral active μ-selective receptor agonist. Frakefamide is unable to penetrate the blood-brain-barrier and enter the central nervous system.
|
-
- HY-108011
-
|
Naftazone
|
Others
|
Cardiovascular Disease
|
|
Naftazone is a naphthoquinone derivative, it can be used for the research of venous insufciency. Naftazone protects blood vessels, increases venous tonicity and capillary resistance, and improves lymphatic and venous circulation.
|
-
- HY-18204S2
-
-
- HY-133775
-
-
- HY-131279
-
|
Olmesartan ethyl ester
|
Drug Metabolite
|
Others
|
|
Olmesartan ethyl ester (compound 11) is an Olmesartan impurity. Olmesartan (RNH-6270) is an angiotensin II receptor (AT1R) antagonist used to in the high blood pressure study.
|
-
- HY-113643
-
-
- HY-N7693
-
|
Polyporusterone B
|
Others
|
Others
|
|
Polyporusterone B is a triterpene carboxylic acid isolated from Polyporus umbellatus Fries. Polyporusterone B has inhibitory effect on free radical-induced lysis of red blood cells (hemolysis).
|
-
- HY-B0303
-
-
- HY-13909
-
|
RGFP966
|
HDAC
|
Cancer
|
|
RGFP966 is a highly selective HDAC3 inhibitor with an IC50 of 80 nM and shows no inhibition to other HDACs at concentrations up to 15 μM. RGFP966 can penetrate the blood brain barrier (BBB).
|
-
- HY-18204S3
-
-
- HY-N0684S3
-
-
- HY-16403
-
|
Polythiazide
|
Others
|
Cardiovascular Disease
|
|
Polythiazide is a potent and orally active thiazide diuretic agent that has antihypertensive effect. Polythiazide can decrease edema and decrease blood pressure. Polythiazide also has phototoxicity.
|
-
- HY-144004
-
|
DSPE-PEG-Maleimide
|
Liposome
|
Others
|
|
DSPE-PEG-Maleimide has DSPE phospholipid and maleimide to prepare nanostructured lipid carrier. DSPE-PEG-Maleimide extends blood circulation time and higher stability for encapsulated agents.
|
-
- HY-10231
-
-
- HY-B0946S2
-
|
Sulfamonomethoxine-13C6
|
Bacterial
Antibiotic
|
Infection
|
|
Sulfamonomethoxine- 13C6 is the 13C6 labeled Sulfamonomethoxine. Sulfamonomethoxine is a long acting sulfonamide antibacterial agent, used in blood kinetic studies,and blocks the synthesis of folic acid by inhibiting synthetase of dihydropteroate.
|
-
- HY-106147B
-
|
Frakefamide TFA
|
Opioid Receptor
|
Neurological Disease
|
|
Frakefamide TFA is a potent analgesic that acts as a peripheral active μ-selective receptor agonist. Frakefamide is unable to penetrate the blood-brain-barrier and enter the central nervous system.
|
-
- HY-N0726
-
|
Dracorhodin perchlorate
Dracohodin perochlorate
|
Apoptosis
|
Cancer
|
|
Dracorhodin perchlorate (Dracohodin perochlorate) is a natural product extracted from a natural medicine Dragon's blood. Dracorhodin perchlorate inhibits cell proliferation and induces cell cycle arrest and apoptosis.
|
-
- HY-128868B
-
|
FITC-Dextran (MW 3000-5000)
|
Biochemical Assay Reagents
|
Others
|
|
FITC-Dextran (MW 3000-5000) is a fluorescent probe for fluorescein isothiocyanate (FITC) dextran (Ex=495 nm; Em=525 nm). FITC-Dextran (MW 3000-5000) can be used as a marker to reveal heat shock-induced cell damage and to study the early and late stages of apoptosis. FITC-Dextran (MW 3000-5000) can also be used for cell permeability studies, such as blood-brain barrier permeability and determination of the extent of blood-brain barrier disruption. Storage: protect from light.
|
-
- HY-141616
-
-
- HY-120924
-
-
- HY-B1192
-
|
Estradiol benzoate
β-Estradiol 3-benzoate; 17β-Estradiol 3-benzoate
|
Estrogen Receptor/ERR
|
Endocrinology
Cancer
|
|
Estradiol Benzoate (β-Estradiol 3-benzoate), a proagent of estradiol, acts as a steroid sex hormone. It exhibits mild anabolic and metabolic properties, and increases blood coagulability.
|
-
- HY-138795
-
|
Curcumin-β-D-glucuronide
|
Others
|
Cancer
|
|
Curcumin-β-D-glucuronide is a major metabolite after oral intake of Curcumin in hepatic tissue and portal blood. Curcumin-β-D-glucuronide can be used for the research of colon cancer.
|
-
- HY-145912
-
-
- HY-18204S1
-
|
Valsartan-d3
CGP 48933-d3
|
Angiotensin Receptor
|
|
|
Valsartan-d3 is the deuterium labeled Valsartan[1]. Valsartan (CGP 48933) is an angiotensin II receptor antagonist and has the potential for high blood pressure and heart failure research[2].
|
-
- HY-105860
-
|
Selurampanel
BGG 492
|
iGluR
|
Neurological Disease
|
|
Selurampanel (BGG 492) is an orally active and competitive AMPA receptor antagonist with an IC50 of 190 nM. Selurampanel has reasonable blood-brain barrier penetration. Selurampanel can be used for epilepsy research.
|
-
- HY-149278
-
-
- HY-135379
-
-
- HY-N0684S1
-
-
- HY-15922A
-
|
Luminol sodium salt
|
Fluorescent Dye
|
Others
|
|
Luminol sodium salt is a chemical that exhibits chemiluminescence with pKa values of 6.74 and 15.1. Luminol sodium salt exhibits chemiluminescence (CL) at 425 nm λmax. Luminol sodium salt is commonly used in forensics as a diagnostic tool for the detection of blood stains.
|
-
- HY-113358
-
-
- HY-120160
-
|
Darglitazone
CP-86325
|
PPAR
|
Metabolic Disease
Neurological Disease
|
|
Darglitazone (CP-86325), a thiazolidinedione, is a potent, selective, and orally active PPAR-γ agonist. Darglitazone is effective in controlling blood glucose and lipid metabolism, and can be used for type II diabetes research.
|
-
- HY-140740
-
|
DSPE-PEG-Maleimide (MW 5000)
|
Others
|
Cancer
|
|
DSPE-PEG-Maleimide (MW 5000) has DSPE phospholipid and maleimide to prepare nanostructured lipid carrier. DSPE-PEG-maleimide extends blood circulation time and higher stability for encapsulated agents.
|
-
- HY-113067
-
|
Phytanic acid
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Phytanic acid is an endogenous metabolite present in Blood that can be used for the research of Zellweger Syndrome, Alpha Methylacyl CoA Racemase Deficiency, Rhizomelic Chondrodysplasia Punctata and Infantile Refsum Disease.
|
-
- HY-101485
-
|
AUTEN-99 hydrobromide
Autophagy enhancer-99 hydrobromide
|
Others
|
Neurological Disease
|
|
AUTEN-99 (hydrobromide) is a novel inhibitor of the myotubularin phosphatase Jumpy (also called MTMR14). AUTEN-99 (hydrobromide) crosses the blood-brain barrier and exerts potent neuroprotective effects.
|
-
- HY-120980
-
-
- HY-A0124A
-
|
Sapropterin dihydrochloride
(6R)-BH4 dihydrochloride; (6R)-Tetrahydro-L-biopterin dihydrochloride
|
Others
|
Cardiovascular Disease
|
|
Sapropterin ((6R)-BH4) dihydrochloride is an orally active phenylalanine hydroxylase (PAH) cofactor, which is effective in reducing blood phenylalanine concentrations. Sapropterin dihydrochloride can be used in study of phenylketonuria (PKU).
|
-
- HY-103242
-
|
CRANAD-2
|
Amyloid-β
|
Neurological Disease
|
|
CRANAD-2 is a near-infrared (NIR) Aβ plaque-specific fluorescent probe. CRANAD 2 penetrates the blood brain barrier and has a high affinity for Aβ aggregates with a Kd of 38 nM.
|
-
- HY-143209
-
|
DSPE-PEG
|
Liposome
|
Others
|
|
DSPE-PEG is a phospholipids-polymer conjugate that can be used in drug delivery applications. DSPE-PEG is a material for the formulation of nanocarriers for achieving prolonged blood circulation time, improved stability and enhanced encapsulation efficiency.
|
-
- HY-15922
-
|
Luminol
Diogenes reagent
|
Fluorescent Dye
|
Others
|
|
Luminol is a chemical that exhibits chemiluminescence with pKa values of 6.74 and 15.1. Luminol exhibits chemiluminescence (CL) at 425 nm λmax. Luminol is commonly used in forensics as a diagnostic tool for the detection of blood stains.
|
-
- HY-A0124
-
|
Sapropterin
(6R)-BH4; (6R)-Tetrahydro-L-biopterin
|
Others
|
Metabolic Disease
|
|
Sapropterin ((6R)-BH4) is an orally active phenylalanine hydroxylase (PAH) cofactor, which is effective in reducing blood phenylalanine concentrations. Sapropterin can be used in study of phenylketonuria (PKU).
|
-
- HY-17591S
-
|
Penicillin G-d5 potassium
Benzylpenicillin-d5 (potassium)
|
Bacterial
Antibiotic
|
Infection
|
|
Penicillin G-d5 (potassium) is the deuterium labeled Penicillin G potassium. Penicillin G potassium is a fast-acting antibiotic; used to treat bacterial infections that affect the blood, heart, lungs, joints, and genital areas[1][2].
|
-
- HY-109018A
-
|
Velagliflozin proline
|
SGLT
|
Metabolic Disease
|
|
Velagliflozin proline is an oral sodium-glucose cotransporter 2 (SGLT2) inhibitor with antidiabetic activity. Velagliflozin proline reduces renal glucose reabsorption and stimulates glycosuria, which lowers blood sugar and insulin concentrations.
|
-
- HY-W010936
-
|
Nitrobenzylthioinosine
NBMPR
|
Adenosine Receptor
|
Neurological Disease
|
|
Nitrobenzylthioinosine is an ENT1 transporter inhibitor that binds to ENT1 transporter with high affinity. Nitrobenzylthioinosine is a photoaffinity probe for adenosine uptake sites in brain. Nitrobenzylthioinosine can cross the blood-brain barrier.
|
-
- HY-B0109
-
|
Dorzolamide
L671152; MK507
|
Carbonic Anhydrase
|
Cancer
|
Dorzolamide (L671152) is a potent carbonic anhydrase II inhibitor, with IC50 values of 0.18 nM and 600 nM for red blood cell CA-II and CA-I respectively. Dorzolamide possesses anti-tumor activity.
|
-
- HY-100870
-
|
Obefazimod
ABX464
|
HIV
|
Infection
|
|
Obefazimod (ABX464) is a potent anti-HIV agent. Obefazimod inhibits HIV-1 replication in stimulated peripheral blood mononuclear cells (PBMCs) with an IC50 ranging between 0.1 μM and 0.5 μM.
|
-
- HY-N0684S
-
-
- HY-N4195
-
|
Resveratroloside
Resveratrol glycoside; trans-Resveratrol 4'-O-β-D-glucopyranoside
|
Glucosidase
|
Metabolic Disease
Cardiovascular Disease
|
|
Resveratroloside (Resveratrol glycoside) is a competitive inhibitior of α-glucosidase with an IC50 of 22.9 μM. Resveratroloside has the ability to regulate PBG (postprandial blood glucose) levels. Resveratroloside exhibits cardioprotective effect.
|
-
- HY-B0109A
-
|
Dorzolamide hydrochloride
L671152 hydrochloride; MK507 hydrochloride
|
Carbonic Anhydrase
|
Others
|
Dorzolamide (L671152) hydrochloride is a potent carbonic anhydrase II inhibitor, with IC50 values of 0.18 nM and 600 nM for red blood cell CA-II and CA-I respectively. Dorzolamide possesses anti-tumor activity.
|
-
- HY-112197
-
-
- HY-135373
-
-
- HY-N2072
-
|
Crocetin
Transcrocetin; trans-Crocetin
|
iGluR
Endogenous Metabolite
|
Cancer
|
|
Crocetin (Transcrocetin), extracted from saffron (Crocus sativus L.), acts as an NMDA receptor antagonist with high affinity. Crocetin is capable of crossing the blood-brain barrier and reach the central nervous system (CNS).
|
-
- HY-N2421
-
|
Sequoyitol
5-O-Methyl-myo-inositol
|
Others
|
Metabolic Disease
|
|
Sequoyitol (5-O-Methyl-myo-inositol) is isolated from plants. Sequoyitol (5-O-Methyl-myo-inositol) decreases blood glucose, improves glucose intolerance, and is used to treat diabetes.
|
-
- HY-U00046
-
|
Apyramide
|
COX
|
Inflammation/Immunology
|
|
Apyramide is an?anti-inflammatory?agent (NSAID) and behaves as a proagent of indomethacin (HY-14397). Indomethacin is a potent, blood-brain permeable and nonselective inhibitor of?COX1?and?COX2.
|
-
- HY-U00037
-
|
Ecopladib
PLA 725
|
Phospholipase
|
Inflammation/Immunology
|
|
Ecopladib is a sub-micromolar inhibitor of cytosolic phospholipase A2α (cPLA2α), with IC50s of 0.15 μM and 0.11 μM in the GLU micelle and rat whole blood assays, respectively.
|
-
- HY-15722
-
-
- HY-B0762
-
|
Acetyl-L-carnitine hydrochloride
O-Acetyl-L-carnitine hydrochloride; ALCAR hydrochloride
|
Endogenous Metabolite
|
Neurological Disease
|
|
Acetyl-L-carnitine (O-Acetyl-L-carnitine) hydrochloride is a blood-brain permeable acetyl ester of the amino acid L-carnitine found in the body. Acetyl-L-carnitine hydrochloride is often used as a dietary supplement, and exibits anti-stress-related psychiatric disorders.
|
-
- HY-10959
-
|
RG7112
RO5045337
|
MDM-2/p53
E1/E2/E3 Enzyme
|
Cancer
|
|
RG7112 is a potent, selective, first clinical, orally active and blood-brain barrier crossed MDM2-p53 inhibitor, with an IC50 of 18 nM and a KD of 11 nM for binding to MDM2.
|
-
- HY-B0946S3
-
|
Sulfamonomethoxine-d3-1
|
Bacterial
Antibiotic
|
Infection
|
|
Sulfamonomethoxine-d3-1 is the deuterium labeled Sulfamonomethoxine[1]. Sulfamonomethoxine is a long acting sulfonamide antibacterial agent, used in blood kinetic studies,and blocks the synthesis of folic acid by inhibiting synthetase of dihydropteroate[2].
|
-
- HY-138944
-
-
- HY-P0004
-
|
Lysipressin
Lysine vasopressin; [Lys8]-Vasopressin
|
Adenylate Cyclase
|
Others
|
|
Lysipressin (Lysine vasopressin) is antidiuretic hormone that have been found in pigs and some marsupial families. Lysipressin induces contraction of the rabbit urinary bladder smooth muscle, activate adenylate-cyclase.
|
-
- HY-147393
-
-
- HY-B0351
-
|
Taurine
2-Aminoethanesulfonic acid
|
Autophagy
Endogenous Metabolite
|
Metabolic Disease
Cancer
|
|
Taurine, a sulphur-containing amino acid and an organic osmolyte involved in cell volume regulation, provides a substrate for the formation of bile salts, and plays a role in the modulation of intracellular free calcium concentration. Taurine has the ability to activate autophagy in adipocytes.
|
-
- HY-124489
-
-
- HY-P0004A
-
|
Lysipressin acetate
Lysine vasopressin acetate; [Lys8]-Vasopressin acetate
|
Adenylate Cyclase
|
Others
|
|
Lysipressin (Lysine vasopressin) acetate is antidiuretic hormone that have been found in pigs and some marsupial families. Lysipressin acetate induces contraction of the rabbit urinary bladder smooth muscle, activate adenylate-cyclase.
|
-
- HY-W010144
-
|
Phenidone
|
COX
Lipoxygenase
|
Inflammation/Immunology
Cardiovascular Disease
|
|
Phenidone, an orally active dual inhibitor of cyclooxygenase (COX) and lipoxygenase (LOX), ameliorates rat paralysis in experimental autoimmune encephalomyelitis. Phenidone is a potent hypotensive agent in the spontaneously hypertensive rat. Phenidone is used as a photographic developer.
|
-
- HY-14362
-
|
GSK-25
|
ROCK
Ribosomal S6 Kinase (RSK)
|
Cardiovascular Disease
|
|
GSK-25 is a potent, selective and orally bioavailable ROCK1 inhibitor (IC50=7 nM). GSK-25 maintains good selectivity against a panel of 31 kinases (>100 fold), as well as RSK1 and p70S6K (RSK1: IC50=398 nM, p70S6K: IC50=1 μM). GSK-25 inhibits P450 profile (IC50s of 2.5, 5.2, 2.5 µM for CYP2C9, CYP2D6, CYP3A4, respectively).
|
-
- HY-111778
-
|
EHMT2-IN-1
|
Histone Methyltransferase
|
Cancer
|
|
EHMT2-IN-1 is a potent EHMT inhibitor, with IC50s of all <100 nM for EHMT1 peptide, EHMT2 peptide and cellular EHMT2. Used in the research of blood disorder or cancer.
|
-
- HY-120160A
-
|
Darglitazone Sodium
CP 86325 Sodium
|
PPAR
|
Metabolic Disease
Neurological Disease
|
|
Darglitazone Sodium, a thiazolidinedione, is an orally active, potent, and selective PPAR-γ (peroxisome proliferator-activated receptor) agonist. Darglitazone Sodium is effective in controlling blood glucose and lipid metabolism, and can be used for type II diabetes research.
|
-
- HY-W013989
-
-
- HY-D0300S
-
-
- HY-116477
-
|
URB937
|
FAAH
|
Inflammation/Immunology
Neurological Disease
|
|
URB937 is an orally active and peripherally restricted FAAH inhibitor (IC50=26.8 nM) and increases anandamide levels. URB937 fails to affect FAAH activity in the brain (not penetrate the blood-brain barrier).
|
-
- HY-149980
-
|
DCN-83
|
Others
|
Infection
|
|
DCN-83, an anti-leishmania agent, is most potent against the amastigote form with an IC50 of 0.71 μM. DCN-83 has the potential to cross the blood-brain barrier and central nervous system.
|
-
- HY-111904
-
|
EHMT2-IN-2
|
Histone Methyltransferase
|
Cancer
|
|
EHMT2-IN-2 is a potent EHMT inhibitor, with IC50s of all <100 nM for EHMT1 peptide, EHMT2 peptide and cellular EHMT2. Used in the research of blood disease or cancer.
|
-
- HY-N1480S
-
|
(-)-Fucose-13C
6-Desoxygalactose-13C; L-(-)-Fucose-13C; L-Galactomethylose-13C
|
Parasite
Endogenous Metabolite
|
Infection
Metabolic Disease
|
|
(-)-Fucose- 13C is the 13C labeled (-)-Fucose. (-)-Fucose is classified as a member of the hexoses, plays a role in A and B blood group antigen substructure determination, selectin-mediated leukocyte-endothelial adhesion, and host-microbe interacti[1]
|
-
- HY-W016586
-
|
Acivicin
AT-125; U-42126
|
Parasite
|
Cancer
Infection
|
|
Acivicin (AT-125), a natural product produced by Streptomyces sviceus is a γ-glutamyl transpeptidase (GGT) inhibitor. Acivicin can across the blood-brain barrier and has anti-cancer, anti-parasitic properties.
|
-
- HY-B1410
-
|
Ioversol
MP-328
|
Others
|
Others
|
|
Ioversol (MP-328) is a nonionic iodinated contrast medium (CM) that is used during a CT scan or x-ray in animal experiment. Ioversol does not damage the blood-brain barrier (BBB) in animal.
|
-
- HY-B0186A
-
|
Cefoselis hydrochloride
|
Bacterial
Antibiotic
|
Infection
|
|
Cefoselis hydrochloride, the fourth gen-eration of cephalosporin, is a β-lactam antibiotic. Cefoselis hydrochloride exhibits good activity against a wide range of Gram-positive and Gram-negative organisms. Cefoselis hydrochloride penetrates the blood-brain barrier.
|
-
- HY-N1480S2
-
|
(-)-Fucose-13C-2
6-Desoxygalactose-13C-2; L-(-)-Fucose-13C-2; L-Galactomethylose-13C-2
|
Parasite
Endogenous Metabolite
|
Infection
Metabolic Disease
|
|
(-)-Fucose- 13C-2 is the 13C labeled (-)-Fucose. (-)-Fucose is classified as a member of the hexoses, plays a role in A and B blood group antigen substructure determination, selectin-mediated leukocyte-endothelial adhesion, and host-microbe interacti[
|
-
- HY-N1501
-
|
Beta-asarone
|
Others
|
Inflammation/Immunology
Neurological Disease
|
|
Beta-asarone is a major ingredient of Acorus tatarinowii Schott, penetrates blood brain barrier, with the properties of
immunosuppression, central nervous system inhibition, sedation, and hypothermy. Beta-asarone protects against Parkinson’s disease.
|
-
- HY-B0627
-
-
- HY-B1395A
-
-
- HY-N11551
-
|
Salvifaricin
|
Others
|
Metabolic Disease
Others
|
|
Salvifaricin is an orally active diterpenoid compound that can be isolated from Salvia leucantha Cav. and Salvia hispanica L.. Salvifaricin significantly reduces fasting blood glucose and serum triglyceride (TG) levels, and has anti-diabetic effect.
|
-
- HY-100642
-
|
3-O-Methyltolcapone
Ro 40-7591
|
COMT
|
Neurological Disease
|
|
3-O-Methyltolcapone (Ro 40-7591) is a metabolite of Tolcapone. Tolcapone is an orally active, reversible, selective and potent COMT inhibitor. Tolcapone crosses the blood-brain barrier, and can be used for treatment of Parkinson's disease.
|
-
- HY-P2813
-
|
Hirudin
|
Thrombin
Apoptosis
|
Cancer
Cardiovascular Disease
|
|
Hirudin is a thrombin inhibitor with blood anticoagulant property. Hirudin has potent anti-thrombotic, wound repair, anti-fibrosis, anti-tumor and anti-hyperuricemia effects. Hirudin also affects diabetic complications, cerebral hemorrhage, and others.
|
-
- HY-N11691
-
|
Thapsigargicin
Thapsigargicine
|
Others
|
Inflammation/Immunology
|
|
Thapsigargicin (Thapsigargicine) is a activator of mast cells and leukocytes. Thapsigargicin induces histamine release from rat peritoneal mast cells and human basophil leukocytes. Thapsigargicin increases the cytoplasmic free calcium level in intact human blood platelets.
|
-
- HY-50098
-
-
- HY-N1480S3
-
|
(-)-Fucose-13C-3
6-Desoxygalactose-13C-3; L-(-)-Fucose-13C-3; L-Galactomethylose-13C-3
|
Parasite
Endogenous Metabolite
|
Infection
Metabolic Disease
|
|
(-)-Fucose- 13C-3 is the 13C labeled (-)-Fucose. (-)-Fucose is classified as a member of the hexoses, plays a role in A and B blood group antigen substructure determination, selectin-mediated leukocyte-endothelial adhesion, and host-microbe interacti[
|
-
- HY-B0439S
-
|
Sulfadoxine-d4
Sulphadoxine-d4
|
Parasite
HIV
Antibiotic
Endogenous Metabolite
|
Infection
|
|
Sulfadoxine-d4 is the deuterium labeled Sulfadoxine. Sulfadoxine(Sulphadoxine) is a long acting sulfonamide that is used, usually in combination with other agents, for respiratory, urinary tract and malarial infections. Sulfadoxine inhibits HIV replication in peripheral blood mononuclear cells.
|
-
- HY-B2130
-
-
- HY-A0282
-
|
L-Ornithine L-aspartate
|
Others
|
Metabolic Disease
|
|
L-Ornithine L-aspartate is a stable salt of two natural nonessential L-amino acids: ornithine and aspartic acid. L-Ornithine L-aspartate lowers blood ammonia concentration and to eliminate symptoms of hepatic encephalopathy associated with liver cirrhosis.
|
-
- HY-W016586A
-
|
Acivicin hydrochloride
AT-125 hydrochloride; U-42126 hydrochloride
|
Parasite
|
Cancer
Infection
|
|
Acivicin hydrochloride (AT-125 hydrochloride), a natural product produced by Streptomyces sviceus, is a γ-glutamyl transpeptidase (GGT) inhibitor. Acivicin hydrochloride can across the blood-brain barrier and has anti-cancer, anti-parasitic properties.
|
-
- HY-50098A
-
|
Mardepodect hydrochloride
PF-2545920 hydrochloride
|
Phosphodiesterase (PDE)
|
Cancer
|
|
Mardepodect hydrochloride (PF-2545920 hydrochloride) is a potent, orally active and selective PDE10A inhibitor with an IC50 of 0.37 nM, with >1000-fold selectivity over other PDEs. Mardepodect hydrochloride can cross the blood-brain barrier.
|
-
- HY-N1480S1
-
|
(-)-Fucose-13C-1
6-Desoxygalactose-13C-1; L-(-)-Fucose-13C-1; L-Galactomethylose-13C-1
|
Parasite
Endogenous Metabolite
|
Infection
Metabolic Disease
|
|
(-)-Fucose- 13C-1 is the 13C labeled (-)-Fucose. (-)-Fucose is classified as a member of the hexoses, plays a role in A and B blood group antigen substructure determination, selectin-mediated leukocyte-endothelial adhesion, and host-microbe interacti[
|
-
- HY-148711
-
-
- HY-15976
-
|
P7C3
|
Others
|
Neurological Disease
|
|
P7C3 is an orally bioavailable and blood-brain barrier penetrant aminopropyl carbazole, with neuroprotective effects. P7C3 can be used for the research of neurodegenerative diseases, including Parkinson's disease.
|
-
- HY-B0186
-
|
Cefoselis
|
Bacterial
Antibiotic
|
Infection
|
|
Cefoselis, the fourth gen-eration of cephalosporin, is a β-lactam antibiotic. Cefoselis exhibits good activity against a wide range of Gram-positive and Gram-negative organisms. Cefoselis penetrates the blood-brain barrier.
|
-
- HY-109061
-
|
Lazertinib
YH25448; GNS-1480
|
EGFR
|
Cancer
|
|
Lazertinib (YH25448) is a potent, highly mutant-selective, blood-brain barrier permeable, orally available and irreversible third-generation EGFR tyrosine kinase inhibitor, and can be used in the research of non-small cell lung cancer.
|
-
- HY-B1395
-
-
- HY-B0683
-
|
Limaprost
17α,20-dimethyl-δ2-PGE1; ONO1206; OP1206
|
PGE synthase
|
Inflammation/Immunology
Cardiovascular Disease
|
|
Limaprost (OP1206) is a PGE1 analogue and a potent and orally active vasodilator. Limaprost increases blood flow and inhibits platelet aggregation. Limaprost pain relief, has antianginal effects, and can be used for ischaemic symptoms research.
|
-
- HY-12947
-
|
GNE-3511
|
MAP3K
|
Neurological Disease
|
|
GNE-3511 is an orally active bioavailable and brain-penetrant dual leucine zipper kinase (DLK) inhibitor with a Ki of 0.5 nM. GNE-3511 can cross the blood-brain-barrier and can be used for the research of neurodegenerative diseases.
|
-
- HY-N8307
-
|
Syringaresinol
|
Others
|
Inflammation/Immunology
Cardiovascular Disease
|
|
Syringaresinol is a lignan that can be extracted from from Dragon’s Blood of Dracaena cambodiana. Syringaresinol has anti-inflammatory activity. Syringaresinol also causes vasorelaxation. Syringaresinol elevates NO production through the phosphorylation and dimerization of endothelial NO synthase.
|
-
- HY-I1111S4
-
|
Fmoc-L-Val-OH-15N
|
Isotope-Labeled Compounds
|
Others
|
|
Fmoc-L-Val-OH- 15N is a 15N-labeled Leucomalachite green. Leucomalachite green is a triphenylmethane dye used to detect blood. Leucomalachite green, a major metabolite of malachite green, is a potential carcinogen, teratogen and mutagen[1][2].
|
-
- HY-N0003
-
|
Honokiol
NSC 293100
|
Akt
Autophagy
HCV
ERK
|
Cancer
|
|
Honokiol is a bioactive, biphenolic phytochemical that possesses potent antioxidative, anti-inflammatory, antiangiogenic, and anticancer activities by targeting a variety of signaling molecules. It inhibits the activation of Akt. Honokiol can readily cross the blood brain barrier.
|
-
- HY-B0303AS1
-
-
- HY-B0692A
-
|
Cefepime chloride
BMY-28142 chloride
|
Antibiotic
Bacterial
|
Infection
|
|
Cefepime (BMY-28142) chloride is a broad-spectrum and cross the blood-brain barrier cephalosporin. Cefepime chloride shows antibacterial effects against both Gram-positive and Gram-negative aerobic bacteria. Cefepime chloride induces neurotoxicity.
|
-
- HY-125301
-
|
Thymoctonan
|
Others
|
Inflammation/Immunology
|
|
Thymoctonan (THF-γ2) is the immunomodulatory octapeptide, thymic humoral factor γ2. Thymoctonan has the half-life less than 6 min at 37 °C in blood from human, rat and mouse.
|
-
- HY-B0303AS
-
-
- HY-B0692
-
|
Cefepime
BMY-28142
|
Antibiotic
Bacterial
|
Infection
Cancer
|
|
Cefepime (BMY-28142) is a broad-spectrum and cross the blood-brain barrier cephalosporin. Cefepime shows antibacterial effects against both Gram-positive and Gram-negative aerobic bacteria. Cefepime induces neurotoxicity.
|
-
- HY-125139
-
|
(all-Z)-8,11,14,17-Eicosatetraenoic acid ethyl ester
Δ8,11,14,17-Eicosatetraenoic acid ethyl ester
|
Biochemical Assay Reagents
|
Others
|
|
omega-3 Arachidonic Acid ethyl ester is a rare polyunsaturated fatty acid found in very small amounts in dietary sources. Omega-3 fatty acids are known to be essential for the growth and development of infants, and they protect against heart disease, blood clots, high blood pressure, and inflammatory and autoimmune diseases. In human platelet membranes, omega-3 arachidonic acid inhibits arachidonyl-CoA synthetase with a Ki of 14 μM. It also inhibits arachidonoyl-CoA synthetase in calf brain extract with an IC50 of approximately 5 μM. Omega-3 ethyl arachidonate is the more lipophilic form of the free acid.
|
-
- HY-111455
-
|
LP-211
|
5-HT Receptor
|
Neurological Disease
|
|
LP-211 is a selective and blood−brain barrier penetrant 5-HT7 receptor agonist, with a Ki of 0.58 nM, with high selectivity over 5-HT1A receptor (Ki, 188 nM) and D2 receptor (Ki, 142 nM).
|
-
- HY-B1009
-
|
Ethylenediaminetetraacetic acid trisodium salt
EDTA trisodium salt; Trisodium EDTA
|
Ferroptosis
|
Others
|
|
Ethylenediaminetetraacetic acid trisodium salt (EDTA trisodium salt) is used to bind metal ions in the practice of chelation therapy, for treating mercury and lead poisoning, used in a similar manner to remove excess iron from the body, for treating the complication of repeated blood transfusions, as would be applied to treat thalassaemia.
|
-
- HY-N3015
-
|
Bruceine E
|
Others
|
Metabolic Disease
|
|
Bruceine E is a quassinoid from seeds of Brucea javanica (L.) Merr, exhibiting hypoglycemia effect. Bruceine E exhibits blood glucose lowering effect in both nondiabetic mice and Streptozotocin (STZ)-induced diabetic rats at lower dose.
|
-
- HY-152632
-
|
BuChE-IN-7
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
BuChE-IN-7 is a highly selective inhibitor of hBuChe and eqBuChE with IC50 values of 40 nM, 80 nM respectively. BuChE-IN-7 can promote cognitive with blood-brain penetration and improves situational and phobic memory, showing preference for new things.
|
-
- HY-11030
-
-
- HY-122015
-
|
ASP2905
|
Potassium Channel
|
Neurological Disease
|
|
ASP2905 is a potent and selective potassium channel Kv12.2 inhibitor encoded by the Kcnh3/BEC1 gene. ASP2905 can cross the blood-brain barrier and has antipsychotic activities.
|
-
- HY-B0318A
-
-
- HY-113042
-
-
- HY-N7513
-
|
Homovanillyl alcohol
|
Drug Metabolite
|
Cardiovascular Disease
|
|
Homovanillyl alcohol is a biological metabolite of Hydroxytyrosol. Hydroxytyrosol is a phenolic compound that is present in virgin olive oil (VOO) and wine. Homovanillyl alcohol protects red blood cells (RBCs) from oxidative injury and has protective effect on cardiovascular disease.
|
-
- HY-123268
-
|
Ro 363
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Ro 363, an effective inotropic stimulant, is a potent and highly selective β1-adrenoceptor agonist. RO 363 is a cardiovascular modulator that reduces diastolic blood pressure and pronounces increases in myocardial contractility.
|
-
- HY-126425
-
|
NCGC00262650
|
Others
|
Infection
|
|
NCGC00262650 is a potent apical membrane antigen 1-rhoptry neck protein 2 (AMA1-RON2) interaction inhibitor. NCGC00262650 can block entry of merozoites into red blood cells.
|
-
- HY-123268A
-
|
Ro 363 hydrochloride
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Ro 363 hydrochloride, an effective inotropic stimulant, is a potent and highly selective β1-adrenoceptor agonist. Ro 363 hydrochloride is a cardiovascular modulator that reduces diastolic blood pressure and pronounces increases in myocardial contractility.
|
-
- HY-143877
-
|
NN-390
|
HDAC
|
Cancer
|
|
NN-390 is a potent and selective HDAC6 inhibitor, with an IC50 of 9.8 nM. NN-390 penetrates the blood-brain barrier (BBB). NN-390 shows study potential in metastatic Group 3 MB (medulloblastoma).
|
-
- HY-N0304
-
|
L-DOPA
Levodopa; 3,4-Dihydroxyphenylalanine
|
Dopamine Receptor
Endogenous Metabolite
|
Neurological Disease
|
|
L-DOPA (Levodopa) is an orally active metabolic precursor of neurotransmitters dopamine. L-DOPA can cross the blood-brain barrier and is converted into dopamine in the brain. L-DOPA has anti-allodynic effects and the potential for Parkinson's disease.
|
-
- HY-B2130A
-
|
Uric acid sodium
Monosodium urate
|
Reactive Oxygen Species
Endogenous Metabolite
|
Metabolic Disease
|
|
Uric acid sodium (Monosodium urate), scavenger of oxygen radical, is a very important antioxidant that help maintains the stability of blood pressure and antioxidant stress. Uric acid sodium can remove reactive oxygen species (ROS) such as singlet oxygen and peroxynitrite, inhibiting lipid peroxidation.
|
-
- HY-P3160
-
|
Fibronectin
|
Integrin
|
Inflammation/Immunology
Cardiovascular Disease
|
|
Fibronectin, a glycoprotein (~500 kDa) present in blood as well as in cells, is a biomarker of tissue injury. Fibronectin binds to membrane-spanning receptor proteins called integrins. Fibronectin also binds to other extracellular matrix proteins such as collagen, fibrin, and heparan sulfate proteoglycans.
|
-
- HY-148465
-
|
Gadoteric acid
|
Biochemical Assay Reagents
|
Cancer
Cardiovascular Disease
|
|
Gadoteric acid is a macrocyclic, paramagnetic, gadolinium-based contrast agent that can be used for magnetic resonance imaging (MRI) of the brain, spine, and related tissues. In particular, Gadoteric acid is able to detect and visualize areas of blood-brain barrier disruption and abnormal vascular distribution.
|
-
- HY-101456
-
-
- HY-110180
-
|
VU0409106
|
mGluR
|
Neurological Disease
|
|
VU0409106 is a potent and selective mGlu5 negative allosteric modulator (NAM) with an IC50 of 24 nM. VU0409106 shows anxiolytic effects in rat models in a concentration-dependent manner. VU0409106 also penetrates the blood-brain barrier (BBB).
|
-
- HY-125017
-
|
Bozitinib
PLB-1001; CBT-101; Vebreltinib
|
c-Met/HGFR
|
Cancer
|
|
Bozitinib (PLB-1001) is a highly selective c-MET kinase inhibitor with blood-brain barrier permeability. Bozitinib (PLB-1001) is a ATP-competitive small-molecule inhibitor, binds to the conventional ATP-binding pocket of the tyrosine kinase superfamily.
|
-
- HY-17004S1
-
-
- HY-B0589
-
-
- HY-10328
-
|
Neflamapimod
VX-745
|
p38 MAPK
Autophagy
|
Inflammation/Immunology
|
|
Neflamapimod (VX-745) is a potent, blood-brain barrier penetrant, highly selective inhibitor of p38α inhibitor with an IC50 for p38α of 10 nM and for p38β of 220 nM. Neflamapimod (VX-745) possesses anti-inflammatory activity.
|
-
- HY-B1287
-
|
Citalopram hydrobromide
(±)-Citalopram hydrobromide; Lu 10-171
|
Serotonin Transporter
Autophagy
|
Neurological Disease
Cancer
|
|
Citalopram hydrobromide is a selective serotonin reuptake inhibitor (SSRI). Citalopram hydrobromide inhibits 5-HT uptake into synaptosomes with an IC50 of 1.8 nM. Citalopram hydrobromideinhibits the 5-HT uptake in rabbit blood platelets with an IC50 of 14 nM. Antidepressant effect.
|
-
- HY-D0873
-
|
HEPPS
EPPS
|
Amyloid-β
|
Neurological Disease
|
|
HEPPS (EPPS) is a buffering agent with the useful pH range from 7.3 ~ 8.7. HEPPS reduces Aβ-aggregate-induced memory deficits and rescues cognitive deficits in mice. EPPS is orally active and penetrates the blood-brain barrier.
|
-
- HY-105077A
-
|
Nemifitide diTFA
INN 00835 diTFA
|
5-HT Receptor
|
Neurological Disease
|
|
Nemifitide diTFA (INN 00835 diTFA) is a synthetic pentapeptide antidepressant with a potential for rapid onset of action. Nemifitide diTFA is a peptide analog of melanocyte-inhibiting factor (MIF). Nemifitide diTFA can cross the blood-brain barrier.
|
-
- HY-143464
-
|
BChE-IN-4
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
BChE-IN-4 is a potent and cross the blood-brain barrier BChE inhibitor. BChE-IN-4 attenuates learning and memory deficits caused by cholinergic deficit in mouse model. BChE-IN-4 has the potential for the research of alzheimer’s disease.
|
-
- HY-129441
-
-
- HY-P2491
-
-
- HY-P3585
-
|
Epobis
|
TNF Receptor
|
Inflammation/Immunology
Neurological Disease
|
|
Epobis, a dendrimeric peptide, is a recombinant form of erythropoietin. Epobis is a potent erythropoietin receptor agonist. Epobis promotes neuritogenesis in primary motoneurons. Epobis decrease TNF release and crosses the blood-brain barrier. Epobis has anti-inflammatory and memory enhancing properties.
|
-
- HY-127034
-
-
- HY-15556A
-
-
- HY-15556
-
-
- HY-125791
-
-
- HY-18725
-
-
- HY-148838
-
|
c-Myc inhibitor 8
|
c-Myc
|
Cancer
|
|
c-Myc inhibitor 8 (compound 56) is a c-Myc inhibitor. c-Myc inhibitor 8 effectively inhibits cell viability of a variety of cancer cells. c-Myc inhibitor 8 inhibits human prostate and lung cancer growth in mouse models. c-Myc inhibitor 8 can be used for cancer research.
|
-
- HY-P3069
-
-
- HY-113151
-
-
- HY-135281
-
-
- HY-18725A
-
-
- HY-148922
-
|
PPARα/γ agonist 2
|
PPAR
|
Metabolic Disease
|
|
PPARα/γ agonist 2 is an orally active PPARα full agonist and PPARγ partial agonist. PPARα/γ agonist 2 activates PPARα and PPARγ with EC50 values of 0.95 μM and 0.91 μM respectively. PPARα/γ agonist 2 is also a PTP1B inhibitor. PPARα/γ agonist 2 is an anti-diabetic agent.
|
-
- HY-A0195
-
|
Carboprost tromethamine
|
Prostaglandin Receptor
|
Endocrinology
|
|
Carboprost tromethamine is the synthetic 15-methyl analogue of prostaglandin F2α. Carboprost tromethamine can effectively promote law contraction of the uterus and significantly reduce the amount of bleeding during and after delivery.
|
-
- HY-B0317
-
|
Amlodipine
|
Calcium Channel
|
Cancer
Cardiovascular Disease
|
|
Amlodipine, an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine can be used for the research of high blood pressure and cancer.
|
-
- HY-146588
-
|
NMDA receptor antagonist 4
|
iGluR
|
Neurological Disease
|
|
NMDA receptor antagonist 4 (IIc) is a uncompetitive, voltage-dependent, orally active NMDAR blocker, with an IC50 of 1.93 µM. NMDA receptor antagonist 4 shows a positive predicted blood-brain-barrier (BBB) permeability, and can be studied in Alzheimer's disease.
|
-
- HY-B0317C
-
|
Amlodipine mesylate
|
Calcium Channel
|
Cancer
Cardiovascular Disease
|
|
Amlodipine mesylate, an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine mesylate can be used for the research of high blood pressure and cancer.
|
-
- HY-15321
-
|
Etoricoxib
MK-0663; L-791456
|
COX
|
Inflammation/Immunology
Cancer
|
|
Etoricoxib (MK-0663) is a non steroidal anti-inflammatory agent, acting as a selective and orally active COX-2 inhibitor, with IC50s of 1.1 μM and 116 μM for COX-2 and COX-1 in human whole blood.
|
-
- HY-135377
-
-
- HY-17423E
-
|
Abacavir hydrochloride
|
HIV
Apoptosis
Reverse Transcriptase
Telomerase
|
Cancer
Infection
|
|
Abacavir hydrochloride is a competitive, orally active nucleoside reverse transcriptase inhibitor. Abacavir hydrochloride can inhibits the replication of HIV. Abacavir hydrochloride shows anticancer activity in prostate cancer cell lines. Abacavir hydrochloride can trespass the blood-brain-barrier and suppresses telomerase activity.
|
-
- HY-100238
-
-
- HY-N0029
-
|
Forsythoside B
|
TNF Receptor
NF-κB
|
Inflammation/Immunology
|
|
Forsythoside B is a phenylethanoid glycoside isolated from Forsythia suspensa (Thunb.) Vahl, a Chinese folk medicinal plant for treating inflammatory diseases and promoting blood circulation. Forsythoside B could inhibit TNF-alpha, IL-6, IκB and modulate NF-κB.
|
-
- HY-12515B
-
|
(S)-Nicardipine
(S)-YC-93 free base
|
Calcium Channel
|
Neurological Disease
Cardiovascular Disease
|
|
(S)-Nicardipine ((S)-YC-93 free base) is the less active S enantiomer of Nicardipine. Nicardipine is a calcium channel blocker with an IC50 of 1 μM for blocking cardiac calcium channels. Nicardipine acts as an agent for chronic stable angina and for controlling blood pressure.
|
-
- HY-W145497
-
|
D-(+)-Sorbose
|
Insulin Receptor
|
Metabolic Disease
|
|
D-(+)-Sorbose, an active enantiomer of D-Sorbose, which inhibits disaccharidase activity and demonstrates suppressive action on postprandial blood levels of glucose and insulin in the rat. D-sorbose acts as a sweetener may contribute to the prevention of lifestyle-related diseases, such as type 2 diabetes mellitus.
|
-
- HY-17423
-
|
Abacavir
|
HIV
Reverse Transcriptase
Telomerase
Apoptosis
|
Cancer
Infection
|
|
Abacavir is an orally active and competitive nucleoside reverse transcriptase inhibitor. Abacavir can inhibits the replication of HIV. Abacavir shows anticancer activity in prostate cancer cell lines. Abacavir can trespass the blood-brain-barrier and suppresses telomerase activity.
|
-
- HY-109106A
-
|
Upacicalcet sodium
|
CaSR
|
Endocrinology
|
|
Upacicalcet sodium is an intravenous calcimimetic agent. Upacicalcet suppresses excessive parathyroid hormone (PTH) secretion, thereby lowering blood PTH levels, by acting directly on parathyroid cell membrane calcium-sensing receptors. Upacicalcet can be used for researching the disease of secondary hyperparathyroidism (SHPT).
|
-
- HY-B0259S
-
|
(rac)-Indapamide-d3
|
Potassium Channel
|
Cardiovascular Disease
|
|
(rac)-Indapamide-d3 is a labelled racemic Indapamide. Indapamide is an orally active sulphonamide diuretic agent, that can reduce blood pressure by decreasing vascular reactivity and peripheral vascular resistance. Indapamide is also can reduce left ventricular hypertrophy[1][4].
|
-
- HY-109106
-
|
Upacicalcet
|
CaSR
|
Endocrinology
|
|
Upacicalcet is an intravenous calcimimetic agent. Upacicalcet suppresses excessive parathyroid hormone (PTH) secretion, thereby lowering blood PTH levels, by acting directly on parathyroid cell membrane calcium-sensing receptors. Upacicalcet can be used for researching the disease of secondary hyperparathyroidism (SHPT).
|
-
- HY-B0762S
-
|
Acetyl-L-carnitine-d3 hydrochloride
O-Acetyl-L-carnitine-d3 (hydrochloride)
|
Endogenous Metabolite
|
Neurological Disease
|
|
Acetyl-L-carnitine-d3 (hydrochloride) is the deuterium labeled Acetyl-L-carnitine hydrochloride. Acetyl-L-carnitine hydrochloride is a blood-brain permeable acetyl ester of the amino acid L-carnitine found in the body. Acetyl-L-carnitine hydrochloride is often used as a dietary supplement, and exibits anti-stress-related psychiatric disorders[1].
|
-
- HY-148419
-
|
TNG908
|
Histone Methyltransferase
|
Cancer
|
|
TNG908 is a MTAP-cooperative PRMT5 inhibitor that can pass through the blood-brain barrier. TNG908 is 15 times more selective for MTAP null cell lines than MTAP WT cell lines, and can be used in cancer research.
|
-
- HY-148565
-
-
- HY-N11061
-
|
Withaphysalin D
|
iGluR
|
Neurological Disease
|
|
Withaphysalin D is a selective antagonist against the N-methyl-D-aspartate receptor (NMDAR) containing GluN2B. Withaphysalin D can be isolated from water lilies and has neuroprotective properties. Withaphysalin D is able to cross the blood-brain barrier.
|
-
- HY-109018B
-
|
Velagliflozin proline hydrate
|
SGLT
|
Metabolic Disease
|
|
Velagliflozin proline hydrate is the clinical form of Velagliflozin (HY-109018). Velagliflozin is an oral sodium-glucose cotransporter 2 (SGLT2) inhibitor with antidiabetic activity. Velagliflozin reduces renal glucose reabsorption and stimulates glycosuria, which lowers blood sugar and insulin concentrations.
|
-
- HY-17449
-
|
Fosbretabulin disodium
CA 4DP; CA 4P; Combretastatin A4 disodium phosphate
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Fosbretabulin disodium (CA 4DP) is a tubulin destabilizing agent. Fosbretabulin disodium is the Combretastatin A4 proagent that selectively targets endothelial cells, induces regression of nascent tumour neovessels, reduces tumour blood flow and causes central tumour necrosis.
|
-
- HY-N0304A
-
|
L-DOPA sodium
Levodopa sodium; 3,4-Dihydroxyphenylalanine sodium
|
Dopamine Receptor
Endogenous Metabolite
|
Neurological Disease
|
|
L-DOPA (Levodopa) sodium is an orally active metabolic precursor of neurotransmitters dopamine. L-DOPA sodium can cross the blood-brain barrier and is converted into dopamine in the brain. L-DOPA sodium has anti-allodynic effects, and can be used for Parkinson's disease research.
|
-
- HY-N6608
-
|
Physostigmine
Eserine
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Physostigmine (Eserine) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine can crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine is also an antidote for anticholinergic poisoning.
|
-
- HY-N2160
-
|
6'''-Feruloylspinosin
|
GABA Receptor
|
Neurological Disease
|
|
6'''-Feruloylspinosin is a flavonoid isolated from seeds of Ziziphus jujuba. 6'''-Feruloylspinosin can across the blood-brain barrier and enhance the expression of GABAAα1, GABAAα5, and GABABR1 mRNA in rat hippocampal neurons.
|
-
- HY-108295
-
|
Pivagabine
CXB-722
|
GABA Receptor
|
Neurological Disease
|
|
Pivagabine (CXB 722) is a hydrophobic 4-aminobutyric acid derivative with neuromodulatory activity. Pivagabine penetrates the blood-brain barrier in rats. Pivagabine antagonizes the effects of foot shock on both GABAA receptor function and corticotropin-releasing factor (CRF) concentrations in rat brain.
|
-
- HY-106509
-
|
Velaresol
BW 12C; 12C79; BW 12C79
|
Others
|
Others
|
|
Velaresol (BW 12C) is a potent left-shifting anti-sickling compound in vitro. Sickle cell disease is an inherited disorder of the hemoglobin molecule. When hemoglobin molecules are exposed to a variety of environments, the red blood cell hemoglobin polymerizes, twists, and morphs into a sickle shape.
|
-
- HY-18236
-
|
MDL-28170
Calpain Inhibitor III
|
Proteasome
|
Inflammation/Immunology
Neurological Disease
|
|
MDL-28170 (Calpain Inhibitor III) is a potent, selective and membrane-permeable cysteine protease inhibitor of calpain that rapidly penetrates the blood-brain barrier following systemic administration. MDL-28170 also block γ-secretase.
|
-
- HY-W050031
-
|
(S)-3-Hydroxybutanoic acid
(S)-β-Hydroxybutanoic acid; L-(+)-3-Hydroxybutyric acid; L-β-Hydroxybutyric acid
|
Endogenous Metabolite
|
Others
|
|
(S)-3-Hydroxybutanoic acid is a normal human metabolite, that has been found elevated in geriatric patients remitting from depression. In humans, 3-Hydroxybutyric acid is synthesized in the liver from acetyl-CoA, and can be used as an energy source by the brain when blood glucose is low.
|
-
- HY-B0762S1
-
|
Acetyl-L-carnitine-d3-1 hydrochloride
O-Acetyl-L-carnitine-d3-1 (hydrochloride)
|
Endogenous Metabolite
|
Neurological Disease
|
|
Acetyl-L-carnitine-d3-1 (hydrochloride) is the deuterium labeled Acetyl-L-carnitine hydrochloride. Acetyl-L-carnitine hydrochloride is a blood-brain permeable acetyl ester of the amino acid L-carnitine found in the body. Acetyl-L-carnitine hydrochloride is often used as a dietary supplement, and exibits anti-stress-related psychiatric disorders[1].
|
-
- HY-N0496
-
|
Ruscogenin
|
NOD-like Receptor (NLR)
|
Cardiovascular Disease
|
|
Ruscogenin, an important steroid sapogenin derived from Ophiopogon japonicus, attenuates cerebral ischemia-induced blood-brain barrier dysfunction by suppressing TXNIP/NLRP3 inflammasome activation and the MAPK pathway and exerts significant anti-inflammatory and anti-thrombotic activities.
|
-
- HY-B0317A
-
|
Amlodipine maleate
|
Calcium Channel
|
Cancer
Cardiovascular Disease
|
|
Amlodipine maleate is a dihydropyridine calcium channel blocker, acts as an orally active antianginal agent. Amlodipine maleate blocks the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine maleate can be used for the research of high blood pressure and cancer.
|
-
- HY-B0757A
-
-
- HY-19837
-
-
- HY-P1052
-
|
Myelin Basic Protein(87-99)
|
Others
|
Inflammation/Immunology
|
|
Myelin Basic Protein(87-99) is an encephalitogenic peptide that induces basic protein-specific T cell proliferation. Myelin Basic Protein(87-99) causes a Th1 polarization in peripheral blood mononuclear cells with is implicated of multiple sclerosis (MS).
|
-
- HY-152141
-
|
hCAII-IN-9
|
Carbonic Anhydrase
|
Others
|
|
hCAII-IN-9 is a potent carbonic anhydrase inhibitor with IC50s of 1.18 μM (hCA II), 0.17 μM (hCA IX), and 2.99 μM (hCA XII), respectively. hCAII-IN-9 has no blood-brain barrier permeability.
|
-
- HY-17034B
-
-
- HY-136346S
-
-
- HY-103023
-
|
CLP290
|
Potassium Channel
|
Neurological Disease
|
|
CLP290 is an orally available activator of the neuron-specific K +-Cl − cotransporter KCC2, displays potential for treatment of a wide range of neurological and psychiatric indications. CLP290 can significantly lower blood arginine-vasopressin (AVP) and glucose levels in STZ rats.
|
-
- HY-108024A
-
|
Ganaplacide hydrochloride
KAF156 hydrochloride; GNF156 hydrochloride
|
Parasite
|
Infection
|
|
Ganaplacide (KAF156) hydrochloride is a first-in-class, orally active imidazolopiperazine antimalarial agent. Ganaplacide hydrochloride is active against a broad range of Plasmodium species, including drug-resistant parasites. Ganaplacide hydrochloride is parasiticidal against both asexual and sexual blood stages as well as the liver stages of the parasite.
|
-
- HY-A0115S1
-
-
- HY-139464
-
-
- HY-B1192S
-
|
Estradiol benzoate-d3
β-Estradiol 3-benzoate-d3; 17β-Estradiol 3-benzoate-d3
|
Estrogen Receptor/ERR
|
|
|
Estradiol benzoate-d3 is the deuterium labeled Estradiol benzoate. Estradiol Benzoate (β-Estradiol 3-benzoate), a proagent of estradiol, acts as a steroid sex hormone. It exhibits mild anabolic and metabolic properties, and increases blood coagulability[1][2][3][4].
|
-
- HY-B0227S1
-
|
Ketoprofen-d4
RP-19583-d4
|
COX
Apoptosis
|
Inflammation/Immunology
|
|
Ketoprofen-d4 is the deuterium labeled Ketoprofen. Ketoprofen (RP-19583) is a non-steroidal antiinflammatory agent, acting as a potent inhibitor of COX, with IC50s of 2 nM and 26 nM for COX-1 and COX-2 in human blood monocytes, respectively[1].
|
-
- HY-B0109S
-
|
Dorzolamide-d5
|
Carbonic Anhydrase
|
Cancer
|
|
Dorzolamide-d5 is the deuterium labeled Dorzolamide. Dorzolamide (L671152) is a potent carbonic anhydrase II inhibitor, with IC50 values of 0.18 nM and 600 nM for red blood cell CA-II and CA-I respectively. Dorzolamide possesses anti-tumor activity[1][2].
|
-
- HY-13788
-
-
- HY-15760
-
-
- HY-B0569
-
|
Hexamethonium Bromide
|
nAChR
Apoptosis
|
Neurological Disease
Cardiovascular Disease
|
|
Hexamethonium Bromide is a non-selective ganglionic nicotinic-receptor antagonist (nAChR) antagonist, with mixed competitive and noncompetitive activity. Hexamethonium Bromide has anti-hypertensive activity. Hexamethonium Bromide attenuates sympathetic activity and blood pressure in spontaneously hypertensive animal models.
|
-
- HY-17034
-
-
- HY-32015
-
|
Cot inhibitor-1
|
MAP3K
|
Inflammation/Immunology
|
|
Cot inhibitor-1 (compound 28) is a selective tumor progression loci-2 (Tpl2) kinase inhibitor with an IC50 of 28 nM. Cot inhibitor-1 shows an inhibition of TNF-alpha production in human whole blood with an IC50 of 5.7 nM.
|
-
- HY-B0186B
-
|
Cefoselis sulfate
FK-037
|
Bacterial
Antibiotic
|
Infection
|
|
Cefoselis sulfate (FK-037), the fourth gen-eration of cephalosporin, is a β-lactam antibiotic. Cefoselis sulfate exhibits good activity against a wide range of Gram-positive and Gram-negative organisms. Cefoselis sulfate penetrates the blood-brain barrier.
|
-
- HY-149212
-
|
SD-6
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
SD-6 is an orally active inhibitor of hAChE and hBChE with IC50 values of 0.907 µM and 1.579 µM, respectively. SD-6 has excellent blood-brain barrier (BBB) permeability and no neurotoxicity, which can be used for research on Alzheimer's disease.
|
-
- HY-11030A
-
-
- HY-120738
-
|
p-MPPI hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
|
p-MPPI hydrochloride is a selective 5-HT1A receptor antagonist with high affinity for 5-HT1A receptors. p-MPPI hydrochloride can crosses the blood-brain barrier, and has clear antidepressant and anxiolytic-like effects.
|
-
- HY-13788B
-
-
- HY-50682
-
|
Azeliragon
TTP488; PF-04494700
|
Amyloid-β
|
Neurological Disease
|
|
Azeliragon (TTP488) is an orally bioavailable inhibitor of the receptor for advanced glycation end products (RAGE) in development as a potential treatment to slow disease progression in patients with mild Alzheimer’s disease (AD). Azeliragon also can cross the blood-brain barrier (BBB).
|
-
- HY-B0227S
-
|
Ketoprofen-d3
RP-19583-d3
|
COX
Apoptosis
|
Inflammation/Immunology
|
|
Ketoprofen-d3 is the deuterium labeled Ketoprofen. Ketoprofen (RP-19583) is a non-steroidal antiinflammatory agent, acting as a potent inhibitor of COX, with IC50s of 2 nM and 26 nM for COX-1 and COX-2 in human blood monocytes, respectively[1].
|
-
- HY-N6857
-
|
Armepavine
|
NF-κB
|
Inflammation/Immunology
|
|
Armepavine, an active compound from Nelumbo nucifera, exerts not only anti-inflammatory effects on human peripheral blood mononuclear cells, but also immunosuppressive effects on T lymphocytes and on lupus nephritic mice. Armepavine inhibits TNF-α-induced MAPK and NF-κB signaling cascades.
|
-
- HY-N6685S1
-
-
- HY-16693
-
|
LDN-27219
|
Others
|
Others
|
|
LDN-27219 is a reversible, slow-binding inhibitor of TGase. LDN-27219 inhibits human TGase with an IC50 value of 0.6 μM. LDN-27219 effectively decreases blood pressure and induces vasodilation, it can be used for the research of cardiovascular disease.
|
-
- HY-B0589E
-
-
- HY-132392S
-
-
- HY-15981
-
|
Omarigliptin
MK-3102
|
Dipeptidyl Peptidase
|
Metabolic Disease
Neurological Disease
|
|
Omarigliptin (MK-3102) is a potent, selective, orally active and cross the blood-brain barrier dipeptidyl peptidase 4 (DPP-4) inhibitor. Omarigliptin shows anti-parkinsonian activity. Omarigliptin has the neuroprotective effect to improve diabetes-associated cognitive dysfunction.
|
-
- HY-109106B
-
|
(Rac)-Upacicalcet
|
CaSR
|
Endocrinology
|
|
(Rac)-Upacicalcet is the racemate of Upacicalcet.Upacicalcet is an intravenous calcimimetic agent. Upacicalcet suppresses excessive parathyroid hormone (PTH) secretion, thereby lowering blood PTH levels, by acting directly on parathyroid cell membrane calcium-sensing receptors. Upacicalcet can be used for researching the disease of secondary hyperparathyroidism (SHPT).
|
-
- HY-P2752
-
|
Lipoprotein lipase
LPL
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Lipoprotein lipase Lipoprotein lipase is a multifunctional enzyme from adipose tissue, heart and skeletal muscle, islets and macrophages. Lipoprotein lipase promotes normal lipoprotein metabolism, delivery and utilization of tissue-specific substrates. Lipoprotein lipase catalyzes the rate-limiting step of lipids in blood circulation.
|
-
- HY-17547
-
|
NMS-E973
|
HSP
|
Cancer
|
|
NMS-E973 is a potent and selective inhibitor of HSP90. NMS-E973 binds to the ATP binding site of Hsp90α with a DC50 of <10 nM. NMS-E973 is able to cross the blood-brain barrier (BBB). Antitumor efficacy.
|
-
- HY-N7109
-
|
Erucic acid
|
PI3K
Endogenous Metabolite
|
Neurological Disease
|
|
Erucic acid, a monounsaturated fatty acid (MUFA), is isolated from the seed of Raphanus sativus L. Erucic acid can readily cross the blood-brain barrier (BBB), it has been reported to normalize the accumulation of very long-chain fatty acids in the brain. Erucic acid can improve cognitive impairment and be effective against dementia
.
|
-
- HY-12515C
-
|
(R)-Nicardipine
(R)-YC-93 free base
|
Calcium Channel
|
Neurological Disease
Cardiovascular Disease
|
|
(R)-Nicardipine ((R)-YC-93 free base) is the less active R enantiomer of Nicardipine. Nicardipine (YC-93) is a calcium channel blocker with an IC50 of 1 μM for blocking cardiac calcium channels. Nicardipine acts as an agent for chronic stable angina and for controlling blood pressure.
|
-
- HY-106667
-
|
DL 071IT
|
Adrenergic Receptor
|
Endocrinology
Cardiovascular Disease
|
|
DL 071IT is a potent non-selective beta-adrenergic receptor blocker. DL 071IT exhibits intrinsic sympathomimetic activity and weak membrane stabilizing activity. DL 071IT reduces exercise heart rate and systolic blood pressure, and even significantly lowers resting heart rate.
|
-
- HY-112948
-
|
2-Methylbutyrylcarnitine
|
Endogenous Metabolite
|
Metabolic Disease
|
|
2-Methylbutyrylcarnitine is a fatty acid metabolite. 2-Methylbutyrylcarnitine is found mainly in the blood and urine of humans and animals and is produced through the pyruvate carboxylation pathway. 2-Methylbutyrylcarnitine exhibits high level in the plasma of subjects with steatohepatitis (NASH) and can be used as an indicator for the diagnosis of metabolic diseases.
|
-
- HY-145884
-
|
BTK-IN-8
|
Btk
|
Inflammation/Immunology
|
|
BTK-IN-8 is a potent selective peripheral covalent BTK inhibitor (IC50=0.22 nM; Kd=0.91 nM). BTK-IN-8 has good whole blood CD69 cellular potency (IC50=0.029 µM).
|
-
- HY-B0317B
-
|
Amlodipine besylate
Amlodipine benzenesulfonate
|
Calcium Channel
|
Cancer
Cardiovascular Disease
|
|
Amlodipine besylate (Amlodipine benzenesulfonate), an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine besylate can be used for the research of high blood pressure and cancer.
|
-
- HY-151615
-
|
DCI-Br-3
|
Fluorescent Dye
|
Neurological Disease
|
|
DCI-Br-3 is a rapid, highly sensitive, and selective probe to monitor thiols in the epileptic brain. (λex=537 nm, λem=675 nm).DCI-Br-3 can effectively cross the blood-brain barrier (BBB). Storage: protect from light.
|
-
- HY-129411
-
|
Sinbaglustat
ACT-519276; OGT2378
|
Glucosylceramide Synthase (GCS)
|
Metabolic Disease
|
|
Sinbaglustat (OGT2378) is a dual inhibitor of glucosylceramide synthase (GCS) and non-lysosomal glucosyl ceramidase (GBA2). Sinbaglustat is an orally available N-alkyl iminosugar that crosses the blood-brain barrier. Sinbaglustat can be used for the research of central neurodegenerative diseases associated with lysosomal dysfunctions.
|
-
- HY-108448
-
|
N-Oleoyldopamine
OLDA
|
TRP Channel
|
Cardiovascular Disease
|
|
N-Oleoyldopamine (OLDA) is a product of condensation of oleic acid and dopamine (DA) and an endogenous TRPV1 selective agonist. N-Oleoyldopamine (OLDA) can crosses the blood-brain barrier. N-oleoyl-dopamine protects the heart against ischemia-reperfusion injury via activation of TRPV1.
|
-
- HY-B0002A
-
|
Ondansetron hydrochloride dihydrate
GR 38032 hydrochloride dihydrate; SN 307 hydrochloride dihydrate
|
5-HT Receptor
|
Neurological Disease
|
|
Ondansetron (GR 38032) hydrochloride dehydrate is an orally active, highly selective and competitive 5-HT3 receptor antagonist (crosses the blood-brain barrier). Ondansetron hydrochloride dehydrate can be used in studies of preventing nausea and vomiting associated with cancer chemotherapy, radiation therapy and surgery.
|
-
- HY-W127357
-
|
Tripelargonin
|
Biochemical Assay Reagents
|
Others
|
|
Glyceryl trinonanoate is a triacylglycerol containing nonanoic acid at the sn-1, sn-2 and sn-3 positions. It has been found in Schizochytrium biomass. 1 1,2,3-Trinonanoyl-rac-glycerol increases blood levels of the ketone body D-(-)-3-hydroxybutyrate in neonatal rhesus monkeys. 2|1. Mioso, R., Toledo Marante, FJ, González, JE, et al. Schizochytrium sp. metabolite analysis. Oleaginous microbial sources of biodiesel by GC-MS. braz. J. Microbiology. 45(2), 403-409 (2014).|2. Tetrick, MA, Greer, FR and Benevenga, NJ Blood D- (?)-3-Hydroxybutyric acid concentration. Compare. medicine. 60(6), 486-490 (2010).
|
-
- HY-15321S
-
|
Etoricoxib-d4
MK-0663-d4; L-791456-d4
|
COX
|
Others
|
|
Etoricoxib-d4 is a deuterium labeled Etoricoxib. Etoricoxib is a non steroidal anti-inflammatory agent, acting as a selective and orally active COX-2 inhibitor, with IC50s of 1.1 μM and 116 μM for COX-2 and COX-1 in human whole blood.
|
-
- HY-103234
-
|
GYKI 52466
|
iGluR
|
Neurological Disease
|
|
GYKI 52466 is an orally active, highly selective and noncompetitive AMPA/kainate receptor antagonist with the IC50 values of 7.5 and 11μM, respectively. GYKI 52466 has good blood brain barrier permeability and anticonvulsant effect. GYKI 52466 can be used in Parkinson's disease research.
|
-
- HY-N0712
-
|
Typhaneoside
|
Autophagy
|
Inflammation/Immunology
Cardiovascular Disease
|
|
Typhaneoside, extracted from Typha angustifolia L., Typhaneoside can inhibit the excessive autophagy of hypoxia/reoxygenation cells and increase the phosphorylation of Akt and mTOR. Typhaneoside has certain effects on the cardiovascular system, including lowering blood lipid levels, promoting antiatherosclerosis activities, as well as improving immune and coagulation function.
|
-
- HY-B0589A
-
-
- HY-N0729
-
|
Linoleic acid
octadeca-9,12-dienoic acid
|
Endogenous Metabolite
|
Metabolic Disease
Cardiovascular Disease
Cancer
|
|
Linoleic acid is a common polyunsaturated (PUFA) found in plant-based oils, nuts and seeds. Linoleic acid is a part of membrane phospholipids, and functions as a structural component to maintain a certain level of membrane fluidity of the transdermal water barrier of the epidermis. Linoleic acid induces red blood cells and hemoglobin damage via oxidative mechanism .
|
-
- HY-149242
-
|
MAO-B-IN-20
|
Monoamine Oxidase
|
Neurological Disease
|
|
MAO-B-IN-20 (Compound C14) is a potent MAO-B inhibitor with an IC50 of 0.037 μM. MAO-B-IN-20 displays good metabolic stability and brain-blood barrier permeability. MAO-B-IN-20 can be used for the research of Parkinson's disease.
|
-
- HY-103234A
-
|
GYKI 52466 dihydrochloride
|
iGluR
|
Neurological Disease
|
|
GYKI 52466 dihydrochloride is an orally active, highly selective and noncompetitive AMPA/kainate receptor antagonist with the IC50 values of 7.5 and 11μM, respectively. GYKI 52466 dihydrochloride has good blood brain barrier permeability and anticonvulsant effect. GYKI 52466 dihydrochloride can be used in Parkinson's disease research.
|
-
- HY-103200
-
-
- HY-W083062
-
|
hMAO-B-IN-5
|
Monoamine Oxidase
|
Neurological Disease
|
|
hMAO-B-IN-5(B15) is a potent, selective and reversible inhibitor of human monoamine oxidase hMAO-B with IC50 of 0.12 μM. hMAO-B-IN-5 can pass through the blood-brain barrier and can be used in the research of neurodegenerative diseases.
|
-
- HY-N7062
-
|
JNJ-1661010
Takeda-25
|
FAAH
|
Neurological Disease
|
|
JNJ-1661010 (Takeda-25) a potent and selective fatty acid amide hydrolase (FAAH) inhibitor with IC50s of 34 and 33 nM for rat FAAH and human FAAH, respectively. JNJ-1661010 can cross the blood-brain barrier and used as broad-spectrum analgesics.
|
-
- HY-15615A
-
|
Dordaviprone
TIC10; ONC-201
|
TNF Receptor
Apoptosis
|
Cancer
|
|
Dordaviprone (TIC10) is a potent, orally active, and stable tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) inducer which acts by inhibiting Akt and ERK, consequently activating Foxo3a and significantly inducing cell surface TRAIL. Dordaviprone can cross the blood-brain barrier.
|
-
- HY-103460
-
|
IRL 2500
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
IRL 2500 is a potent Endothelin receptor antagonist. IRL 2500 shows IC50 values of 1.3 and 94 nM for ETB and ETA receptors, respectively. IRL 2500 inhibits ETB receptor-mediated blood pressure increase and renal vascular resistance in rats in vivo.
|
-
- HY-113067S
-
|
Phytanic acid-d3
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Phytanic acid-d3 is the deuterium labeled Phytanic acid[1]. Phytanic acid is an endogenous metabolite present in Blood that can be used for the research of Zellweger Syndrome, Alpha Methylacyl CoA Racemase Deficiency, Rhizomelic Chondrodysplasia Punctata and Infantile Refsum Disease[2][3][4][5][6].
|
-
- HY-14858
-
|
Derenofylline
SLV 320
|
Adenosine Receptor
|
Cardiovascular Disease
|
|
Derenofylline (SLV 320) is a potent, selective and orally active adenosine A1 receptor antagonist, with Ki values of 1 nM, 200 nM and 398 nM for human A1, A3 and A2A receptors respectively. Derenofylline suppresses cardiac fibrosis and attenuates albuminuria without affecting blood pressure in rats.
|
-
- HY-100672
-
-
- HY-17423B
-
|
Abacavir monosulfate
|
HIV
Reverse Transcriptase
Telomerase
Apoptosis
|
Cancer
Infection
|
|
Abacavir monosulfate is a competitive, orally active nucleoside reverse transcriptase inhibitor. Abacavir monosulfate can inhibits the replication of HIV. Abacavir monosulfate shows anticancer activity in prostate cancer cell lines. Abacavir monosulfate can trespass the blood-brain-barrier and suppresses telomerase activity.
|
-
- HY-151894
-
|
I-BET432
|
Epigenetic Reader Domain
|
Cancer
|
|
I-BET432 is a BET inhibitor. I-BET432 inhibits BRD4 N-terminal bromodomain (BD1) and the C-terminal bromodomain (BD2) with pIC50 values of 7.5 and 7.2, respectively. I-BET432 can be used as an oral candidate quality molecule for the research of multiple oncology and inflammatory diseases.
|
-
- HY-B0883
-
|
Proflavine hemisulfate
Proflavin hemisulfate; 3,6-Diaminoacridine hemisulfate
|
Bacterial
Potassium Channel
Autophagy
|
Infection
Cancer
|
|
Proflavine hemisulfate, an acridine dye, is a known DNA intercalating agent. Anti-microbial agent. Proflavine hemisulfate behaves as a pore blocker for Kir3.2. Proflavine hemisulfate is a potential lead compound for Kir3.2-associated neurological diseases.
|
-
- HY-B1741
-
|
Proflavine
3,6-Diaminoacridine
|
Bacterial
|
Neurological Disease
|
|
Proflavine, an acridine dye, is a known DNA intercalating agent. Anti-microbial agent. Proflavine behaves as a pore blocker for Kir3.2. Proflavine is a potential lead compound for Kir3.2-associated neurological diseases.
|
-
- HY-B0562
-
|
Methyclothiazide
|
Carbonic Anhydrase
|
Metabolic Disease
Cardiovascular Disease
|
|
Methyclothiazide is an orally active antihypertensive agent and a diuretic agent. Methyclothiazide leads to a reduction of the vascular response to the action of endogenous vasoconstricting stimuli, such as Norepinephrine (HY-13715). Methyclothiazide is against voltage-dependent Ca-channel (VDCC) activity in vitro.
|
-
- HY-79457
-
-
- HY-18974
-
-
- HY-112070
-
-
- HY-N2492
-
|
(E)-Methyl 4-coumarate
Methyl trans-p-coumarate
|
Bacterial
Apoptosis
|
Cancer
Infection
|
|
(E)-Methyl 4-coumarate (Methyl 4-hydroxycinnamate), found in several plants, such as Allium cepa or Morinda citrifolia L. leaves. (E)-Methyl 4-coumarate cooperates with Carnosic Acid in inducing apoptosis and killing acute myeloid leukemia cells, but not normal peripheral blood mononuclear cells. Antioxidant and antimicrobial activity.
|
-
- HY-B0162
-
|
Ivabradine
|
HCN Channel
|
Cardiovascular Disease
|
|
Ivabradine is a potent and orally active HCN (hyperpolarization-activated cyclic nucleotide-gated) channel blocker that inhibits the cardiac pacemaker current (If). Ivabradine reduces dose-dependently heart rate without modification of blood pressure. Ivabradine shows anticonvulsant, anti-ischaemic and anti-anginal activity.
|
-
- HY-B2099
-
|
Buformin
1-Butylbiguanide
|
AMPK
|
Cancer
Metabolic Disease
|
|
Buformin (1-Butylbiguanide), a potent AMPK activator, acts as an orally active biguanide antidiabetic agent. Buformin decreases hepatic gluconeogenesis and lowers blood glucose production in vivo. Buformin also has anti-cancer activities and is applied in cancer study (such as, cervical cancer and breast cancer, et al).
|
-
- HY-146049
-
|
Antitrypanosomal agent 4
|
Parasite
|
Infection
|
|
Antitrypanosomal agent 4 (compound 19) is a potent and blood-brain barrier permeable antitrypanosomal agent. Antitrypanosomal agent 4 has good activity against Trypanosoma cruzi (T. cruzi) and Trypanosoma brucei brucei (T. b. brucei) with IC50s of 1.2 μM and 70 nM, respectively.
|
-
- HY-108625
-
|
SHA 68
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
SHA 68 is a potent and selective non-peptide neuropeptide S receptor (NPSR) antagonist with IC50s of 22.0 and 23.8 nM for NPSR Asn 107 and NPSR Ile 107, respectively. SHA 68 has limited the blood-brain barrier (BBB) penetration and the activity in neuralgia.
|
-
- HY-B2099A
-
|
Buformin hydrochloride
1-Butylbiguanide hydrochloride
|
AMPK
|
Cancer
|
|
Buformin hydrochloride (1-Butylbiguanide hydrochloride), a potent AMPK activator, acts as an orally active biguanide antidiabetic agent. Buformin hydrochloride decreases hepatic gluconeogenesis and lowers blood glucose production in vivo. Buformin hydrochloride also has anti-cancer activities and is applied in cancer study (such as, cervical cancer and breast cancer, et al).
|
-
- HY-144610
-
|
Mu opioid receptor antagonist 5
|
Opioid Receptor
|
Neurological Disease
|
|
Mu opioid receptor antagonist 5 (compound NAP) is a selective and blood-brain barrier (BBB) penetrant μ opioid receptor (MOR) antagonist with an EC50 value of 1.14 nM and a Ki value of 0.37 nM. Mu opioid receptor antagonist 5 can be used for researching opioid use disorders (OUD).
|
-
- HY-139293
-
|
PF-07059013
|
Others
|
Cardiovascular Disease
|
|
PF-07059013 is an orally active and potent noncovalent modulator of sickled hemoglobin (HbS). PF-07059013 specifically binds to Hb with nanomolar affinity and displays strong partitioning into red blood cells (RBCs). PF-07059013 can be used for sickle cell disease (SCD) research.
|
-
- HY-115475
-
|
SW-100
|
HDAC
|
Neurological Disease
|
|
SW-100, a selective histone deacetylase 6 (HDAC6) inhibitor with an IC50 of 2.3 nM, shows at least 1000-fold selectivity for HDAC6 relative to all other HDAC isozymes. SW-100 displays a significantly improved ability to cross the blood-brain-barrier.
|
-
- HY-143264
-
|
FAAH/MAGL-IN-2
|
FAAH
MAGL
|
Neurological Disease
|
|
FAAH/MAGL-IN-2 is a potent, reversible, orally active, and cross the blood-brain barrier FAAH and MAGL inhibitor with IC50s of 11 nM and 36 nM (Kis of 28 nM and 60 nM), respectively . FAAH/MAGL-IN-2 has the potential to research neuropathic pain without causing locomotion impairment.
|
-
- HY-129554
-
|
cis-9,10-Epoxystearic acid
cis-9,10-Epoxyoctadecanoic acid
|
Endogenous Metabolite
|
Others
|
|
cis-9,10-Epoxystearic acid (cis-9,10-Epoxyoctadecanoic acid) is an endogenous constituent in human blood and urine. cis-9,10-Epoxystearic acid (cis-9,10-Epoxyoctadecanoic acid) can be produced from oleic acid by enzymic and non-enzymic epoxidation.
|
-
- HY-B1266
-
|
Physostigmine salicylate
Eserine salicylate
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Physostigmine salicylate (Eserine salicylate) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine salicylate crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine salicylate can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine salicylate is also an antidote for anticholinergic poisoning.
|
-
- HY-B0162A
-
|
Ivabradine hydrochloride
|
HCN Channel
|
Cardiovascular Disease
Endocrinology
Cancer
|
|
Ivabradine hydrochloride is a potent and orally active HCN (hyperpolarization-activated cyclic nucleotide-gated) channel blocker that inhibits the cardiac pacemaker current (If). Ivabradine hydrochloride reduces dose-dependently heart rate without modification of blood pressure. Ivabradine hydrochloride shows anticonvulsant, anti-ischaemic and anti-anginal activity.
|
-
- HY-B0589C
-
|
(3S,5S)-Atorvastatin
|
Cytochrome P450
|
Metabolic Disease
|
|
(3S,5S)-Atorvastatin is a inactive enantiomer of Atorvastatin. (3S,5S)-Atorvastatin can activate pregnane X receptor (PXR). Atorvastatin is an orally active HMG-CoA reductase inhibitor, has the ability to effectively decrease blood lipids.
|
-
- HY-A0230
-
|
Spirapril
SCH 33844
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
Spirapril is a potent and cross the blood-brain barrier angiotensin converting enzyme (ACE) inhibitor with antihypertensive activity. Spirapril competitively binds to ACE and prevents the conversion of angiotensin I to angiotensin II. Spirapril is an orally active proagent of Spiraprilat and can be used for the research of hypertension, congestive heart failure.
|
-
- HY-103415
-
|
Nemonapride
YM-09151-2; Emilace; Emonapride
|
Dopamine Receptor
5-HT Receptor
|
Neurological Disease
|
|
Nemonapride is a highly potent dopamine D2 receptor antagonist with a Ki of 0.06 nM. Nemonapride also activates 5-HT1A receptor with an IC50 of 34 nM. Nemonapride is an antipsychotic that readily passes through the blood brain barrier and exhibits potent neuroleptic effects in animals.
|
-
- HY-109012A
-
-
- HY-113854
-
-
- HY-P1136B
-
-
- HY-100642S
-
|
3-O-Methyltolcapone-d7
Ro 40-7591 d7
|
COMT
|
Neurological Disease
|
|
3-O-Methyltolcapone-d7 is a deuterium labeled 3-O-Methyltolcapone. 3-O-Methyltolcapone is a metabolite of Tolcapone. Tolcapone is an orally active, reversible, selective and potent COMT inhibitor. Tolcapone crosses the blood-brain barrier, and can be used for treatment of Parkinson's disease[1][2].
|
-
- HY-147953
-
|
MAO-B-IN-13
|
Monoamine Oxidase
|
Neurological Disease
|
|
MAO-B-IN-13 (compound 12a) is a highly potent, reversible and blood-brain barrier (BBB) penetrant MAO-B inhibitor with an IC50 value of 10 nM. MAO-B-IN-13 has neuroprotective and antioxidant activity. MAO-B-IN-13 can be used for researching Parkinson’s disease.
|
-
- HY-151808
-
|
JS25
|
Btk
|
Cancer
|
|
JS25 is a selective and covalent inhibitor of BTK that inactivates BTK with an IC50 value of 5.8 nM by chelating Tyr551. JS25 inhibits cancer cells proliferation, pronounces cell death, and promotes murine xenograft model of Burkitt’s lymphoma. JS25 effectively crosses the blood-brain barrier.
|
-
- HY-126944
-
|
2-Aminobenzanilide
2-Amino-N-phenylbenzamide
|
Biochemical Assay Reagents
|
Cancer
|
|
2-Aminobenzamide is a neutral and stable compound used as fluorescent tag, numerously in Glycan analysis. 2-aminobenzamide acts as the starting material for several important reactions like Bargellini reaction as an competent ambident nucleophile. Specifically 2-aminobenzamide and its derivatives are used in the blood coagulation cascade.
|
-
- HY-128865
-
|
BPR1M97
|
Opioid Receptor
|
Neurological Disease
|
|
BPR1M97 is a dual-acting mu opioid receptor (MOP) and nociceptin-orphanin FQ peptide (NOP) receptor agonist with Ki values of 1.8 and 4.2 nM, respectively. BPR1M97 shows high potency and blood-brain barrier penetration, and produces potent antinociceptive effects.
|
-
- HY-13458S1
-
|
Droxidopa-13C2,15N hydrochloride
L-DOPS-13C2,15N hydrochloride; DOPS-13C2,15N hydrochloride; SM5688-13C2,15N hydrochloride
|
Isotope-Labeled Compounds
Adrenergic Receptor
|
Neurological Disease
|
|
Droxidopa- 13C2, 15N (hydrochloride) is deuterium labeled Droxidopa. Droxidopa(L-DOPS), the mixture of Droxidopa (w/w80%) and Pharmaceutical starch (w/w20%), acts as a proagent to the neurotransmitters norepinephrine (noradrenaline) and epinephrine (adrenaline); Droxidopa(L-DOPS) is capable of crossing the protective blood–brain barrier[1][2].
|
-
- HY-114320
-
|
BuChE-IN-TM-10
TM-10
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
BuChE-IN-TM-10 (TM-10) is a potent butyrylcholinesterase (BuChE) inhibitor, with an IC50 of 8.9 nM. BuChE inhibitor 1 inhibits and disaggregates self-induced Aβ aggregation, exhibiting potent antioxidant activity and good blood-brain barrier (BBB) penetration. Has potential to treat Alzheimer’s disease.
|
-
- HY-P1531
-
-
- HY-17401
-
|
Ranolazine dihydrochloride
CVT 303 dihydrochloride; RS 43285
|
Calcium Channel
Sodium Channel
Autophagy
|
Cardiovascular Disease
Cancer
|
|
Ranolazine dihydrochloride (CVT 303 dihydrochloride) is an anti-angina agent that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP). Ranolazine dihydrochloride is also a partial fatty acid oxidation inhibitor.
|
-
- HY-101402
-
|
Cyclo(his-pro)
Cyclo(histidyl-proline); Histidylproline diketopiperazine
|
NF-κB
Endogenous Metabolite
|
Inflammation/Immunology
Neurological Disease
|
|
Cyclo(his-pro) (Cyclo(histidyl-proline)) is an orally active cyclic dipeptide structurally related to tyreotropin-releasing hormone. Cyclo(his-pro) could inhibit NF-κB nuclear accumulation. Cyclo(his-pro) can cross the brain-blood-barrier and affect diverse inflammatory and stress responses.
|
-
- HY-131455A
-
-
- HY-N0304S
-
|
L-DOPA-d6
Levodopa-d6; 3,4-Dihydroxyphenylalanine-d6
|
Dopamine Receptor
Endogenous Metabolite
|
Neurological Disease
|
|
L-DOPA-d6 is the deuterium labeled L-DOPA. L-DOPA (Levodopa) is an orally active metabolic precursor of neurotransmitters dopamine. L-DOPA can cross the blood-brain barrier and is converted into dopamine in the brain. L-DOPA has anti-allodynic effects and the potential for Parkinson's disease[1][2][3].
|
-
- HY-P1422
-
|
Spadin
|
Potassium Channel
5-HT Receptor
|
Neurological Disease
|
|
Spadin, a natural peptide derived from a propeptide released in blood, is a potent TREK-1 channel blocker with IC50 value of 10 nM. Spadin enhances dorsal raphe nucleus 5-HT neurotransmission in mice and induces hippocampal CREB activation and neurogenesis. Spadin can be used for antidepressant research.
|
-
- HY-76772
-
|
Cevimeline hydrochloride hemihydrate
SNI-2011; AF102B hydrochloride hemihydrate
|
mAChR
|
Neurological Disease
Cancer
|
|
Cevimeline hydrochloride hemihydrate (SNI-2011) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline hydrochloride hemihydrate stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia. Cevimeline hydrochloride hemihydrate can cross the blood-brain barrier (BBB).
|
-
- HY-B0589S1
-
-
- HY-15010
-
|
L-371,257
|
Oxytocin Receptor
Vasopressin Receptor
|
Endocrinology
|
|
L-371,257 is an orally bioavailable, non-blood-brain barrier penetrant, selective and competitive antagonist of oxytocin receptor (pA2=8.4) with high affinity at both the oxytocin receptor (Ki=19 nM) and vasopressin V1a receptor (Ki=3.7 nM).
|
-
- HY-W014049
-
|
N'-Nitro-D-arginine
|
NO Synthase
|
Others
|
|
N'-Nitro-D-arginine, a nitric oxide synthesis inhibitor, also is a vasodilator that relaxes the smooth muscles and increases blood flow to the penis, improving erections. N'-Nitro-D-arginine also inhibits neutrophil migration by blocking receptors for tumour necrosis factor alpha (TNFα) and interleukin 8 (IL8).
|
-
- HY-B2130S1
-
|
Uric acid-15N2
|
Endogenous Metabolite
Reactive Oxygen Species
|
Inflammation/Immunology
|
|
Uric acid- 15N2 is the 15N labeled Uric acid[1]. Uric acid, scavenger of oxygen radical, is a very important antioxidant that help maintains the stability of blood pressure and antioxidant stress. Uric acid can remove reactive oxygen species (ROS) such as singlet oxygen and peroxynitrite, inhibiting lipid peroxidation[2][3].
|
-
- HY-N2320
-
|
Physostigmine hemisulfate
Eserine hemisulfate
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Physostigmine hemisulfate (Eserine hemisulfate) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine hemisulfate can crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine hemisulfate can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine hemisulfate is also an antidote for anticholinergic poisoning.
|
-
- HY-134494
-
|
MS48107
|
GPR68
|
Neurological Disease
|
|
MS48107 is a potent and selective positive allosteric modulator of G protein-coupled receptor 68 (GPR68). MS48107 is selective for GPR68 over the closely related proton GPCRs, neurotransmitter transporters, and hERG ion channels. MS48107 can readily cross the blood-brain barrier (BBB) in mice.
|
-
- HY-B0227S2
-
-
- HY-120717
-
|
VU6001966
|
mGluR
|
Others
|
|
VU6001966 (compound 15m) is a potent and cross the blood-brain barrier mGlu2 (metabotropic glutamate receptor 2) negative allosteric modulator with IC50s of 78 nM and >30 µM for mGlu2 and mGlu3, respectively. VU6001966 can serve as an mGlu2 PET tracer.
|
-
- HY-70020B
-
|
Cevimeline hydrochloride
AF102B hydrochloride
|
mAChR
|
Neurological Disease
|
|
Cevimeline hydrochloride (AF102B hydrochloride) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline hydrochloride stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia. Cevimeline hydrochloride can cross the blood-brain barrier (BBB).
|
-
- HY-10835
-
|
DG-041
|
Prostaglandin Receptor
|
Cardiovascular Disease
|
|
DG-041 is a potent, high affinity and selective EP3 receptor antagonist with IC50s of 4.6 nM and 8.1 nM in the binding and FLIPR assay, respectively. DG-041 inhibits PGE2 facilitation of platelet aggregation. DG-041 crosses the blood-brain barrier.
|
-
- HY-17423A
-
|
Abacavir sulfate
Abacavir Hemisulfate; ABC sulfate
|
Reverse Transcriptase
HIV
Telomerase
Apoptosis
|
Infection
|
|
Abacavir sulfate (Abacavir Hemisulfate) is a competitive, orally active nucleoside reverse transcriptase inhibitor. Abacavir sulfate can inhibits the replication of HIV. Abacavir sulfate shows anticancer activity in prostate cancer cell lines. Abacavir sulfate can trespass the blood-brain-barrier and suppresses telomerase activity.
|
-
- HY-N6608S
-
|
Physostigmine-d3
Eserine-d3
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Physostigmine-d3 is the deuterium labeled Physostigmine. Physostigmine (Eserine) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine can crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine is also an antidote for anticholinergic poisoning[1][2][3][4].
|
-
- HY-12305
-
|
Q-VD-OPh
QVD-OPH; Quinoline-Val-Asp-Difluorophenoxymethylketone
|
Caspase
HIV
|
Cancer
Infection
|
|
Q-VD-OPh is an irreversible pan-caspase inhibitor with potent antiapoptotic properties; inhibits caspase 7 with an IC50 of 48 nM and 25-400 nM for other caspases including caspase 1, 3, 8, 9, 10, and 12. Q-VD-OPh can inhibits HIV infection. Q-VD-OPh is able to cross the blood-brain barrier.
|
-
- HY-16531A
-
|
YF-2 hydrochloride
|
Histone Acetyltransferase
|
Cancer
Neurological Disease
|
|
YF-2 hydrochloride is a highly selective, blood-brain-barrier permeable histone acetyltransferase activator, acetylates H3 in the hippocampus, with EC50s of 2.75 μM, 29.04 μM and 49.31 μM for CBP, PCAF, and GCN5, respectively, shows no effect on HDAC. Anti-cancer and anti-Alzheimer's disease.
|
-
- HY-B1334
-
|
Perhexiline
|
Mitochondrial Metabolism
Apoptosis
|
Cancer
Cardiovascular Disease
|
|
Perhexiline is an orally active CPT1 and CPT2 inhibitor that reduces fatty acid metabolism. Perhexiline induces mitochondrial dysfunction and apoptosis in hepatic cells. Perhexiline can cross the blood brain barrier (BBB) and shows anti-tumor activity. Perhexiline can be used in the research of cancers, and cardiovascular disease like angina.
|
-
- HY-B1320
-
|
Meclofenamic acid sodium
Meclofenamate sodium
|
Gap Junction Protein
Endogenous Metabolite
|
Inflammation/Immunology
|
|
Meclofenamic acid (Meclofenamate) sodium is a nonsteroidal anti-inflammatory agent (NSAID) approved for use in arthritis (osteo and rheumatoid), analgesia (mild to moderate pain), dysmenorrhea, and heavy menstrual blood loss (menorrhagia). Meclofenamic acid sodium is a non-selective gap-junction blocker and a highly selective inhibitor of fat mass and obesity-associated (FTO) enzyme inhibitor.
|
-
- HY-B0146
-
|
Verteporfin
CL 318952
|
YAP
Apoptosis
Autophagy
|
Cancer
|
|
Verteporfin (CL 318952) is a photosensitizer for photodynamic therapy to eliminate the abnormal blood vessels in the eye associated with conditions such as age-related macular degeneration. Verteporfin is a YAP inhibitor which disrupts YAP-TEAD interactions. Verteporfin induces cell apoptosis. Verteporfinis an autophagy inhibitor that blocks autophagy at an early stage by inhibiting autophagosome formation.
|
-
- HY-132310
-
|
MAGL-IN-4
|
MAGL
|
Neurological Disease
|
|
MAGL-IN-4 is an orally active, selective and reversible monoacylglycerol lipase (MAGL) inhibitor with an IC50 of 6.2 nM. MAGL-IN-4 can penetrate the blood-brain barrier (BBB). MAGL-IN-4 enhances endocannabinoid signaling mostly by the increase in the level of 2-AG via selective MAGL inhibition in the brain.
|
-
- HY-144126
-
|
S1P1 agonist 5
|
LPL Receptor
|
Inflammation/Immunology
|
|
S1P1 agonist 5 is a selective and orally active S1P1 agonist. S1P1 agonist 5 inhibits the lymphocyte egress from the lymphoid tissue to the peripheral blood. S1P1 agonist 5 has the potential for the research of multiple sclerosis (MS).
|
-
- HY-B0589S
-
-
- HY-N9539
-
|
Phanginin A
|
Salt-inducible Kinase (SIK)
|
Metabolic Disease
|
|
Phanginin A is a potent and orally active SIK1 (salt-induced kinase 1) activator. Phanginin A inhibited gluconeogenesis. Phanginin A increases the expression of p-SIK1 and decreases the expression of p-CREB. Phanginin A reduces blood glucose levels and improves glucose tolerance and dyslipidemia. Phanginin A has the potential for the research of type 2 diabetes.
|
-
- HY-146762
-
-
- HY-B1334A
-
|
Perhexiline maleate
|
Mitochondrial Metabolism
Apoptosis
|
Cancer
Cardiovascular Disease
|
|
Perhexiline maleate is an orally active CPT1 and CPT2 inhibitor that reduces fatty acid metabolism. Perhexiline maleate induces mitochondrial dysfunction and apoptosis in hepatic cells. Perhexiline maleate can cross the blood brain barrier (BBB) and shows anti-tumor activity. Perhexiline maleate can be used in the research of cancers, and cardiovascular disease like angina.
|
-
- HY-10545
-
|
Taribavirin
|
HBV
HCV
|
Infection
|
|
Taribavirin is an orally active inosine monophosphate dehydrogenase inhibitor, has activity against a wide range of viruses, especially the hepatitis C virus and influenza virus. Taribavirin, is a ribavirin proagent, is designed to concentrate within the liver to target HCV-infected hepatocytes while minimizing distribution within red blood cells (RBCs) and the development of hemolytic anemia.
|
-
- HY-151545
-
|
WNK1-IN-1
|
Ser/Thr Protease
|
Cancer
Cardiovascular Disease
|
|
WNK1-IN-1 is a selective inhibitor of WNK1 with an IC50 value of 1.6 μM. WNK1-IN-1 inhibits OSR1 phosphorylation with an IC50 value of 4.3 μM. WNK1-IN-1 can be used for the research of blood pressure regulation and cancer.
|
-
- HY-Y0271
-
|
Urea
Carbamide; Carbonyldiamide; Carbonyl diamide
|
Endogenous Metabolite
|
Cardiovascular Disease
Cancer
|
|
Urea is a powerful protein denaturant via both direct and indirect mechanisms. A potent emollient and keratolytic agent. Used as a diuretic agent. Blood urea nitrogen (BUN) has been utilized to evaluate renal function. Widely used in fertilizers as a source of nitrogen and is an important raw material for the chemical industry.
|
-
- HY-112226
-
|
VRT-043198
|
Caspase
Drug Metabolite
|
Inflammation/Immunology
|
|
VRT-043198, the agent metabolite of VX-765 (Belnacasan), is a potent, selective and blood-brain barrier permeable inhibitor of interleukin-converting enzyme/caspase-1 subfamily caspases. VRT-043198 exhibits Ki values of 0.8 nM and 0.6 nM for ICE/caspase-1 and caspase-4, respectively.
|
-
- HY-136731
-
|
APE1-IN-1
|
DNA/RNA Synthesis
|
Cancer
|
|
APE1-IN-1 is a potent and blood-brain barrier (BBB) penetrant apurinic/apyrimidinic (AP) endonuclease 1 (APE1) inhibitor with an IC50 value of 2 μM. APE1-IN-1 can potentiate the cytotoxicity of the alkylating agents Methylmethane sulfonate and Temozolomide (HY-17364) to cancer cells.
|
-
- HY-N0304S2
-
|
L-DOPA-13C
|
Dopamine Receptor
Endogenous Metabolite
|
|
|
L-DOPA- 13C is the 13C labeled L-DOPA[1]. L-DOPA (Levodopa) is an orally active metabolic precursor of neurotransmitters dopamine. L-DOPA can cross the blood-brain barrier and is converted into dopamine in the brain. L-DOPA has anti-allodynic effects and the potential for Parkinson's disease[2][3][4].
|
-
- HY-B0317AS
-
|
Amlodipine-d4 maleate
|
Calcium Channel
|
Cancer
Cardiovascular Disease
|
|
Amlodipine-d4 (maleate) is the deuterium labeled Amlodipine maleate. Amlodipine maleate is a dihydropyridine calcium channel blocker, acts as an orally active antianginal agent. Amlodipine maleate blocks the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine maleate can be used for the research of high blood pressure and cancer[1][2][3].
|
-
- HY-16531
-
|
YF-2
|
Histone Acetyltransferase
|
Cancer
Neurological Disease
|
|
YF-2 is a highly selective, blood-brain-barrier permeable histone acetyltransferase activator, acetylates H3 in the hippocampus, with EC50s of 2.75 μM, 29.04 μM and 49.31 μM for CBP, PCAF, and GCN5, respectively, shows no effect on HDAC. Anti-cancer and anti-Alzheimer's disease.
|
-
- HY-100501
-
|
M2698
MSC2363318A
|
Ribosomal S6 Kinase (RSK)
Akt
|
Cancer
|
|
M2698 (MSC2363318A) is an orally active, ATP competitive, selective p70S6K and Akt dual-inhibitor with IC50s of 1 nM for p70S6K, Akt1 and Akt3. M2698 can cross the blood-brain barrier and has anti-cancer activity.
|
-
- HY-19838
-
|
JNJ-63533054
|
GPR139
|
Neurological Disease
|
|
JNJ-63533054 is a potent, selective and orally active GPR139 agonist with an EC50 of 16 nM for human GPR139 (hGPR139). JNJ-63533054 shows selective for GPR139 over other GPCRs, ion channels, and transporters. JNJ-63533054 can cross the blood-brain barrier (BBB).
|
-
- HY-116673
-
|
TTK21
|
Histone Acetyltransferase
|
Neurological Disease
|
|
TTK21 is an activator of the histone acetyltransferases CBP/p300. TTK21 passes the blood–brain barrier, induces no toxicity, and reaches different parts of the brain when conjugated to glucose-based carbon nanosphere (CSP). TTK21 has beneficial implications for the brain functions of adult neurogenesis and long-term memory.
|
-
- HY-A0064S
-
|
Verapamil-d3 hydrochloride
(±)-Verapamil-d3 (hydrochloride); CP-16533-1-d3 (hydrochloride)
|
Calcium Channel
P-glycoprotein
Cytochrome P450
|
Cardiovascular Disease
|
|
Verapamil-d3 (hydrochloride) is the deuterium labeled Verapamil hydrochloride. Verapamil hydrochloride ((±)-Verapamil hydrochloride) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil hydrochloride also inhibits CYP3A4. Verapamil hydrochloride has the potential for high blood pressure, heart arrhythmias and angina research[1][2][3].
|
-
- HY-135374
-
-
- HY-10545A
-
|
Taribavirin hydrochloride
|
HBV
HCV
|
Infection
|
|
Taribavirin hydrochloride is an orally active inosine monophosphate dehydrogenase inhibitor, has activity against a wide range of viruses, especially the hepatitis C virus and influenza virus. Taribavirin hydrochloride is a Ribavirin proagent, is designed to concentrate within the liver to target HCV-infected hepatocytes while minimizing distribution within red blood cells (RBCs) and the development of hemolytic anemia.
|
-
- HY-N2168
-
|
Pinoresinol 4-O-β-D-glucopyranoside
(+)-Pinoresinol 4-O-β-D-glucopyranoside
|
Others
|
Cardiovascular Disease
|
|
Pinoresinol 4-O-β-D-glucopyranoside ((+)-Pinoresinol 4-O-β-D-glucopyranoside) is the major active furofuran type lignans in Fructus Forsythiae. Pinoresinol 4-O-β-D-glucopyranoside shows antioxidant, blood pressure reducing, and cyclic adenosine monophosphate (cAMP) phosphodiesterase inhibitory effects.
|
-
- HY-P1178
-
|
Cyclotraxin B
|
Trk Receptor
|
Neurological Disease
|
|
Cyclotraxin B, a cyclic peptide, is a highly potent and selective TrkB inhibitor without altering the binding of BDNF. Cyclotraxin B non-competitively inhibits BDNF-induced TrkB activity with an IC50 of 0.30 nM. Cyclotraxin B can crosse the blood-brain-barrier and has analgesic and anxiolytic-like behavioral effects.
|
-
- HY-15112
-
|
JTP-4819
|
Prolyl Endopeptidase (PREP)
|
|
|
JTP-4819 is a potent and specific inhibitor of prolyl endopeptidase (PREP) with IC50s of 0.83 nM (in rat brain supernatant) and 5.43 nM (in Flavobacterium meningosepticum). JTP-4819 has blood-brain penetration, also improves the retention time of amnesia rats induced by Scopolamine (HY-N2096).
|
-
- HY-13289A
-
|
Nepicastat hydrochloride
SYN-117 hydrochloride; RS-25560-197 hydrochloride
|
Dopamine β-hydroxylase
|
Cardiovascular Disease
|
|
Nepicastat hydrochloride (SYN-117 hydrochloride) is a selective, potent, and orally active inhibitor of dopamine-beta-hydroxylase. Nepicastat hydrochloride produces concentration-dependent inhibition of bovine (IC50=8.5 nM) and human (IC50=9 nM) dopamine-beta-hydroxylase. Nepicastat hydrochloride can cross the blood-brain barrier (BBB).
|
-
- HY-100642S1
-
|
3-O-Methyltolcapone-d4
Ro 40-7591-d4
|
COMT
|
Neurological Disease
|
|
3-O-Methyltolcapone-d4 is the deuterium labeled 3-O-Methyltolcapone. 3-O-Methyltolcapone (Ro 40-7591) is a metabolite of Tolcapone. Tolcapone is an orally active, reversible, selective and potent COMT inhibitor. Tolcapone crosses the blood-brain barrier, and can be used for treatment of Parkinson's disease[1][2].
|
-
- HY-P1422A
-
|
Spadin TFA
|
Potassium Channel
5-HT Receptor
|
Neurological Disease
|
|
Spadin TFA, a natural peptide derived from a propeptide released in blood, is a potent TREK-1 channel blocker with an IC50 value of 10 nM. Spadin TFA enhances dorsal raphe nucleus 5-HT neurotransmission in mice and induces hippocampal CREB activation and neurogenesis. Spadin TFA can be used for antidepressant research.
|
-
- HY-W009276
-
|
γ-Linolenic Acid methyl ester
Methyl GLA
|
Apoptosis
|
Cancer
|
|
γ-Linolenic Acid methyl ester (Methyl GLA) is an esterified version of γ-Linolenic Acid (GLA), which is an ω-6 fatty acid, serves as melanoma cell proliferation inhibitors. γ-Linolenic Acid methyl ester inhibits ADP-induced blood platelet aggregation and induces apoptosis.
|
-
- HY-134189
-
|
EST73502
|
Opioid Receptor
Sigma Receptor
|
Neurological Disease
|
|
EST73502 is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioid receptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with Kis of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 has antinociceptive activity.
|
-
- HY-122347A
-
|
Orvepitant maleate
GW823296 maleate
|
Neurokinin Receptor
|
Neurological Disease
|
|
Orvepitant maleate (GW823296 maleate) is potent, selective, orally active and well-tolerated neurokinin-1 receptor (NK-1) antagonist with a pKi of 10.2 for human neurokinin-1 receptor. Orvepitant maleate can across the blood-brain barrier. Orvepitant maleate has the potential for depressive disorder and chronic refractory cough (CRC) treatment.
|
-
- HY-144309
-
-
- HY-131350
-
|
LXE408
|
Proteasome
Parasite
|
Infection
|
|
LXE408 is an orally active, non-competitive and kinetoplastid-selective proteasome inhibitor. LXE408 has an IC50 of 0.04 μM for L. donovani proteasome and an EC50 of 0.04 μM for L. donovani. LXE408 has a low propensity to cross the blood brain barrier. LXE408 has the potential for visceral leishmaniasis (VL) research.
|
-
- HY-70020
-
|
Cevimeline
AF102B
|
mAChR
|
Neurological Disease
|
|
Cevimeline (AF-102B) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia. Cevimeline can cross the blood-brain barrier (BBB).
|
-
- HY-15121
-
|
L-Theanine
L-Glutamic Acid γ-ethyl amide; Nγ-Ethyl-L-glutamine
|
Apoptosis
Endogenous Metabolite
Reactive Oxygen Species
|
Cancer
Neurological Disease
|
|
L-Theanine (L-Glutamic Acid γ-ethyl amide) is a non-protein amino acid contained in green tea leaves, which blocks the binding of L-glutamic acid to glutamate receptors in the brain, and with neuroprotective, anticancer and anti-oxidative activities. L-Theanine can pass through the blood–brain barrier and is orally active.
|
-
- HY-118342
-
|
PQCA
|
mAChR
|
Neurological Disease
|
|
PQCA is a highly selective and potent muscarinic M1 receptor positive allosteric modulator. PQCA has an EC50 value of 49 nM and 135 nM on rhesus and human M1 receptor, respectively. PQCA is inactive for other muscarinic receptors. PQCA has potential to reduce the cognitive deficits associated with Alzheimer's disease.
|
-
- HY-A0039
-
|
Eletriptan
UK-116044
|
5-HT Receptor
|
Inflammation/Immunology
Neurological Disease
|
|
Eletriptan (UK-116044) is a highly selective and orally active serotonin 5-HT1B and 5-HT1D receptor agonist, with pKi values of 8.0 and 8.9, respectively. Eletriptan has inhibitory effects on markers of neurogenic inflammation in rats. Eletriptan can be used for researching migraine.
|
-
- HY-150598
-
|
CHMFL-PI4K-127
|
PI4K
PI3K
|
Infection
|
|
CHMFL-PI4K-127 (compound 15g) is an orally active, potent and high selective PfPI4K (Plasmodium falciparum PI4K kinase) inhibitor, with an IC50 of 0.9 nM. CHMFL-PI4K-127 exhibits potent activity against 3D7 Plasmodium falciparum, with an EC50 of 25.1 nM. CHMFL-PI4K-127 shows antimalaria efficacy.
|
-
- HY-101813
-
|
Laflunimus
HR325
|
Dihydroorotate Dehydrogenase
DNA/RNA Synthesis
Prostaglandin Receptor
|
Inflammation/Immunology
|
|
Laflunimus (HR325) is an immunosuppressive agent and an analogue of the Leflunomide-active metabolite A77 1726. Laflunimus is an orally active inhibitor of dihydroorotate dehydrogenase (DHODH). Laflunimus suppresses immunoglobulin (Ig) secretion, with IC50 values of 2.5 and 2 µM for IgM and IgG, respectively. Laflunimus also is a prostaglandin endoperoxide H synthase (PGHS) -1 and -2 inhibitor.
|
-
- HY-B1486
-
-
- HY-136589
-
-
- HY-N7748A
-
-
- HY-143793
-
|
RBP4 inhibitor 1
|
Others
|
Metabolic Disease
|
|
RBP4 inhibitor 1 (compound 43b) is a potent and orally active retinol-binding protein 4 (RBP4) inhibitor with IC50s of 28 nM and 110 nM for human and mouse RBP4. RBP4 inhibitor 1 has a potent and long-lasting blood RBP4-level-reducing effect in mice.
|
-
- HY-W016420
-
|
Fosfomycin sodium
MK-0955 sodium
|
Bacterial
Antibiotic
|
Infection
Cancer
|
|
Fosfomycin (MK-0955) sodium is a blood-brain barrier penetrating, broad-spectrum antibiotic by irreversibly inhibiting an early stage in cell wall synthesis. Fosfomycin sodium shows both in vivo and in vitro activity against a wide range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria.
|
-
- HY-B2130S
-
|
Uric acid-13C,15N3
|
Reactive Oxygen Species
Endogenous Metabolite
|
Inflammation/Immunology
|
|
Uric acid- 13C, 15N3 is the 13C-labeled and 15N-labeled Uric acid. Uric acid, scavenger of oxygen radical, is a very important antioxidant that help maintains the stability of blood pressure and antioxidant stress. Uric acid can remove reactive oxygen species (ROS) such as singlet oxygen and peroxynitrite, inhibiting lipid peroxidation[1][2].
|
-
- HY-119873
-
|
Celiprolol
REV 5320
|
NO Synthase
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Celiprolol (REV 5320) is a potent, cardioselective and orally active β1-andrenoceptor r antagonist with partial β2 agonist activity, with Ki values of 0.14-8.3 μM. Celiprolol has antihypertensive and antianginal activity, and can be used for the research of cardiovascular disease such as high blood pressure.
|
-
- HY-119757
-
|
Tyrphostin AG1433
SU1433; AG1433
|
PDGFR
VEGFR
|
Cancer
|
|
Tyrphostin AG1433 (SU1433) is a tyrosine kinases inhibitor. AG1433 is also a selective PDGFRβ and VEGFR-2 (Flk-1/KDR) inhibitor with IC50s of 5.0 μM and 9.3 μM, respectively. Tyrphostin AG1433 prevents blood vessel formation.
|
-
- HY-17364
-
|
Temozolomide
NSC 362856; CCRG 81045; TMZ
|
DNA Alkylator/Crosslinker
Autophagy
Apoptosis
|
Cancer
|
|
Temozolomide (NSC 362856) is an oral active DNA alkylating agent that crosses the blood-brain barrier. Temozolomide is also a proautophagic and proapoptotic agent. Temozolomide is effective against tumor cells that are characterized by low levels of O6-alkylguanine DNA alkyltransferase (OGAT) and a functional mismatch repair system. Temozolomide has antitumor and antiangiogenic effects.
|
-
- HY-13289
-
|
Nepicastat
SYN117; RS-25560-197
|
Dopamine β-hydroxylase
|
Cardiovascular Disease
|
|
Nepicastat (SYN117) is a selective, potent, and orally active inhibitor of dopamine-beta-hydroxylase. Nepicastat (SYN117) produces concentration-dependent inhibition of bovine (IC50=8.5 nM) and human (IC50=9 nM) dopamine-beta-hydroxylase. Nepicastat (SYN117) can cross the blood-brain barrier (BBB).
|
-
- HY-15771
-
|
Tirabrutinib
ONO-4059; GS-4059
|
Btk
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Tirabrutinib (ONO-4059) is an orally active Bruton’s Tyrosine Kinase (BTK) inhibitor (can cross the blood-brain barrier (BBB)), with an IC50 of 6.8 nM. Tirabrutinib irreversibly and covalently binds to BTK and inhibits aberrant B cell receptor signaling. Tirabrutinib can be used in studies of autoimmune diseases and hematological malignancies.
|
-
- HY-14397S
-
|
Indomethacin-d4
Indometacin-d4
|
COX
Autophagy
|
Cancer
Inflammation/Immunology
|
|
Indomethacin-d4 is a deuterium labeled Indomethacin. Indomethacin is a potent, blood-brain permeable and nonselective inhibitor of COX1 and COX2, with IC50s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells[1]. Indomethacin disrupts autophagic flux by disturbing the normal functioning of lysosomes[2].
|
-
- HY-148643
-
|
STING modulator-5
|
STING
|
Inflammation/Immunology
|
|
STING modulator-5 (compound 38) is a STING modulator with a pIC50 value of 9.5. STING modulator-5 antagonizes peripheral blood mononuclear cells (PBMC) with a pIC50 value of 8.1. STING modulator-5 is a antagonist of THP-1 cells, it can be used for immunological disease research.
|
-
- HY-100740C
-
|
(1α,1'S,4β)-Lanabecestat
(1α,1'S,4β)-AZD3293; (1α,1'S,4β)-LY3314814
|
Beta-secretase
|
Neurological Disease
|
|
(1α,1'S,4β)-Lanabecestat ((1α,1'S,4β)-AZD3293) a less active enantiomer of Lanabecestat. Lanabecestat is a potent, orally active and blood-brain barrier penetrating BACE1 inhibitor with a Ki of 0.4 nM.
|
-
- HY-10232
-
|
THIP
Gaboxadol
|
GABA Receptor
|
Neurological Disease
|
|
THIP (Gaboxadol) is a selective extrasynaptic GABAA receptors (eGABARs) agonist (with blood-brain barrier permeability), shows an EC50 value of 13 µM for δ-GABAAR. THIP induces strong tense GABAA-mediated currents in layer 2/3 neurons, but shows on effect on miniature IPSCs. THIP can be used in studies of sleep disorders.
|
-
- HY-111274
-
|
Indomethacin farnesil
Indometacin farnesil
|
COX
Autophagy
|
Inflammation/Immunology
|
|
Indomethacin farnesil is an orally active proagent of Indomethacin. Indomethacin (Indometacin) is a potent, blood-brain permeable and nonselective inhibitor of COX1 and COX2, with IC50s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells. Indomethacin disrupts autophagic flux by disturbing the normal functioning of lysosomes.
|
-
- HY-B1395S1
-
|
Mecamylamine hydrochloride-13C4,15N
|
nAChR
|
Neurological Disease
|
|
Mecamylamine (hydrochloride)- 13C4, 15N is the 13C-labeled and 15N-labeled Mecamylamine hydrochloride. Mecamylamine hydrochloride is an orally active, nonselective, noncompetitive nAChR antagonist that can treat various neuropsychiatric disorders. Mecamylamine hydrochloride is originally used as a ganglionic blocker in treating hypertension. Mecamylamine hydrochloride can easily crosses the blood-brain barrier[1][2].
|
-
- HY-101402A
-
|
Cyclo(his-pro) TFA
Cyclo(histidyl-proline) TFA; Histidylproline diketopiperazine TFA
|
NF-κB
Endogenous Metabolite
|
Inflammation/Immunology
Neurological Disease
|
|
Cyclo(his-pro) TFA (Cyclo(histidyl-proline) TFA) is an orally active cyclic dipeptide structurally related to tyreotropin-releasing hormone. Cyclo(his-pro) TFA could inhibit NF-κB nuclear accumulation. Cyclo(his-pro) TFA can cross the brain-blood-barrier and affect diverse inflammatory and stress responses.
|
-
- HY-P1136C
-
-
- HY-B1451
-
|
Imidapril hydrochloride
TA-6366
|
Angiotensin-converting Enzyme (ACE)
MMP
|
Metabolic Disease
Cardiovascular Disease
|
|
Imidapril hydrochloride (TA-6366) is an orally active angiotensin-converting enzyme (ACE) and MMP-9 inhibitor. Imidapril hydrochloride suppresses the conversion of angiotensin I to angiotensin II and thereby reduces total peripheral resistance and systemic blood pressure. Imidapril hydrochloride can be used for hypertension, type 1 diabetic, nephropathy and chronic heart failure research.
|
-
- HY-P1178A
-
|
Cyclotraxin B TFA
|
Trk Receptor
|
Neurological Disease
|
|
Cyclotraxin B TFA, a cyclic peptide, is a highly potent and selective TrkB inhibitor without altering the binding of BDNF. Cyclotraxin B TFA non-competitively inhibits BDNF-induced TrkB activity with an IC50 of 0.30 nM. Cyclotraxin B TFA can crosse the blood-brain-barrier and has analgesic and anxiolytic-like behavioral effects.
|
-
- HY-108492
-
|
TC-SP 14
|
LPL Receptor
|
Inflammation/Immunology
|
|
TC-SP 14 (compound 14) is an orally active and potent S1P1 agonist (EC50 = 0.042 μM) with minimal activity at S1P3 (EC50 = 3.47 μM). TC-SP 14 significantly reduces blood lymphocyte counts and attenuates a delayed type hypersensitivity (DTH) response to antigen challenge.
|
-
- HY-N0304S1
-
|
L-DOPA-d6-1
Levodopa-d6-1; 3,4-Dihydroxyphenylalanine-d6-1
|
Dopamine Receptor
Endogenous Metabolite
|
|
|
L-DOPA-d6-1 is the deuterium labeled L-DOPA[1]. L-DOPA (Levodopa) is an orally active metabolic precursor of neurotransmitters dopamine. L-DOPA can cross the blood-brain barrier and is converted into dopamine in the brain. L-DOPA has anti-allodynic effects and the potential for Parkinson's disease[2][3][4].
|
-
- HY-B1075A
-
|
Fosfomycin
MK-0955
|
Bacterial
Antibiotic
|
Infection
|
|
Fosfomycin (MK-0955) is a broad-spectrum antibiotic. Fosfomycin can cross blood-brain barrier penetrating, and irreversibly inhibits an early stage in cell wall synthesis. Fosfomycin shows anti-bacteria activity for a range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria.
|
-
- HY-A0067
-
|
Oxybenzone
Benzophenone 3
|
RAR/RXR
Autophagy
Apoptosis
|
Neurological Disease
|
|
Oxybenzone (Benzophenone 3) is a commonly used UV filter in sun tans and skin protectants. Oxybenzone act as endocrine disrupting chemicals (EDCs) and can pass through the placental and blood-brain barriers. Benzophenone-3 impairs autophagy, alters epigenetic status, and disrupts retinoid X receptor signaling in apoptotic neuronal cells.
|
-
- HY-134189A
-
-
- HY-B0280
-
|
Ranolazine
CVT 303; RS 43285-003
|
Sodium Channel
Calcium Channel
|
Cardiovascular Disease
Cancer
|
|
Ranolazine (CVT 303) is an anti-angina drug that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP). Ranolazine is also a partial fatty acid oxidation (FAO) inhibitor. Antianginal agent.
|
-
- HY-P99822
-
|
Recaticimab
SHR-1209
|
Ser/Thr Protease
|
Metabolic Disease
|
|
Recaticimab (SHR-1209) is a humanized monoclonal antibody that inhibits PCSK9. Receticimab mediates the degradation of PCSK9 by binding to PCSK9, increasing the level of low-density lipoprotein (LDL) receptors on the surface of hepatocytes, reducing the level of LDL in plasma, and achieving the goal of lowering blood lipids. Recaticimab has potential application in hypercholesterolemia.
|
-
- HY-12717AS
-
|
Phentolamine-d4 hydrochloride
|
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Phentolamine-d4 (hydrochloride) is the deuterium labeled Phentolamine hydrochloride. Phentolamine hydrochloride is a reversible, non-selective, and orally active blocker of α1 and α2 adrenergic receptor that expands blood vessels to reduce peripheral vascular resistance. Phentolamine hydrochloride can be used for the research of pheochromocytoma-related hypertension, heart failure and erectile dysfunction[1][2][3].
|
-
- HY-B1264
-
|
Celiprolol hydrochloride
|
NO Synthase
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Celiprolol (REV 5320) is a potent, cardioselective and orally active β1-andrenoceptor r antagonist with partial β2 agonist activity, with Ki values of 0.14-8.3 μM. Celiprolol has antihypertensive and antianginal activity, and can be used for the research of cardiovascular disease such as high blood pressure.
|
-
- HY-15771A
-
|
Tirabrutinib hydrochloride
ONO-4059 hydrochloride; GS-4059 hydrochloride
|
Btk
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Tirabrutinib (ONO-4059) hydrochloride is an orally active Bruton’s Tyrosine Kinase (BTK) inhibitor (can cross the blood-brain barrier (BBB)), with an IC50 of 6.8 nM. Tirabrutinib hydrochloride irreversibly and covalently binds to BTK and inhibits aberrant B cell receptor signaling. Tirabrutinib hydrochloride can be used in studies of autoimmune diseases and hematological malignancies.
|
-
- HY-13340
-
|
VU0152100
VU152100
|
mAChR
|
Neurological Disease
|
|
VU0152100 (VU152100) is a highly selective mAChR positive allosteric modulator (permeable to the blood-brain barrier). VU0152100 reverses Amphetamine-induced hypermotility in rats and increased levels of extracellular dopamine in nucleus accumbens and caudate-putamen. VU0152100 has good research potential in psychosis and cognitive impairment associated with mental disorders such as schizophrenia.
|
-
- HY-103461
-
|
FAAH-IN-6
|
FAAH
|
Neurological Disease
|
|
FAAH-IN-6 (compound 21d) is a potent, orally active and cross the blood-brain barrier fatty acid amide hydrolase (FAAH) inhibitor with IC50s of 0.72, 0.28 nM for hFAAH, rFAAH, respectively. FAAH-IN-6 shows dose-dependent analgesic efficacy in animal models of both neuropathic and inflammatory pain.
|
-
- HY-107531
-
|
A 1070722
|
GSK-3
|
Cancer
|
|
A 1070722 is a potent and selective glycogen synthase kinase 3 (GSK-3) inhibitor, with a Ki of 0.6 nM for both GSK-3α and GSK-3β. A 1070722 can penetrate the blood-brain barrier (BBB) and accumulates in brain regions, thus potential for PET radiotracer for the quantification of GSK-3 in brain.
|
-
- HY-138568
-
|
HPK1-IN-3
|
MAP4K
|
Inflammation/Immunology
|
|
HPK1-IN-3 is a potent and selective ATP-competitive hematopoietic progenitor kinase 1 (HPK1; MAP4K1) inhibitor with an IC50 of 0.25 nM. HPK1-IN-3 has IL-2 cellular potency with an EC50 of 108 nM in human peripheral blood mononuclear cells (PBMCs).
|
-
- HY-N3187
-
-
- HY-17638
-
|
Mizagliflozin
DSP-3235 free base; KGA-3235 free base; GSK-1614235 free base
|
SGLT
|
Metabolic Disease
|
|
Mizagliflozin (DSP-3235 free base) is a potent, orally active and selective SGLT1 inhibitor, with a Ki of 27 nM for human SGLT1. Mizagliflozin displays 303-fold selectivity over SGLT2. Mizagliflozin is used as an antidiabetic agent that can modify postprandial blood glucose excursion. Mizagliflozin also exhibits potential in the amelioration of chronic constipation.
|
-
- HY-14166
-
|
MK-886
L 663536
|
FLAP
Leukotriene Receptor
PPAR
Apoptosis
|
Cancer
|
|
MK-886 (L 663536) is a potent, cell-permeable and orally active FLAP (IC50 of 30 nM) and leukotriene biosynthesis (IC50s of 3 nM and 1.1 μM in intact leukocytes and human whole blood, respectively) inhibitor. MK-886 is also a non-competitive PPARα antagonist and can induce apoptosis.
|
-
- HY-144604
-
|
FPR2 agonist 2
|
Others
|
Infection
Neurological Disease
|
|
FPR2 agonist 2 is a potent and permeates the blood−brain barrier FPR2 agonist with an EC50 of 0.13 µM, 1.1 µM for FPR2 and FPR1, respectively. FPR2 agonist 2 inhibits the production of pro-inflammatory cytokines, counterbalances the changes in mitochondrial function, and inhibits caspase-3 activity.
|
-
- HY-128530
-
|
Tetrathiomolybdate
|
Others
|
Metabolic Disease
Inflammation/Immunology
Cardiovascular Disease
|
|
Tetrathiomolybdate, an orally active anti-copper agent, reduces copper levels in the body. Tetrathiomolybdate has a protective effect on collagen-induced arthritis in mice. Tetrathiomolybdate also reduces blood sugar, but has no effect on mice with hereditary diabetes (db/db). Tetrathiomolybdate inhibit angiogenesis, also shows antiangiogenic effects in malignant pleural mesothelioma.
|
-
- HY-124160
-
|
JNJ-56022486
|
iGluR
|
Neurological Disease
|
|
JNJ-56022486 is an orally active and potent negative AMPA receptor modulator (Ki=19 nM) selective for TARP-γ8. JNJ-56022486 is also a TARP-γ8 receptor antagonist, with blood brain barrier (BBB) permeability. JNJ-56022486 can be used for research of Epilepsy.
|
-
- HY-109012
-
|
Seltorexant
JNJ-42847922
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
Endocrinology
|
|
Seltorexant (JNJ-42847922) is an orally active, high-affinity, and selective orexin-2 receptor (OX2R) antagonist (pKi values of 8.0 and 8.1 for human and rat OX2R). Seltorexant (JNJ-42847922) crosses the blood-brain barrier and quickly occupies OX2R binding sites in the rat brain.
|
-
- HY-B1075
-
|
Fosfomycin calcium
MK-0955 calcium
|
Bacterial
Antibiotic
|
Infection
Cancer
|
|
Fosfomycin (MK-0955) calcium is a blood-brain barrier penetrating, broad-spectrum antibiotic by irreversibly inhibiting an early stage in cell wall synthesis. Fosfomycin calcium shows both in vivo and in vitro activity against a wide range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria.
|
-
- HY-152614
-
|
Antimalarial agent 19
|
Parasite
|
Infection
|
|
Antimalarial agent 19 (compound 6e) is an antimalarial active agent. Antimalarial agent 19 has antimalarial activity for the blood stage of P. falciparum K1 and P. berghei with EC50 values of 0.3 µM, 15.3 µM, respectively. Antimalarial agent 19 has good aqueous solubility, intestinal permeability and microsomal stability compared to gamhepathiopine.
|
-
- HY-106850
-
|
3′-Azido-2′,3′-dideoxyuridine
AzdU; AzddU; CS-87
|
HIV
|
Infection
|
|
3′-Azido-2′,3′-dideoxyuridine (AzdU) is a nucleoside analog of Zidovudine (HY-17413). 3′-Azido-2′,3′-dideoxyuridine is a potent inhibitor of human immunodeficiency virus (HIV) replication in human peripheral blood mononuclear cells (PBMC) with limited toxicity for human bone marrow cells (BMC).
|
-
- HY-15321S1
-
|
Etoricoxib-13C,d3
MK-0663-13C,d3; L-791456-13C,d3
|
COX
|
Inflammation/Immunology
Cancer
|
|
Etoricoxib- 13C,d3 is the 13C- and deuterium labeled Etoricoxib. Etoricoxib (MK-0663) is a non steroidal anti-inflammatory agent, acting as a selective and orally active COX-2 inhibitor, with IC50s of 1.1 μM and 116 μM for COX-2 and COX-1 in human whole blood.
|
-
- HY-B0609
-
|
Fosfomycin tromethamine
MK-0955 tromethamine
|
Bacterial
Antibiotic
|
Infection
Cancer
|
|
Fosfomycin (MK-0955) tromethamine is a blood-brain barrier penetrating, broad-spectrum antibiotic by irreversibly inhibiting an early stage in cell wall synthesis. Fosfomycin tromethamine shows both in vivo and in vitro activity against a wide range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria.
|
-
- HY-16056
-
|
Arbutamine
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Arbutamine is a short-acting, potent and nonselective β-adrenoceptor agonist. Arbutamine stimulates cardiac β1-, tracheal β2-, and adiopocyte β3- adrenergic receptors. Arbutamine provides cardiac stress increases heart rate, cardiac contractility, and systolic blood pressure. Arbutamine can be used for cardiac stress agent .
|
-
- HY-12554
-
|
Terlipressin
|
Vasopressin Receptor
|
Endocrinology
Inflammation/Immunology
Cardiovascular Disease
|
|
Terlipressin is a vasopressin analogue with potent vasoactive properties. Terlipressin is a highly selective vasopressin V1 receptor agonist that reduces the splanchnic blood flow and portal pressure and controls acute variceal bleeding. Terlipressin exerts anti-inflammatory and anti-oxidative effects. Terlipressin has the potential for hepatorenal syndrome and norepinephrine-resistant septic shock research.
|
-
- HY-16056A
-
|
Arbutamine hydrochloride
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Arbutamine hydrochloride is a short-acting, potent and nonselective β-adrenoceptor agonist. Arbutamine hydrochloride stimulates cardiac β1-, tracheal β2-, and adiopocyte β3- adrenergic receptors. Arbutamine hydrochloride provides cardiac stress increases heart rate, cardiac contractility, and systolic blood pressure. Arbutamine hydrochloride can be used for cardiac stress agent .
|
-
- HY-10202A
-
|
Tandutinib hydrochloride
MLN518 hydrochloride; CT53518 hydrochloride
|
FLT3
c-Kit
PDGFR
Apoptosis
|
Cancer
|
|
Tandutinib hydrochloride (MLN518 hydrochloride) is a potent and selective inhibitor of the FLT3 with an IC50 of 0.22 μM, and also inhibits c-Kit and PDGFR with IC50s of 0.17 μM and 0.20 μM, respectively. Tandutinib hydrochloride can be used for acute myelogenous leukemia (AML). Tandutinib hydrochloride has the ability to cross the blood-brain barrier.
|
-
- HY-148417
-
|
ZZL-7
|
Serotonin Transporter
|
Neurological Disease
|
|
ZZL-7 is a fast-onset antidepressant agent. ZZL-7 works by disrupting the interaction between the serotonin transporter (SERT) and neuronal nitric oxide synthase (nNOS) in the dorsal raphe nucleus (DRN). ZZL-7 can cross the blood-brain barrier readily. ZZL-7 can be used for the research of major depressive disorder (MDD).
|
-
- HY-14397S1
-
|
Indomethacin-d4 Methyl Ester
|
COX
Autophagy
|
Cancer
Inflammation/Immunology
|
|
Indomethacin-d4 Methyl Ester is the deuterium labeled Indomethacin. Indomethacin (Indometacin) is a potent, blood-brain permeable and nonselective inhibitor of COX1 and COX2, with IC50s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells[1]. Indomethacin disrupts autophagic flux by disturbing the normal functioning of lysosomes[2].
|
-
- HY-151985
-
|
TACC3 inhibitor 1
|
Apoptosis
|
Cancer
|
|
TACC3 inhibitor 1 is a potent and cross the blood-brain barrier TACC3 inhibitor. TACC3 inhibitor 1 induces Apoptosis and cell cycle arrest at G2/M phase. TACC3 inhibitor 1 induces the generation of intracellular ROS. TACC3 inhibitor 1 shows antiproliferative and anti-tumor activity.
|
-
- HY-100864
-
|
mPGES1-IN-3
|
PGE synthase
|
Inflammation/Immunology
|
|
mPGES1-IN-3 (Compound 17d) is a potent and selective microsomal prostaglandin E2 synthase-1 (mPGES-1) inhibitor, which exhibits excellent mPGES-1 enzyme (IC50: 8 nM), cell (A549 IC50: 16.24 nM) and human whole blood potency (IC50: 249.9 nM).
|
-
- HY-112540
-
|
Acetoacetic acid
|
Endogenous Metabolite
|
Neurological Disease
Metabolic Disease
|
|
Acetoacetic acid is an endogenous metabolite present in Cerebrospinal_Fluid and Blood that can be used for the research of Meningitis, Pregnancy, 3 Hydroxy 3 Methylglutaryl CoA Lyase Deficiency, Preeclampsia/Eclampsia, Diabetes Mellitus Type 2, Glucose Transporter Type 1 Deficiency Syndrome and Succinyl CoA:3 Oxoacid CoA Transferase Deficiency.
|
-
- HY-33009
-
|
AS057278
|
Others
|
Neurological Disease
|
|
AS057278 is a potent, selective, orally active and blood-brain barrier (BBB) penetrant non-peptidic D-amino acid oxidase (DAAO) inhibitor with an IC50 value of 0.91 μM and EC50 of 2.2-3.95 μM. AS057278 can normalize phencyclidine (PCP)-induced prepulse inhibition in mice. AS057278 can be used for researching schizophrenia.
|
-
- HY-B0364A
-
|
Dyclonine hydrochloride
Dyclocaine hydrochloride
|
Bacterial
Fungal
Aldehyde Dehydrogenase (ALDH)
|
Cancer
Infection
|
|
Dyclonine (Dyclocaine) hydrochloride is an orally effective ALDH covalent inhibitor (crosses blood-brain barrier), with an IC50 of 35 µM for ALDH2 and 76 µM for ALDH3A1. Dyclonine hydrochloride has sensitizing activities for targeted cancer cells and antibacterial. Dyclonine hydrochloride is also a local anesthetic that blocks the transmission of various nerve impulses or stimuli and inhibits the sensation of touch and pain.
|
-
- HY-B0317S
-
|
Amlodipine-1,1,2,2-d4 maleate
|
Calcium Channel
|
Cancer
Cardiovascular Disease
|
|
Amlodipine-1,1,2,2-d4 (maleate) is the deuterium labeled Amlodipine. Amlodipine, an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine can be used for the research of high blood pressure and cancer[1][2][3].
|
-
- HY-N0729S3
-
|
Linoleic acid-13C1
|
Endogenous Metabolite
|
Metabolic Disease
Cardiovascular Disease
|
|
Linoleic acid- 13C1 is the 13C labeled Linoleic acid. Linoleic acid is a common polyunsaturated (PUFA) found in plant-based oils, nuts and seeds. Linoleic acid is a part of membrane phospholipids, and functions as a structural component to maintain a certain level of membrane fluidity of the transdermal water barrier of the epidermis. Linoleic acid induces red blood cells and hemoglobin damage via oxidative mechanism [1][2].
|
-
- HY-A0064S2
-
|
Verapamil-d3-1 hydrochloride
(±)-Verapamil-d3-1 hydrochloride; CP-16533-1-d3-1 hydrochloride
|
P-glycoprotein
Calcium Channel
Cytochrome P450
|
|
|
Verapamil-d3-1 (hydrochloride) is the deuterium labeled Verapamil hydrochloride[1]. Verapamil hydrochloride ((±)-Verapamil hydrochloride) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil hydrochloride also inhibits CYP3A4. Verapamil hydrochloride has the potential for high blood pressure, heart arrhythmias and angina research[2][3][4].
|
-
- HY-B2099S
-
|
Buformin-d9 hydrochloride
1-Butylbiguanide-d9 (hydrochloride)
|
AMPK
|
Cancer
Metabolic Disease
|
|
Buformin-d9 (hydrochloride) is the deuterium labeled Buformin. Buformin (1-Butylbiguanide), a potent AMPK activator, acts as an orally active biguanide antidiabetic agent. Buformin decreases hepatic gluconeogenesis and lowers blood glucose production in vivo. Buformin also has anti-cancer activities and is applied in cancer study (such as, cervical cancer and breast cancer, et al)[1].
|
-
- HY-12554A
-
|
Terlipressin acetate
|
Vasopressin Receptor
|
Endocrinology
Inflammation/Immunology
Cardiovascular Disease
|
|
Terlipressin acetate is a vasopressin analogue with potent vasoactive properties. Terlipressin acetate is a highly selective vasopressin V1 receptor agonist that reduces the splanchnic blood flow and portal pressure and controls acute variceal bleeding. Terlipressin acetate exerts anti-inflammatory and anti-oxidative effects. Terlipressin acetate has the potential for hepatorenal syndrome and norepinephrine-resistant septic shock research.
|
-
- HY-10974
-
|
MK-0752
|
γ-secretase
|
Neurological Disease
Cancer
|
|
MK-0752 is a potent, orally active and specific γ-secretase inhibitor, showing dose-dependent reduction of Aβ40 with an IC50 of 5 nM in human SH-SY5Y cells. MK-0752 crosses the blood-brain barrier. MK-0752 reduces newly generated CNS Aβ in vivo.
|
-
- HY-130795
-
|
GSK-3β inhibitor 2
|
GSK-3
|
Neurological Disease
|
|
GSK-3β inhibitor 2 (Compound 3) is a potent, selective and orally active GSK-3β inhibitor with an IC50 of 1.1 nM. GSK-3β inhibitor 2 can cross the blood-brain barrier. GSK-3β inhibitor 2 has the potential for Alzheimer's disease.
|
-
- HY-B1451A
-
|
Imidapril
TA-6366 free base
|
Angiotensin-converting Enzyme (ACE)
MMP
|
Metabolic Disease
Cardiovascular Disease
|
|
Imidapril (TA-6366 free base) is an orally active angiotensin-converting enzyme (ACE) and MMP-9 inhibitor. Imidapril suppresses the conversion of angiotensin I to angiotensin II and thereby reduces total peripheral resistance and systemic blood pressure. Imidapril can be used for hypertension, type 1 diabetic, nephropathy and chronic heart failure research.
|
-
- HY-150791
-
|
FLDP-5
|
Reactive Oxygen Species
DNA/RNA Synthesis
|
Cancer
|
|
FLDP-5 is a blood-brain barrier (BBB) penetrant curcuminoid analogues. FLDP-5 can induce production of ROS (Reactive Oxygen Species), DNA damage and cell cycle S phase arrest. FLDP-5 exhibits highly potent tumour-suppressive effects with anti-proliferative and anti-migratory activities on LN-18 cells.
|
-
- HY-N0729S5
-
|
Linoleic acid-d2
Deulinoleic acid
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Linoleic Acid-d2 is the deuterium labeled Linoleic acid. Linoleic acid is a common polyunsaturated (PUFA) found in plant-based oils, nuts and seeds. Linoleic acid is a part of membrane phospholipids, and functions as a structural component to maintain a certain level of membrane fluidity of the transdermal water barrier of the epidermis. Linoleic acid induces red blood cells and hemoglobin damage via oxidative mechanism.
|
-
- HY-12496
-
|
NS-1619
|
Potassium Channel
Apoptosis
|
Cancer
Cardiovascular Disease
|
|
NS-1619 is an opener of large conductance Ca 2+-activated K + (BK) channel. NS-1619 is a highly effective relaxant with an EC50 of about 10 – 30 μM in several smooth muscles of blood vessels and other tissues. NS1619 inhibits proliferation and induces apoptosis in A2780 ovarian cancer cells.
|
-
- HY-N0729S2
-
|
Linoleic acid-13C18
|
Endogenous Metabolite
|
Metabolic Disease
Cardiovascular Disease
|
|
Linoleic acid- 13C18 is the 13C labeled Linoleic acid. Linoleic acid is a common polyunsaturated (PUFA) found in plant-based oils, nuts and seeds. Linoleic acid is a part of membrane phospholipids, and functions as a structural component to maintain a certain level of membrane fluidity of the transdermal water barrier of the epidermis. Linoleic acid induces red blood cells and hemoglobin damage via oxidative mechanism [1][2].
|
-
- HY-N0729S
-
|
Linoleic acid-d4
|
Isotope-Labeled Compounds
Endogenous Metabolite
|
Metabolic Disease
Cardiovascular Disease
|
|
Linoleic Acid-d4 is the deuterium labeled Linoleic acid. Linoleic acid is a common polyunsaturated (PUFA) found in plant-based oils, nuts and seeds. Linoleic acid is a part of membrane phospholipids, and functions as a structural component to maintain a certain level of membrane fluidity of the transdermal water barrier of the epidermis. Linoleic acid induces red blood cells and hemoglobin damage via oxidative mechanism [1][2].
|
-
- HY-148030
-
|
XL01126
|
PROTACs
LRRK2
|
Neurological Disease
|
|
XL01126 is a potent degrader of LRRK2 with DC50s of 14 nM (G2019S LRRK2) and 32 nM (WT LRRK2), respectively. XL01126 can cross blood-brain barrier and be used as a degrader probe in Parkinson’s disease research. XL01126 exerts function of study of non-catalytic and scaffolding functions of LRRK2.
|
-
- HY-111964
-
|
Lenacapavir
GS-6207
|
HIV
|
Infection
|
|
Lenacapavir (GS-6207) is a HIV-1 capsid inhibitor. Lenacapavir shows anti-HIV activity with an EC50 of 100 pM in MT-4 cells. Lenacapavir displays a mean EC50 of 50 pM (20-160 pM) against 23 HIV-1 clinical isolates from different subtypes in peripheral blood mononuclear cells (PBMCs).
|
-
- HY-17379
-
-
- HY-132246
-
|
WWL123
|
MAGL
|
Neurological Disease
|
|
WWL123 is a potent and selective ABHD6 inhibitor with an IC50 of 430 nM. WWL123 crosses the blood-brain-barrier and inhibits ABHD6 in brain parenchyma. ABHD6 blockade by WWL123 exerts an antiepileptic effect in Pentylenetetrazole (PTZ)-induced epileptiform seizures and spontaneous seizures in R6/2 mice.
|
-
- HY-B0317BS
-
|
Amlodipine-d4 besylate
Amlodipine (benzenesulfonate)-d4 (besylate)
|
Calcium Channel
|
Cancer
Cardiovascular Disease
|
|
Amlodipine-d4 (besylate) is the deuterium labeled Amlodipine besylate. Amlodipine besylate (Amlodipine benzenesulfonate), an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine besylate can be used for the research of high blood pressure and cancer[1][2][3].
|
-
- HY-109502S
-
|
10-OH-NBP-d4
|
Isotope-Labeled Compounds
|
Neurological Disease
|
|
10-OH-NBP-d4 is deuterium labeled 10-OH-NBP. 10-OH-NBP is a Butylphthalide (3-n-Butylphthalide; NBP; HY-B0647) hydroxylated metabolite and can penetrates the blood-brain barrier (BBB). Butylphthalide exerts neuroprotective effects and has potential for cerebral ischemia research[1].
|
-
- HY-143413
-
|
BuChE-IN-2
|
Amyloid-β
|
Inflammation/Immunology
Neurological Disease
|
|
BuChE-IN-2 is an excellent butyrylcholinesterase (BuChE) inhibitor (IC50s of 1.28 μM and 0.67 μM for BuChE and NO). BuChE-IN-2 can inhibit the aggregation of Aβ, ROS formation and chelate Cu 2+, exhibiting proper blood-brain barrier (BBB) penetration. BuChE-IN-2 has potential to research Alzheimer’s disease.
|
-
- HY-10202
-
|
Tandutinib
MLN518; CT53518
|
FLT3
c-Kit
PDGFR
Apoptosis
|
Cancer
|
|
Tandutinib (MLN518) is a potent and selective inhibitor of the FLT3 with an IC50 of 0.22 μM, and also inhibits c-Kit and PDGFR with IC50s of 0.17 μM and 0.20 μM, respectively. Tandutinib can be used for acute myelogenous leukemia (AML). Tandutinib has the ability to cross the blood-brain barrier.
|
-
- HY-N0729S1
-
|
Linoleic acid-d11
|
Endogenous Metabolite
|
Metabolic Disease
Cardiovascular Disease
|
|
Linoleic acid-d11 is the deuterium labeled Linoleic acid. Linoleic acid is a common polyunsaturated (PUFA) found in plant-based oils, nuts and seeds. Linoleic acid is a part of membrane phospholipids, and functions as a structural component to maintain a certain level of membrane fluidity of the transdermal water barrier of the epidermis. Linoleic acid induces red blood cells and hemoglobin damage via oxidative mechanism [1][2].
|
-
- HY-131334
-
|
AMPK activator 4
|
AMPK
|
Metabolic Disease
|
|
AMPK activator 4 is a potent AMPK activator without inhibition of mitochondrial complex I. AMPK activator 4 selectively activates AMPK in the muscle tissues. AMPK activator 4 dose-dependently improves glucose tolerance in normal mice, and significantly lowers fasting blood glucose level and ameliorates insulin resistance in db/db diabetic mice. Anti-hyperglycemic effect.
|
-
- HY-148250
-
|
TP-050
|
iGluR
|
Neurological Disease
|
|
TP-050 is a potent, orally active and selective NMDAR agonist with an EC50 value of 0.51 µM and 9.6 µM for GluN2A and GluN2D, respecticely. TP-050 can cross the blood-brain barrier (BBB). TP-050 induces hippocampal long-term (LPT) potentiation enhancemen and enhances neuronal signal transmission.
|
-
- HY-B0688
-
|
Dapsone
4,4′-Diaminodiphenyl sulfone; DDS
|
Antibiotic
Parasite
Bacterial
Reactive Oxygen Species
|
Infection
Inflammation/Immunology
|
|
Dapsone (4,4′-Diaminodiphenyl sulfone) is an orally active and blood-brain penetrant sulfonamide antibiotic with bacteriostatic, antimycobacterial and antiprotozoal activities. Dapsone exerts effective antileprosy activity and inhibits folate synthesis in cell extracts of M. leprae. Dapsone is used for dermatologic disorder research, including leprosy, dermatitis herpetiformis, acne vulgaris et al.
|
-
- HY-136527
-
|
BMS-986251
|
ROR
Interleukin Related
|
Inflammation/Immunology
|
|
BMS-986251 is an orally active and selective RORγt inverse agonist with an EC50 of 12 nM for RORγt GAL4. BMS-986251 inhibits IL-17 with an EC50 of 24 nM in human whole blood assay. BMS-986251 demonstrates robust efficacy in mouse acanthosis and Imiquimod-induced (HY-B0180) models (preclinical models of psoriasis).
|
-
- HY-12354
-
|
SB-3CT
|
MMP
|
Cancer
|
|
SB-3CT is a potent and competitive matrix metalloproteinase MMP-2 and MMP-9 inhibitor with Ki values of 13.9 and 600 nM, respectively. SB-3CT has high selectivity for gelatinases. SB-3CT shows blood-brain barrier permeability and has neuroprotective effects and anticancer activity.
|
-
- HY-100822
-
|
(R)-(+)-HA-966
(+)-HA-966
|
iGluR
|
Neurological Disease
|
|
(R)-(+)-HA-966 ((+)-HA-966) is a partial agonist/antagonist of glycine site of the N-methyl-D-aspartate (NMDA) receptor complex. (R)-(+)-HA-966 selectively blocks the activation of the mesolimbic dopamine system by amphetamine. (R)-(+)-HA-966 can cross the blood-brain barrier and has the potential for neuropathic and acute pain.
|
-
- HY-B0228S
-
-
- HY-145845
-
|
HDAC1/MAO-B-IN-1
|
HDAC
Monoamine Oxidase
|
Neurological Disease
|
|
HDAC1/MAO-B-IN-1 is a potent, selective and cross the blood-brain barrier HDAC1/MAO-B inhibitor with IC50 values of 21.4 nM and 99.0 nM for HDAC1 and MAO-B, respectively. HDAC1/MAO-B-IN-1 has the potential for the research of Alzheimer’s disease.
|
-
- HY-W015007S
-
|
Metyrosine-13C9,15N,d7
|
COX
|
Cardiovascular Disease
|
|
Metyrosine- 13C9, 15N,d7 is the deuterium, 13C-, and 15-labeled Metyrosine. Metyrosine is a selective tyrosine hydroxylase enzyme inhibitor. Metyrosine exerts anti-inflammatory and anti-ulcerative effects. Metyrosine significantly inhibits high COX-2 activity[1]. Metyrosine is a very effective agent for blood pressure control[2].
|
-
- HY-111544
-
|
EML741
|
Histone Methyltransferase
|
Cancer
|
|
EML741 is a histone lysine methyltransferase G9a/GLP inhibitor, with an IC50 of 23 nM, Kd of 1.13 μM for G9a. EML741 also inhibits DNMT1 (IC50, 3.1 μM), with no effect on DNMT3a or DNMT3b. EML741 exhibits low cell toxicity, and is membrane permeable and blood-brain barrier penetrated.
|
-
- HY-B0162S
-
|
Ivabradine-d6
|
HCN Channel
|
Cardiovascular Disease
|
|
Ivabradine-d6 is the deuterium labeled Ivabradine[1]. Ivabradine is a potent and orally active HCN (hyperpolarization-activated cyclic nucleotide-gated) channel blocker that inhibits the cardiac pacemaker current (If). Ivabradine reduces dose-dependently heart rate without modification of blood pressure. Ivabradine shows anticonvulsant, anti-ischaemic and anti-anginal activity[2][3][4][5].
|
-
- HY-147678
-
|
GPR40 agonist 5
|
Free Fatty Acid Receptor
|
Metabolic Disease
|
|
GPR40 agonist 5 (compound I-14) is an orally active and potent GPR40 (G protein coupled receptor 40) agonist, with an EC50 of 47 nM. GPR40 agonist 5 decreases the levels of blood glucose and improves the glucose tolerance. GPR40 agonist 5 has sufficient effectiveness for the control of hyperglycemia state in type 2 diabetic mice.
|
-
- HY-153480
-
|
ARC19499
BAX499
|
Factor Xa
|
Others
|
|
ARC19499 is an aptamer that inhibits tissue factor pathway inhibitor (TFPI) , thereby enabling clot initiation and propagation via the extrinsic pathway. The core aptamer binds tightly and specifically to TFPI. ARC19499 blocks TFPI inhibition of both factor Xa and the TF/factor VIIa complex. ARC19499 corrects thrombin generation in hemophilia A and B plasma and restores clotting in FVIII-neutralized whole blood.
|
-
- HY-12098
-
|
Verubulin hydrochloride
MPC-6827 hydrochloride
|
Microtubule/Tubulin
|
Cancer
|
|
Verubulin hydrochloride (MPC-6827 hydrochloride) is a blood brain barrier permeable microtubule-disrupting agent, with potent and broad-spectrum in vitro and in vivo cytotoxic activities. Verubulin hydrochloride (MPC-6827 hydrochloride) exhibits potent anticancer activity in human MX-1 breast and other mouse xenograft cancer models. Verubulin hydrochloride (MPC 6827 hydrochloride) is a promising candidate for the treatment of multiple cancer types.
|
-
- HY-146315
-
|
AChE/BChE-IN-6
|
Cholinesterase (ChE)
Monoamine Oxidase
|
Neurological Disease
|
|
AChE/BChE-IN-6 (compound 22) is a potent dual AChE/BChE inhibitor with IC50 values of 0.809 µM, 2.248 µM and > 100 µM for hBChE, hAChE and hMAO-B, respectively. AChE/BChE-IN-6 penetrates the blood-brain barrier (BBB). AChE/BChE-IN-6 can be used for Alzheimer’s disease (AD) research.
|
-
- HY-D0004
-
|
Azure B
Azure B chloride
|
Monoamine Oxidase
|
Neurological Disease
|
|
Azure B is a cationic dye and the major metabolite of Methylene blue. Azure B is used in making Azure eosin stains for blood smear staining. Azure B is a high-potency, selective and reversible inhibitor of monoamine oxidases (MAO)-A, with IC50s of 11 and 968 nM for recombinant human MAO-A and MAO-B, respectively. Azure B possesses significant antidepressant-like effects.
|
-
- HY-125374
-
|
Larotaxel
XRP9881
|
Apoptosis
|
Cancer
|
|
Larotaxel (XRP9881) is a taxane analogue with preclinical activity against taxane-resistant breast cancer. Larotaxel (XRP9881) exerts its cytotoxic effect by promoting tubulin assembly and stabilizing microtubules, ultimately leading to cell death by apoptosis. It presents the ability to cross the blood brain barrier and has a much lower affinity for P-glycoprotein 1 than Docetaxel.
|
-
- HY-143245
-
|
Monoamine Oxidase B inhibitor 2
|
Monoamine Oxidase
|
Neurological Disease
|
|
Monoamine Oxidase B inhibitor 2 is a potent, reversible, orally active and selective monoamine oxidase B (MAO-B) inhibitor with an IC50 of 1.33 nM. Monoamine Oxidase B inhibitor 2 has antioxidant and anti-neuroinflammatory activities. Monoamine Oxidase B inhibitor 2 can across the blood-brain barrier (BBB), and can be used for Parkinson’s disease study.
|
-
- HY-151389
-
|
BChE-IN-14
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
BChE-IN-14 (compound 19c) is a selective butyrylcholinesterase (BChE) inhibitor with IC50s of 0.23 and 0.011 μM for eqBChE and hBChE, respectively. BChE-IN-14 shows good blood brain barrier permeation and primary cell safety. BChE-IN-14 is able to restore cognitive impairment in vivo, it can be used for the research of Alzheimer’s disease.
|
-
- HY-143244
-
|
Monoamine Oxidase B inhibitor 1
|
Monoamine Oxidase
|
Neurological Disease
|
|
Monoamine Oxidase B inhibitor 1 is a potent, reversible, orally active and selective monoamine oxidase B (MAO-B) inhibitor with an IC50 of 0.02 nM. Monoamine Oxidase B inhibitor 1 has antioxidant and anti-neuroinflammatory activities. Monoamine Oxidase B inhibitor 1 can across the blood-brain barrier (BBB), and can be used for Parkinson’s disease study.
|
-
- HY-117709
-
|
BRD6688
|
HDAC
|
Neurological Disease
|
|
BRD6688 is a selective HDAC2 inhibitor. BRD6688 increases H4K12 and H3K9 histone acetylation in primary mouse neuronal cells. BRD6688 crosses the blood brain barrier and rescues the memory defects associated with p25 induced neurodegeneration in contextual fear conditioning in a CK-p25 mouse model.
|
-
- HY-17401S
-
|
Ranolazine-d8 dihydrochloride
CVT 303-dd8 dihydrochloride; RS 43285-d8
|
Calcium Channel
Sodium Channel
Autophagy
|
Cardiovascular Disease
Cancer
|
|
Ranolazine-d8 (dihydrochloride) is the deuterium labeled Ranolazine dihydrochloride. Ranolazine dihydrochloride (CVT 303 dihydrochloride) is an anti-angina agent that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP)[1][2]. Ranolazine dihydrochloride is also a partial fatty acid oxidation inhibitor[3].
|
-
- HY-B0688S
-
|
Dapsone-d8
4,4′-Diaminodiphenyl sulfone-d8; DDS-d8
|
Antibiotic
Parasite
Bacterial
Reactive Oxygen Species
|
Cancer
Infection
Inflammation/Immunology
|
|
Dapsone-d8 is a deuterium labeled Dapsone. Dapsone is an orally active and blood-brain penetrant sulfonamide antibiotic with antibacterial, antigenic and anti-inflammatory activities[1]. Dapsone exerts effective antileprosy activity and inhibits folate synthesis in cell extracts of M. leprae. Dapsone can be used as an anticonvulsant and also in the research of skin and glioblastoma diseases[2][3][4][5].
|
-
- HY-17368
-
|
Rivastigmine
S-Rivastigmine
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Rivastigmine (S-Rivastigmine) is an orally active and potent cholinesterase (ChE) inhibitor and inhibits butyrylcholinesterase (BChE) and acetylcholinesteras (AChE) with IC50s of 0.037 μM , 4.15 μM, respectively. Rivastigmine can pass the blood brain barrier (BBB). Rivastigmine is a parasympathomimetic or cholinergic agent used for the research of mild to moderate dementia of the Alzheimer's type and dementia due to Parkinson's disease.
|
-
- HY-B1126
-
|
Orphenadrine hydrochloride
|
iGluR
|
Neurological Disease
|
|
Orphenadrine hydrochloride is an orally active and non-competitive NMDA receptor antagonist (crosses the blood-brain barrier) with a Ki of 6.0 μM. Orphenadrine hydrochloride relieves stiffness, pain and discomfort due to muscle strains, sprains or other injuries. Orphenadrine hydrochloride is also used to relieve tremors associated with parkinson's disease. Orphenadrine citrate has good neuroprotective properties, can be used in studies of neurodegenerative diseases.
|
-
- HY-B1684
-
|
Mebrofenin
SQ 26962
|
Biochemical Assay Reagents
|
Others
|
|
Mebrofenin (SQ 26962) is a type of iminodiacetic acid (IDA). Mebrofenin is available as a ready to use the kit for radio-labeling with Tc-99m. Tc-99m Mebrofenin, a diagnostic agent, is used for hepatobiliary imaging. Tc-99m Mebrofenin is the radiopharmaceutical of choice for the evaluation of hepatic function.
|
-
- HY-121238
-
|
Hyocholic Acid
|
Others
|
Metabolic Disease
|
|
Hyocholic Acid is a bile acid found in pig. Hyocholic Acid can also be found in urine samples from patients with cholestasis. Hyocholic Acid promotes GLP-1 secretion via activating TGR5 and inhibiting FXR in enteroendocrine cells. Hyocholic Acid is known for its exceptional resistance to type 2 diabetes .
|
-
- HY-A0119
-
|
Nitroprusside disodium dihydrate
Sodium nitroprusside dihydrate; Sodium Nitroferricyanide(III) Dihydrate
|
Autophagy
|
Cardiovascular Disease
Cancer
|
|
Nitroprusside disodium dehydrate (Sodium nitroprusside dihydrate) is a vasodilator that available for the research of acute hypertension, heart failure. Nitroprusside disodium dehydrate induces autophagy in glutathione-depleted osteoblasts. Nitroprusside disodium dehydrate acts as a nitric oxide (NO) donor in a rat intestinal ischemia reperfusion model.
|
-
- HY-128144
-
-
- HY-131722
-
|
EA4
|
Phospholipase
|
Cardiovascular Disease
|
|
EA4, a derivative of quinone, is an inhibitor for both rPLA and cPLA. EA4 can inhibit rPLA2 with a Ki value of 130 μM. EA4 can be used for the research of hemostasis, thrombosis, and erythropoiesis.
|
-
- HY-15650
-
|
SGC0946
|
Histone Methyltransferase
|
Cancer
|
|
SGC0946 is a selective DOT1LH3K79 methyltransferase) inhibitor, with an IC50 of 0.3 nM. SGC0946 results in G1 arrest, inhibits potential of cell self-renewal and metastatic, also induces cell differentiation. SGC0946 can be used in studies of leukemia and solid tumors and also serve as a probe to further investigate the cellular mechanism of DOT1L in both normal and diseased cells.
|
-
- HY-101834
-
|
ACT-462206
|
Orexin Receptor (OX Receptor)
|
Others
|
|
ACT-462206 is an orally active and potent dual Orexin 1/Orexin 2 receptor antagonist with IC50s of 60 nM (Orexin 1) and 11 nM (Orexin 2), respectively. ACT-462206 exhibits brain penetration properties, and can be used for insomnia, stress/anxiety-related disorders and addiction research.
|
-
- HY-150744
-
|
ODN 24888
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
ODN 24888 is an guanine-modified inhibitory oligonucleotides (INH-ODN), shows potent inhibition on TLR7/TLR9-mediated signaling. ODN 24888 impairs IFN-α level and NF-κB activation, inhibits IL-6 release. ODN 24888 involves in immune and inflammatory responses, can be used as a vaccine adjuvant.
|
-
- HY-147234
-
-
- HY-146059
-
|
Antibacterial agent 99
|
Bacterial
|
Infection
|
|
Antibacterial agent 99 (compound 7b) is a potent antibacterial agent. Antibacterial agent 99 shows significant antibacterial and antifungal activity. Antibacterial agent 99 dose not show haemolytic activity.
|
-
- HY-128463
-
-
- HY-137262
-
|
Protein deglycase DJ-1 against-1
|
Others
|
Neurological Disease
|
|
Protein deglycase DJ-1 against-1, a DJ-1-binding compound, dependently targets DJ1. Protein deglycase DJ-1 against-1 penetrates through the blood brain barrier (BBB). Protein deglycase DJ-1 against-1 is used as a neuroprotective agent and has the potential for Parkinson's disease research.
|
-
- HY-111655
-
|
SKA-31
|
Potassium Channel
|
Cardiovascular Disease
|
|
SKA-31 is a potent potassium channel activator with EC50s of 260 nM, 1.9 μM, 2.9 μM, and 2.9 μM for KCa3.1, KCa2.2, KCa2.1 and KCa2.3, respectively. SKA-31 potentiates endothelium-derived hyperpolarizing factor response and lowers blood pressure.
|
-
- HY-17387
-
|
(-)-Huperzine A
Huperzine A
|
Cholinesterase (ChE)
Apoptosis
iGluR
|
Neurological Disease
|
|
(-)-Huperzine A (Huperzine A) is an alkaloid isolated from Huperzia serrata, with neuroprotective activity. (-)-Huperzine A is a potent, highly specific, reversible and blood-brain barrier penetrant inhibitor of acetylcholinesterase (AChE), with an IC50 of 82 nM. (-)-Huperzine A also is non-competitive antagonist of N-methyl-D-aspartate glutamate (NMDA) receptor. (-)-Huperzine A is developed for the research of neurodegenerative diseases, including Alzheimer’s disease.
|
-
- HY-129460
-
|
XJB-5-131
|
Reactive Oxygen Species
|
Neurological Disease
|
|
XJB-5-131 is a mitochondria-targeted ROS and electron scavenger. XJB-5-131 is a bi-functional antioxidant that comprises a radical scavenger. XJB-5-131 is a synthetic antioxidant that targets mitochondria. XJB-5-131 is an effective ionizing irradiation protector and mitigator of cord blood mononuclear cells (CB MNCs).
|
-
- HY-135749
-
|
BN201
|
Others
|
Inflammation/Immunology
Neurological Disease
|
|
BN201 promotes neuronal differentiation, the differentiation of precursor cells to mature oligodendrocytes (EC50 of 6.3 μM) in vitro, and the myelination of new axons (EC50 of 16.6 μM). BN201 is able to cross the blood-brain barrier by active transport and activate pathways (IGF-1 pathway) associated with the response to stress and neuron survival. BN201 has potently neuroprotective effects.
|
-
- HY-15008
-
|
L-368,899
|
Oxytocin Receptor
|
Endocrinology
|
|
L-368,899 is an orally active and selective OT (oxytocin ) receptor antagonist, with IC50s of 8.9 and 26 nM for uterus of rat and human, respectively. L-368,899 can cross the blood-brain barrier (BBB). L-368,899 inhibits oxytocin-stimulated uterine contractions in rats and can be used in study of preterm labor.
|
-
- HY-12995A
-
|
(S)-BI 665915
|
FLAP
|
Inflammation/Immunology
|
|
(S)-BI 665915 is an orally active oxadiazole-containing 5-lipoxygenase-activating protein (FLAP) inhibitor with an IC50 of 1.7 nM for FLAP binding. (S)-BI 665915 inhibits FLAP functional in human whole blood with an IC50 of 45 nM. (S)-BI 665915 demonstrates an excellent cross-species agent metabolism and pharmacokinetics (DMPK) profile and a dose-dependent inhibition of LTB4 production.
|
-
- HY-N4103
-
|
Fucosterol
|
PARP
Endogenous Metabolite
|
Cancer
Metabolic Disease
|
|
Fucosterol is a sterol isolated from algae, seaweed or diatoms. Fucosterol exhibits various biological activities, including antioxidant, anti-adipogenic, blood cholesterol reducing, anti-diabetic and anti-cancer activities. Fucosterol regulates adipogenesis via inhibition of PPARα and C/EBPα expression and can be used for anti-obesity agents development research.
|
-
- HY-P9928
-
|
Alirocumab
REGN 727; SAR 236553
|
Ser/Thr Protease
|
Metabolic Disease
|
|
Alirocumab (REGN 727) is a human monoclonal antibody inhibiting proprotein convertase subtilisin/kexin type 9 (PCSK9). Alirocumab specifically binds PCSK9, a down regulator of liver low-density lipoprotein (LDL)-receptors, thereby increasing the ability of the liver to bind LDL-cholesterol (LDL-C) and reducing levels of LDL-C in blood. Alirocumab can be used for the research of hypercholesterolemia.
|
-
- HY-150702
-
|
MAGLi 432
|
MAGL
|
Inflammation/Immunology
Neurological Disease
|
|
MAGLi 432 is a non-covalent, potent, highly selective, and reversible MAGL inhibitor. MAGLi 432 binds with high affinity to the MAGL active site, with IC50 values of 4.2 nM (human enzyme) and 3.1 nM (mouse enzyme). MAGLi 432 can be used in the research of chronic inflammation, blood–brain barrier dysfunction, neurological disorders such as multiple sclerosis, Alzheimer’s disease and Parkinson’s disease.
|
-
- HY-P1036
-
|
Compstatin
|
Complement System
|
Others
|
|
Compstatin, a 13-residue cyclic peptide, is a potent inhibitor of the complement system C3 with species specificity. Compstatin binds to baboon C3 and is resistant to proteolytic cleavage in baboon blood (similar to humans). Compstatin inhibits only the activation of primates’ complement system. Compstatin exhibits IC50 values of 63 μM and 12 μM for classical and alterative complement pathway, respectively.
|
-
- HY-17573A
-
|
Carbetocin acetate
|
Oxytocin Receptor
|
Endocrinology
Neurological Disease
|
|
Carbetocin acetate, an oxytocin (OT) analogue, is an oxytocin receptor agonist with a Ki of 7.1 nM. Carbetocin acetate has high affinity to chimeric N-terminus (E1) of the oxytocin receptor (Ki=1.17 μM). Carbetocin acetate has the potential for postpartum hemorrhage research. Carbetocin acetate can crosse the blood-brain barrier and produces antidepressant-like activity via activation of oxytocin receptors in the CNS.
|
-
- HY-149279
-
|
JNK3 inhibitor-7
|
JNK
|
Neurological Disease
|
|
JNK3 inhibitor-7 is a potent, orally active and cross the blood-brain barrier JNK3 inhibitor with IC50 values of 53, 973, 1039 nM for JNK3, JNK2, JNK1, respectively. JNK3 inhibitor-7 shows significant neuroprotective effects. JNK3 inhibitor-7 has the potential for the research of Alzheimer’s disease (AD).
|
-
- HY-B0280S2
-
|
Ranolazine-d3
|
Sodium Channel
Calcium Channel
|
Cardiovascular Disease
Cancer
|
|
Ranolazine-d3 is the deuterium labeled Ranolazine. Ranolazine (CVT 303) is an anti-angina agent that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP)[1][2]. Ranolazine is also a partial fatty acid oxidation (FAO) inhibitor[3]. Antianginal agent.
|
-
- HY-137466
-
|
ARN-21934
|
Topoisomerase
|
Cancer
|
|
ARN-21934 is a potent, highly selective, blood-brain barrier (BBB) penetrant inhibitor for human topoisomerase II α over β. ARN-21934 inhibits DNA relaxation with an IC50 of 2 μM as compared to the anticancer agent Etoposide (IC50=120 μM). ARN-21934 exhibits a favorable in vivo pharmacokinetic profile and is a promising lead compound for anticancer research.
|
-
- HY-17573
-
|
Carbetocin
|
Oxytocin Receptor
|
Endocrinology
Neurological Disease
|
|
Carbetocin, an oxytocin (OT) analogue, is an oxytocin receptor agonist with a Ki of 7.1 nM. Carbetocin has high affinity to chimeric N-terminus (E1) of the oxytocin receptor (Ki=1.17 μM). Carbetocin has the potential for postpartum hemorrhage research. Carbetocin can crosse the blood-brain barrier and produces antidepressant-like activity via activation of oxytocin receptors in the CNS.
|
-
- HY-B0280S
-
|
Ranolazine-d5
CVT 303-d5; RS 43285-003-d5
|
Isotope-Labeled Compounds
Sodium Channel
Calcium Channel
|
Cardiovascular Disease
Cancer
|
|
Ranolazine-d5 is the deuterium labeled Ranolazine. Ranolazine (CVT 303) is an anti-angina drug that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP)[1][2]. Ranolazine is also a partial fatty acid oxidation (FAO) inhibitor[3]. Antianginal agent.
|
-
- HY-B0280S1
-
|
Ranolazine-d8
|
Isotope-Labeled Compounds
Sodium Channel
Calcium Channel
|
Cardiovascular Disease
Cancer
|
|
Ranolazine-d8 is the deuterium labeled Ranolazine. Ranolazine (CVT 303) is an anti-angina agent that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP)[1][2]. Ranolazine is also a partial fatty acid oxidation (FAO) inhibitor[3]. Antianginal agent.
|
-
- HY-128342
-
|
Complement C5-IN-1
|
Complement System
|
Inflammation/Immunology
|
|
Complement C5-IN-1 (Compound 7) is a small-molecule inhibitor of complement component 5 protein (C5). Complement C5-IN-1 interacts with C5 to prevent its cleavage by the C5 convertase and blocks zymosan-induced the membrane-attack complex (MAC) deposition in 50% human whole blood with an IC50 of 0.77 µM.
|
-
- HY-D1684
-
|
DCDAPH
|
Amyloid-β
|
Neurological Disease
|
|
DCDAPH (Compound 2c) is a novel smart NIRF probe for detection of β-amyloid (Aβ) plaques (λex/λem=597/665 nm in PBS). DCDAPH shows high affinity for Aβ aggregates (Ki=37 nM, Kd=27 nM). DCDAPH shows good blood brain barrier permeation and can meet most of the requirements for the detection of Aβ plaques both in vitro and in vivo.
|
-
- HY-147395
-
|
GPR52 agonist-1
|
Others
|
Neurological Disease
|
|
GPR52 agonist-1 is a potent, orally active and blood-brain barrier (BBB) penetrant GPR52 agonist with an pEC50 value of 7.53. GPR52 agonist-1 affects cAMP accumulation through direct interaction with GPR52. GPR52 agonist-1 can significantly suppress Methamphetamine-induced hyperactivity in mice. Antipsychotic activity.
|
-
- HY-B0369A
-
|
Orphenadrine citrate
|
iGluR
|
Neurological Disease
|
|
Orphenadrine citrate is an orally active and non-competitive NMDA receptor antagonist (crosses the blood-brain barrier) with a Ki of 6.0 μM. Orphenadrine citrate relieves stiffness, pain and discomfort due to muscle strains, sprains or other injuries. Orphenadrine citrate is also used to relieve tremors associated with parkinson's disease. Orphenadrine citrate has good neuroprotective properties, can be used in studies of neurodegenerative diseases.
|
-
- HY-149280
-
|
JNK3 inhibitor-8
|
JNK
|
Neurological Disease
|
|
JNK3 inhibitor-8 is a potent, delective, orally active and cross the blood-brain barrier JNK3 inhibitor with IC50 values of 21, 2203, >10000 nM for JNK3, JNK2, JNK1, respectively. JNK3 inhibitor-8 shows significant neuroprotective effects. JNK3 inhibitor-8 has the potential for the research of Alzheimer’s disease (AD).
|
-
- HY-Y0271S
-
|
Urea-15N2
Carbamide-15N2; Carbonyldiamide-15N2
|
Endogenous Metabolite
|
Cardiovascular Disease
Cancer
|
|
Urea- 15N2 is the 15N-labeled Urea. Urea is a powerful protein denaturant via both direct and indirect mechanisms[1]. A potent emollient and keratolytic agent[2]. Used as a diuretic agent. Blood urea nitrogen (BUN) has been utilized to evaluate renal function[3]. Widely used in fertilizers as a source of nitrogen and is an important raw material for the chemical industry.
|
-
- HY-P0203
-
|
α-CGRP, rat
|
CGRP Receptor
|
Metabolic Disease
Inflammation/Immunology
Cardiovascular Disease
|
|
α-CGRP, rat, a neuropeptide (calcitonin gene-related peptide (CGRP)) mainly expressed in neuromuscular junction, is a potent vasodilator. α-CGRP, rat can lead to a fall in blood pressure and an increase in heart rate by peripheral administration, also relax colonie smooth muscle. α-CGRP, rat has the potential in cardiovascular, pro-inflammatory, migraine and metabolic studies.
|
-
- HY-150639
-
|
Everafenib
|
Raf
|
Cancer
|
|
Everafenib is a potent and blood-brain barrier (BBB) penetrant BRAF inhibitor, also inhibits MAPK signaling. Everafenib has inhibitory activity against a panel of V600EBRAF melanoma cell lines with IC50 values of 2-10 nM, which is better than Dabrafenib (HY-14660) and Vemurafenib (HY-12057). Everafenib has efficacy in an intracranial mouse model of metastatic melanoma.
|
-
- HY-Y0271S1
-
|
Urea-d4
1,1,3,3-Tetradeuteriourea; Urea-d4
|
Endogenous Metabolite
|
|
|
Urea-d4 is the deuterium labeled Urea[1]. Urea is a powerful protein denaturant via both direct and indirect mechanisms[2]. A potent emollient and keratolytic agent[3]. Used as a diuretic agent. Blood urea nitrogen (BUN) has been utilized to evaluate renal function[4]. Widely used in fertilizers as a source of nitrogen and is an important raw material for the chemical industry.
|
-
- HY-N4190
-
|
Britannilactone diacetate
1,6-O,O-Diacetylbritannilactone; Di-O-acetylbritannilactone
|
NO Synthase
|
Inflammation/Immunology
Neurological Disease
|
|
Britannilactone diacetate (1,6-O,O-Diacetylbritannilactone; Compound 2) exhibits potential NO inhibition effect. Britannilactone diacetate exhibits activity against NO production induced by LPS in BV-2 microglial cells with the EC50 value of 6.3 μM. Britannilactone diacetate exhibits a favorable blood-brain barriers (BBB) penetration and absorption, distribution, metabolism, excretion, and toxicity (ADMET) property.
|
-
- HY-B0410A
-
|
Pramipexole dihydrochloride hydrate
|
Dopamine Receptor
|
Neurological Disease
|
|
Pramipexole dihydrochloride hydrate is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole dihydrochloride hydrate can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS).
|
-
- HY-19918A
-
|
Anatabine dicitrate
|
NF-κB
Amyloid-β
nAChR
|
Inflammation/Immunology
Neurological Disease
|
|
Anatabine dicitrate is a tobacco alkaloid that can cross the blood-brain barrier. Anatabine dicitrate is a potent α4β2 nAChR agonist. Anatabine dicitrate inhibits NF-κB activation lower amyloid-β (Aβ) production by preventing the β-cleavage of amyloid precursor protein (APP). Anatabine dicitrate has anti-inflammatory effects and has the potential for neurodegenerative disorders treatment.
|
-
- HY-A0067S
-
|
Oxybenzone-d5
|
RAR/RXR
Apoptosis
Autophagy
|
Neurological Disease
|
|
Oxybenzone-d5 is the deuterium labeled Oxybenzone[1]. Oxybenzone (Benzophenone 3) is a commonly used UV filter in sun tans and skin protectants. Oxybenzone act as endocrine disrupting chemicals (EDCs) and can pass through the placental and blood-brain barriers. Benzophenone-3 impairs autophagy, alters epigenetic status, and disrupts retinoid X receptor signaling in apoptotic neuronal cells[2][3][4].
|
-
- HY-N0631
-
|
Cornuside
|
p38 MAPK
NF-κB
|
Inflammation/Immunology
|
|
Cornuside is a secoiridoid glucoside isolated from the fruit of Cornus officinalis Sieb. et Zucc., which is a traditional oriental medicine for treating inflammatory diseases and invigorating blood circulation. Cornuside inhibits mast cell-mediated allergic response by down-regulating MAPK and NF-κB signaling pathways. Cornuside has anti-allergic effects in vivo and in vitro which suggests a therapeutic application of this agent in inflammatory allergic diseases.
|
-
- HY-100432
-
|
LOC14
|
PDI
|
Inflammation/Immunology
Neurological Disease
|
|
LOC14 is a potent Protein disulfide isomerase (PDI) inhibitor with EC50 and Kd values of 500 nM and 62 nM, respectively. LOC14 exhibits high stability in mouse liver microsomes and blood plasma, low intrinsic microsome clearance, and low plasma-protein binding.
LOC14 inhibits PDIA3 activity, decreases intramolecular disulfide bonds and subsequent oligomerization (maturation) of HA in lung epithelial cells.
|
-
- HY-151574
-
|
PfGSK3/PfPK6-IN-1
|
Parasite
|
Infection
|
|
PfGSK3/PfPK6-IN-1 (compound 23e) is a potent inhibitor of plasmodial kinases PfGSK3 and PfPK6, with IC50s of 97 nM and 8 nM, respectively. PfGSK3/PfPK6-IN-1 exerts antiplasmodial activity against blood stage Pf3D7 parasites with an EC50 value of 1.4 mM.
|
-
- HY-13821
-
|
Epoxomicin
BU-4061T
|
Proteasome
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Epoxomicin (BU-4061T) is an epoxyketone-containing natural product and a potent, selective and irreversible proteasome inhibitor. Epoxomicin covalently binds to the LMP7, X, MECL1, and Z catalytic subunits of the proteasome and potently inhibits primarily the chymotrypsin-like activity. Epoxomicin can cross the blood-brain barrier. Epoxomicin has strongly antitumor and anti-inflammatory activity.
|
-
- HY-107384
-
|
Asimadoline
EMD-61753
|
Opioid Receptor
|
Metabolic Disease
Inflammation/Immunology
Neurological Disease
|
|
Asimadoline (EMD-61753) is an orally active, selective and peripherally active κ-opioid agonist with IC50s of 5.6 nM (guinea pig) and 1.2 nM (human recombinant). Asimadoline has low permeability across the blood brain barrier and has peripheral anti-inflammatory actions. Asimadoline ameliorates allodynia in diabetic rats and has the potential for irritable bowel syndrome (IBS).
|
-
- HY-148114
-
|
MOPIPP
|
Others
|
Cancer
|
|
MOPIPP is a novel indolebased chalcone, and vacuolin-1, is a non-lethal vacuoleinducing 2-propyl analog of MOMIPP (HY-148114). MOPIPP induces cellular vacuolization and increases autophagosomes numbers. MOPIPP also triggers methuosis, and interrupts glucose uptake and glycolytic metabolism. MOPIPP can cross the blood-brain barrier and shows efficacy in suppressing tumor progression agaisnt glioblastoma cells.
|
-
- HY-107384A
-
|
Asimadoline hydrochloride
EMD-61753 hydrochloride
|
Opioid Receptor
|
Metabolic Disease
Inflammation/Immunology
Neurological Disease
|
|
Asimadoline (EMD-61753) hydrochloride is an orally active, selective and peripherally active κ-opioid agonist with IC50s of 5.6 nM (guinea pig) and 1.2 nM (human recombinant). Asimadoline hydrochloride has low permeability across the blood brain barrier and has peripheral anti-inflammatory actions. Asimadoline hydrochloride ameliorates allodynia in diabetic rats and has the potential for irritable bowel syndrome (IBS).
|
-
- HY-141661
-
|
Aβ/tau aggregation-IN-1
|
Amyloid-β
|
Neurological Disease
|
|
Aβ/tau aggregation-IN-1 is a potent Aβ1-42 β-sheets formation and tau aggregation inhibitor. The KD values of Aβ/tau aggregation-IN-1 with Aβ1-42 and tau are 160 μM and 337 μM, respectively. Aβ/tau aggregation-IN-1 can permeate the blood-brain barrier.
|
-
- HY-N10534
-
|
Lewis X trisaccharide
Lewis X
|
Parasite
|
Cancer
Infection
Inflammation/Immunology
|
|
Lewis X trisaccharide (Lewis X, Le x) is a potent TH2 regulator, antagonizes LPS-induced IL-12 immune expression. Lewis X trisaccharide is a human histo-blood group antigen, plays an key role in cell-cell adhesion, and servers as a tumor marker. Lewis X trisaccharide is highly expressed in the outer membrane of the parasite, can be used for the immunology research of schistosomiasis.
|
-
- HY-151886
-
|
NU223612
|
PROTACs
Indoleamine 2,3-Dioxygenase (IDO)
|
Cancer
Neurological Disease
|
|
NU223612 is a potent PROTAC (PROTACs) that degrades indoleamine 2,3-dioxygenase 1 (IDO1) (Indoleamine 2,3-Dioxygenase (IDO)) with a Kd of 640 nM. NU223612 potently degrades the IDO1 protein through CRBN-mediated proteasomal degradation. NU223612 is bound to CRBN with an affinity of 290 nM. NU223612 can cross the blood-brain barrier (BBB).
|
-
- HY-P9928A
-
|
Alirocumab (anti-PCSK9)
REGN 727(anti-PCSK9); SAR 236553(anti-PCSK9)
|
Ser/Thr Protease
|
Cardiovascular Disease
|
|
Alirocumab (anti-PCSK9) is a human monoclonal antibody inhibiting proprotein convertase subtilisin/kexin type 9 (PCSK9). Alirocumab specifically binds PCSK9, a down regulator of liver low-density lipoprotein (LDL)-receptors, thereby increasing the ability of the liver to bind LDL-cholesterol (LDL-C) and reducing levels of LDL-C in blood. Alirocumab can be used for the research of hypercholesterolemia.
|
-
- HY-B0228S1
-
|
Adenosine-13C5
Adenine riboside-13C5; D-Adenosine-13C5
|
Apoptosis
Nucleoside Antimetabolite/Analog
Autophagy
Endogenous Metabolite
|
|
|
Adenosine- 13C5 is the 13C labeled Adenosine[1]. Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physiology, including neuronal activity, vascular function, platelet aggregation, and blood cell regulation[2][3].
|
-
- HY-17364S
-
|
Temozolomide-d3
|
DNA Alkylator/Crosslinker
Autophagy
Apoptosis
|
Cancer
|
|
Temozolomide-d3 is the deuterium labeled Temozolomide. Temozolomide (NSC 362856) is an oral active DNA alkylating agent that crosses the blood-brain barrier. Temozolomide is also a proautophagic and proapoptotic agent. Temozolomide is effective against tumor cells that are characterized by low levels of O6-alkylguanine DNA alkyltransferase (OGAT) and a functional mismatch repair system. Temozolomide has antitumor and antiangiogenic effects[1][2].
|
-
- HY-106934
-
|
Peldesine
BCX 34
|
Nucleoside Antimetabolite/Analog
HIV
|
Cancer
Infection
Inflammation/Immunology
|
|
Peldesine (BCX 34) is a potent, competitive, reversible and orally active purine nucleoside phosphorylase (PNP) inhibitor with IC50s of 36 nM, 5 nM, and 32 nM for human, rat, and mouse red blood cell (RBC) PNP, respectively. Peldesine is also a T-cell proliferation inhibitor with an IC50 of 800 nM. Peldesine has the potential for cutaneous T-cell lymphoma, psoriasis and HIV infection research.
|
-
- HY-B0410
-
|
Pramipexole
|
Dopamine Receptor
|
Neurological Disease
|
|
Pramipexole is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS).
|
-
- HY-105066
-
|
Davunetide
|
Microtubule/Tubulin
Amyloid-β
|
Neurological Disease
|
|
Davunetide is an eight amino acid snippet derived from activity-dependent neuroprotective protein (ADNP), a neurotrophic factor that exists in the mammalian CNS. Davunetide possesses neuroprotective, neurotrophic and cognitive protective roperties. Davunetide, a microtubule-stabilizing peptide, interacts with and stabilises neuron-specific βIII-tubulin in vitro. Davunetide penetrates the blood-brain barrier and is non-toxic. Davunetide inhibits Aβ aggregation and Aβ-induced neurotoxicity.
|
-
- HY-118858
-
|
UCPH-102
|
Others
|
Cancer
Neurological Disease
|
|
UCPH-102 is a highly selective EAAT1 inhibitor with an IC50 of 0.43 µM. UCPH-102 exhibits a specific anti-proliferative effect on T-ALL cells. UCPH-102 also shows good blood-brain permeability, which can be used in studies of amyotrophic lateral sclerosis, Alzheimer’s disease, chronic pain and obsessive compulsive disorder.
|
-
- HY-144632
-
|
Antifungal agent 22
|
Fungal
|
Infection
|
|
Antifungal agent 22 (compound D16) is a potential and orally active antifungal agent for CM (cryptococcal meningitis), with an IC50 of 0.5 μg/mL. Antifungal agent 22 can penetrate the blood-brain barrier and kill the C. neoformans H99 cells by destroying the integrity of fungal cell membranes. Antifungal agent 22 shows selective anti-Cryptococcus activity with good metabolic stability and low cytotoxicity.
|
-
- HY-106934A
-
|
Peldesine dihydrochloride
BCX 34 dihydrochloride
|
Nucleoside Antimetabolite/Analog
HIV
|
Cancer
Infection
Inflammation/Immunology
|
|
Peldesine (BCX 34) dihydrochloride is a potent, competitive, reversible and orally active purine nucleoside phosphorylase (PNP) inhibitor with IC50s of 36 nM, 5 nM, and 32 nM for human, rat, and mouse red blood cell (RBC) PNP, respectively. Peldesine dihydrochloride is also a T-cell proliferation inhibitor with an IC50 of 800 nM. Peldesine dihydrochloride has the potential for cutaneous T-cell lymphoma, psoriasis and HIV infection research.
|
-
- HY-150508
-
|
MK-0159
|
CD38
|
Metabolic Disease
Cardiovascular Disease
|
|
MK-0159 (compound 37) is an orally active, potent and selective CD38 inhibitor, with IC50 values of 22, 3, and 70 nM for human, mouse and rat CD38, respectively. MK-0159 also shows good microsomal stability for human and rodent liver microsomes. MK-0159 increases NAD + (nicotinamide adenine dinucleotide) and reduces ADPR (adenosine diphosphate ribose) in whole blood and heart.
|
-
- HY-17355
-
|
Pramipexole dihydrochloride
|
Dopamine Receptor
|
Neurological Disease
|
|
Pramipexole dihydrochloride is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole dihydrochloride can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS).
|
-
- HY-P99371
-
|
Lirentelimab
AK002; Anti-Siglec-8 Reference Antibody (lirentelimab)
|
Apoptosis
|
Inflammation/Immunology
|
|
Lirentelimab (AK002) is a humanized IgG1 monoclonal antibody that targets sialic acid-binding Ig-like lectin 8 (SIGLEC8). Lirentelimab induces cell apoptosis of IL-5-activated eosinophils and inhibits IgE-mediated mast cell activation. Lirentelimab can be used for the research of eosinophilic gastritis and duodenitis.
|
-
- HY-111372
-
|
Finerenone
BAY 94-8862
|
Mineralocorticoid Receptor
|
Cardiovascular Disease
|
|
Finerenone (BAY 94-8862) is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist (IC50=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold). Finerenone has the potential for cardiorenal diseases research, such as type 2 diabetes mellitus and chronic kidney disease.
|
-
- HY-10797
-
-
- HY-151871
-
|
ICeD-2
|
Dipeptidyl Peptidase
HIV
|
Infection
|
|
ICeD-2 is a inducer of cell death, can induce HIV-1 infected cell kill. ICeD-2-mediated HIV-1 infected cell kill is dependent on HIV-1 protease activity. ICeD-2 potently blocks hydrolysis of Gly-Pro-AMC by dipeptidyl peptidase DPP8 and DPP9. ICeD-2 shows strong stabilization of DPP9 in PBMCs.
|
-
- HY-115681
-
|
(2R/S)-6-PNG
6-Prenylnaringenin; (±)-6-Prenylnaringenin
|
Calcium Channel
|
Neurological Disease
|
|
(2R/S)-6-PNG (6-Prenylnaringenin) is a potent and reversible Cav3.2 T-type Ca 2+ channels (T-channels) blocker. (2R/S)-6-PNG can penetrate the blood-brain barrier (BBB). (2R/S)-6-PNG suppresses neuropathic and visceral pain in mice.
|
-
- HY-111817
-
|
ACT-451840
|
Parasite
|
Infection
|
|
ACT-451840 is an orally active, potent and low-toxicity compound, showing activity against sensitive and resistant plasmodium falciparum strains. ACT-451840 targets all asexual blood stages of the parasite, has a rapid onset of action. ACT-451840 behaves in a way similar to artemisinin derivatives, with very rapid onset of action and elimination of parasite. ACT-451840 can be used for the research of malarial.
|
-
- HY-11017
-
|
Rivastigmine tartrate
ENA 713; SDZ-ENA 713
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Rivastigmine tartrate (ENA 713; SDZ-ENA 713) is an orally active and potent cholinesterase (ChE) inhibitor and inhibits butyrylcholinesterase (BChE) and acetylcholinesteras (AChE) with IC50s of 0.037 μM, 4.15 μM, respectively. Rivastigmine tartrate can pass the blood brain barrier (BBB). Rivastigmine tartrate is a parasympathomimetic or cholinergic agent used for the research of mild to moderate dementia of the Alzheimer's type and dementia due to Parkinson's disease.
|
-
- HY-B0688S1
-
|
Dapsone-d4
4,4′-Diaminodiphenyl sulfone-d4; DDS-d4
|
Antibiotic
Parasite
Bacterial
Reactive Oxygen Species
|
Infection
Inflammation/Immunology
|
|
Dapsone-d4 is the deuterium labeled Dapsone. Dapsone (4,4′-Diaminodiphenyl sulfone) is an orally active and blood-brain penetrant sulfonamide antibiotic with bacteriostatic, antimycobacterial and antiprotozoal activities[1]. Dapsone exerts effective antileprosy activity and inhibits folate synthesis in cell extracts of M. leprae. Dapsone is used for dermatologic disorder research, including leprosy, dermatitis herpetiformis, acne vulgaris et al[2][3].
|
-
- HY-108039
-
|
HE 3286
NE-3107
|
NF-κB
|
Metabolic Disease
Inflammation/Immunology
Neurological Disease
|
|
HE 3286 is a synthetic derivative of a natural anti-inflammatory steroid, β-AET. HE 3286 is an orally active partial NF-κB inhibitor. HE3286 reduces proinflammatory signals, including IL-6 and matrix metallopeptidase 3. HE 3286 freely penetrates the blood brain barrier in mice. HE 3286 can be used for the research of the ulcerative colitis, arthritis, experimental autoimmune encephalomyelitis.
|
-
- HY-144607
-
|
Mu opioid receptor antagonist 2
|
Opioid Receptor
|
Neurological Disease
|
|
Mu opioid receptor antagonist 2 (compound 25) is a potent, selective and blood-brain barrier (BBB) penetrant μ opioid receptor (MOR) antagonist with a Ki of 0.37 nM and an EC50 of 0.44 nM. Mu opioid receptor antagonist 2 has remarkable CNS antagonism against morphine, and precipitated fewer withdrawal symptoms than Naloxone. Mu opioid receptor antagonist 2 can be used for researching opioid use disorders (OUD).
|
-
- HY-P1036A
-
|
Compstatin TFA
|
Complement System
|
Others
|
|
Compstatin TFA, a 13-residue cyclic peptide, is a potent inhibitor of the complement system C3 with species specificity. Compstatin TFA binds to baboon C3 and is resistant to proteolytic cleavage in baboon blood (similar to humans). Compstatin TFA inhibits only the activation of primates’ complement system. Compstatin TFA exhibits IC50 values of 63 μM and 12 μM for classical and alterative complement pathway, respectively.
|
-
- HY-103441
-
|
JNJ28871063 hydrochloride
|
EGFR
|
Cancer
|
|
JNJ28871063 hydrochloride is an orally active, highly selective and ATP competitive pan-ErbB kinase inhibitor with IC50 values of 22 nM, 38 nM, and 21 nM for ErbB1, ErbB2, and ErbB4, respectively. JNJ28871063 hydrochloride inhibits phosphorylation of functionally important tyrosine residues in both EGFR and ErbB2. JNJ28871063 hydrochloride crosses the blood-brain barrier and has antitumor activity in human tumor xenograft models that overexpress EGFR and ErbB2.
|
-
- HY-147056
-
|
PKRA83
PKRA7
|
Others
|
Cancer
|
|
PKRA83 (PKRA7) is a potent prokineticin (PK2) antagonist, which can compete for the binding of PK2 to its receptors PKR1 and PKR2. PKRA83 potently inhibits PK2 receptors, with IC50 values of 5.0 nM and 8.2 nM for PKR1 and PKR2, respectively. PKRA83 has anticancer and anti-angiogenic activities. PKRA83 can penetrate the blood-brain barrier.
|
-
- HY-P0203A
-
|
α-CGRP, rat TFA
|
CGRP Receptor
|
Metabolic Disease
Inflammation/Immunology
Cardiovascular Disease
|
|
α-CGRP, rat TFA, a neuropeptide (calcitonin gene-related peptide (CGRP)) mainly expressed in neuromuscular junction, is a potent vasodilator. α-CGRP, rat TFA can lead to a fall in blood pressure and an increase in heart rate by peripheral administration, also relax colonie smooth muscle. α-CGRP, rat TFA has the potential in cardiovascular, pro-inflammatory, migraine and metabolic studies.
|
-
- HY-101855
-
|
Emrusolmin
Anle138b
|
Amyloid-β
|
Neurological Disease
|
|
Emrusolmin (Anle138b), an oligomeric aggregation inhibitor, blocks the formation of pathological aggregates of prion protein (PrPSc) and of α-synuclein (α-syn). Emrusolmin strongly inhibits oligomer accumulation, neuronal degeneration, and disease progression in vivo. Emrusolmin has low toxicity and an excellent oral bioavailability and blood-brain-barrier penetration. Emrusolmin blocks Aβ channels and rescues disease phenotypes in a mouse model for amyloid pathology.
|
-
- HY-125469
-
|
ICA-105665
PF-04895162
|
Potassium Channel
|
Neurological Disease
|
|
ICA-105665 (PF-04895162) is a potent and orally active neuronal Kv7.2/7.3 and Kv7.3/7.5 potassium channels opener. ICA-105665 inhibits liver mitochondrial function and bile salt export protein (BSEP) transport (IC50 of 311 μM). ICA-105665 can penetrate the blood-brain barrier and has antiseizure effects.
|
-
- HY-150720
-
|
TYK2-IN-12
|
JAK
IFNAR
|
Inflammation/Immunology
|
|
TYK2-IN-12 (compound 30) is an orally active, potent and selective TYK2 (tyrosine kinase 2) inhibitor, with a Ki of 0.51 nM. TYK2-IN-12 inhibits IL-12 induced IFNγ, with IC50 values of 2.7 and 7.0 μM in human and mouse whole blood, respectively. TYK2-IN-12 can be used for psoriasis research.
|
-
- HY-100604
-
|
JNJ-40418677
|
γ-secretase
Amyloid-β
|
Neurological Disease
|
|
JNJ-40418677 is an orally active modulator of γ-secretase, can cross the blood-brain barrier. JNJ-40418677 inhibits Aβ42 and NS2B-NS3 protease, with IC50s of 200 nM and 3.9 μM, respectively. JNJ-40418677 displays good biological tolerance, can be use for Alzheimer’s disease research.
|
-
- HY-13240
-
|
LY2886721
|
Beta-secretase
|
Neurological Disease
|
|
LY2886721 is a potent, selective and orally active beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 20.3 nM for recombinant human BACE1. LY2886721 is selectivity against cathepsin D, pepsin, and renin, but lacking selectivity against BACE2 (IC50 of 10.2 nM). LY2886721 can across blood-brain barrier and has the potential for Alzheimer's disease treatment.
|
-
- HY-B0228S9
-
|
Adenosine-13C10,15N5
|
Apoptosis
Nucleoside Antimetabolite/Analog
Autophagy
Endogenous Metabolite
|
|
|
Adenosine- 13C10, 15N5 is the 13C and 15N labeled Adenosine[1]. Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physiology, including neuronal activity, vascular function, platelet aggregation, and blood cell regulation[2][3].
|
-
- HY-16785
-
|
Veledimex
INXN-1001; RG-115932
|
Interleukin Related
|
Cancer
Inflammation/Immunology
|
|
Veledimex (INXN-1001), a synthetic analog of the insect molting hormone ecdysone, is an orally active activator ligand for a proprietary gene therapy promoter system. Veledimex can be used to activate certain genes using the ecdysone receptor (EcR)-based inducible gene regulation system, the RheoSwitch Therapeutic System (RTS). Veledimex can cross blood-brain barrier (BBB) in both orthotopic GL-261 mice and cynomolgus monkeys.
|
-
- HY-B1075AS
-
|
(Rac)-Fosfomycin (benzylamine)-13C3
MK-0955 (benzylamine)-13C3
|
Bacterial
Antibiotic
|
Infection
|
|
(Rac)-Fosfomycin (benzylamine)- 13C3 is the 13C labeled Fosfomycin[1]. Fosfomycin (MK-0955) is a broad-spectrum antibiotic. Fosfomycin can cross blood-brain barrier penetrating, and irreversibly inhibits an early stage in cell wall synthesis. Fosfomycin shows anti-bacteria activity for a range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria[2][3].
|
-
- HY-152671
-
|
hMAO-B-IN-4
|
Monoamine Oxidase
|
Neurological Disease
|
|
hMAO-B-IN-4 (compound B10) is a selective, reversible and blood–brain barrier (BBB) penetrable human monoamine oxidase-B (hMAO-B) inhibitor with an IC50 value and a Ki value of 0.067 and 0.03 μM, respectively. hMAO-B-IN-4 inhibits hMAO-A with an IC50 value of 33.82 μM. hMAO-B-IN-4 can be used for Alzheimer’s disease (AD) and Parkinson’s disease (PD) research.
|
-
- HY-P1122
-
|
Cyclosporin H
|
Formyl Peptide Receptor (FPR)
|
Infection
Inflammation/Immunology
|
|
Cyclosporin H is a selective and potent inhibitor of FPR-1 (formyl peptide receptor 1). Cyclosporin H, a viral transduction enhancer, increases lentiviral transduction up to 10-fold in human cord blood-derived hematopoietic stem and progenitor cells (HSPCs). Cyclosporin H displays an additive effect when combined with Rapamycin (HY-10219) or Prostaglandin E2 (HY-101952). Cyclosporin H lacks immunosuppressant activity of Cyclosporin A.
|
-
- HY-17368S1
-
|
(rac)-Rivastigmine-d6
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
(rac)-Rivastigmine-d6 is a labelled racemic Rivastigmine. Rivastigmine (S-Rivastigmine) is an orally active and potent cholinesterase (ChE) inhibitor and inhibits butyrylcholinesterase (BChE) and acetylcholinesteras (AChE) with IC50s of 0.037 μM , 4.15 μM, respectively. Rivastigmine can pass the blood brain barrier (BBB). Rivastigmine is a parasympathomimetic or cholinergic agent used for the research of mild to moderate dementia of the Alzheimer's type and dementia due to Parkinson's disease[1][2].
|
-
- HY-152026
-
|
NADPH oxidase-IN-1
|
NADPH Oxidase
|
Neurological Disease
|
|
NADPH oxidase-IN-1 is an orally active NADPH oxidase (Nox) inhibitor, related with neuronal inflammation. NADPH oxidase-IN-1 can cross the blood-brain barrier (BBB), inhibits Nox2 and Nox4 with IC50s of 1.9 μM and 2.47 μM, respectively. NADPH oxidase-IN-1 suppresses pro-inflammatory cytokines production and LPS-mediated microglial migration, also has in vivo efficacy.
|
-
- HY-Y0271S2
-
|
Urea-13C,15N2
|
Endogenous Metabolite
|
|
|
Urea- 13C, 15N2 is the 13C and 15N labeled Urea[1]. Urea is a powerful protein denaturant via both direct and indirect mechanisms[1]. A potent emollient and keratolytic agent[2]. Used as a diuretic agent. Blood urea nitrogen (BUN) has been utilized to evaluate renal function[3]. Widely used in fertilizers as a source of nitrogen and is an important raw material for the chemical industry.
|
-
- HY-14327
-
|
FAUC 213
|
Dopamine Receptor
|
Neurological Disease
|
|
FAUC 213 is an orally active and highly selective dopamine D4 receptor complete antagonist with a Ki of 2.2 nM for hD4.4. FAUC 213 has less activity on D2 and D3 receptors (Kis of 3.4 μM, 5.3 μM for hD2, hD3, respectively). FAUC 213 can cross the blood-brain barrier (BBB). FAUC 213 exhibits atypical antipsychotic characteristic.
|
-
- HY-B2163
-
|
Astaxanthin
|
PPAR
Reactive Oxygen Species
STAT
NF-κB
Apoptosis
|
Cancer
Metabolic Disease
Cardiovascular Disease
|
|
Astaxanthin, the red dietary carotenoid, is an orally effective and potent antioxidant. Astaxanthin inhibits NF-κB and down-regulates VEGF in blood glucose. Astaxanthin exerts anti-cancer cell proliferation, increases apoptosis, impairs migration and invasion by activating PPARγ and reducing the expression of STAT3. Astaxanthin also has neuroprotective and anti-inflammatory activity and can be used in studies of cancer, diabetic retinopathy, cardiovascular disease, and in the coloring of animal feed.
|
-
- HY-146351
-
|
HDAC-IN-38
|
HDAC
|
Neurological Disease
|
|
HDAC-IN-38 (compound 13) is a potent HDAC inhibitor. HDAC-IN-38 shows similar micro-molar inhibitory activity toward HDAC1, 2, 3, 5, 6, and 8. HDAC-IN-38 increases cerebral blood flow (CBF), attenuates cognitive impairment, and improves hippocampal atrophy. HDAC-IN-38 also increases the level of histone acetylation (H3K14 or H4K5).
|
-
- HY-E70047
-
|
alpha-1,4-Galactosyltransferase (LgtC)
A4GALT
|
Endogenous Metabolite
|
Metabolic Disease
|
|
alpha-1,4-Galactosyltransferase (LgtC) (A4GALT) is a glycosphingolipid-specific glycosyltransferase. alpha-1,4-Galactosyltransferase (LgtC) transfers a galactose to the alpha-1,4 position of lactosylceramide to form globotriaosylceramide. alpha-1,4-Galactosyltransferase (LgtC) can be used for the synthesis of P1 blood group antigens.
|
-
- HY-17366A
-
|
Clozapine N-oxide dihydrochloride
|
mAChR
Dopamine Receptor
Drug Metabolite
|
Neurological Disease
|
|
Clozapine N-oxide dihydrochloride is a major metabolite of Clozapine and a human muscarinic designer receptors (DREADDs) agonist. Clozapine N-oxide dihydrochloride activates the DREADD receptor hM3Dq and hM4Di. Clozapine N-oxide dihydrochloride can cross the blood-brain barrier. Clozapine is a potent dopamine antagonist and also a potent and selective muscarinic M4 receptor (EC50=11 nM) agonist.
|
-
- HY-152142
-
|
DN-1289
|
JNK
|
Neurological Disease
|
|
DN-1289 is an orally active and selective inhibitor of dual leucine zipper kinase (DLK; IC50=17 nM) and leucine zipper-bearing kinase (LZK; IC50=40 nM). DN-1289 results significant attenuation of optic nerve crush (ONC)-induced p-c-Jun in mice model. DN-1289 has excellent in vivo plasma half-life and blood-brain barrier permeability.
|
-
- HY-17366
-
|
Clozapine N-oxide
|
mAChR
Dopamine Receptor
Drug Metabolite
|
Neurological Disease
|
|
Clozapine N-oxide is a major metabolite of Clozapine and a human muscarinic designer receptors (DREADDs) agonist. Clozapine N-oxide activates the DREADD receptor hM3Dq and hM4Di. Clozapine N-oxide can cross the blood-brain barrier. Clozapine is a potent dopamine antagonist and also a potent and selective muscarinic M4 receptor (EC50=11 nM) agonist.
|
-
- HY-135382
-
|
PROTAC IRAK4 degrader-2
|
PROTACs
IRAK
|
Cancer
Inflammation/Immunology
|
|
PROTAC IRAK4 degrader-2 (Compound 9) is a PROTAC-based IRAK4 degrader that affords potent IRAK4 degradation with a DC50 in peripheral blood mononuclear cells (PBMCs) cells of 151 nM. PROTAC IRAK4 degrader-2 induce a reduction of IRAK4 protein levels with a DC50 of 36 nM in PBMC cells. PROTAC IRAK4 degrader-2 also leads to the inhibition of multiple cytokines in PBMCs.
|
-
- HY-151444
-
|
LRRK2-IN-6
|
LRRK2
|
Neurological Disease
|
|
LRRK2-IN-6 (compound 22) is a potent, orally active, selective leucine rich repeat protein kinase 2 gene (LRRK2) inhibitor with IC50 values of 4.6 and 49 μM for GS LRRK2 and WT LRRK2, respectively. LRRK2-IN-6 inhibits LRRK2 Ser1292 and Ser925 autophosphorylation. LRRK2-IN-6 can cross the blood-brain barrier.
|
-
- HY-151441
-
|
LRRK2-IN-5
|
LRRK2
|
Neurological Disease
|
|
LRRK2-IN-5 (compound 25) is a potent, orally active, selective leucine rich repeat protein kinase 2 gene (LRRK2) inhibitor with IC50 values of 1.2 and 16 μM for GS LRRK2 and WT LRRK2, respectively. LRRK2-IN-5 inhibits LRRK2 Ser1292 and Ser925 autophosphorylation. LRRK2-IN-5 can cross the blood-brain barrier.
|
-
- HY-W008947
-
|
SEW2871
|
LPL Receptor
ERK
Akt
|
Metabolic Disease
Inflammation/Immunology
Neurological Disease
|
|
SEW2871 is an orally active, potent, highly selective S1P1 (sphingosine-1-phosphate type 1 receptor) agonist, with an EC50 of 13.8 nM. SEW2871 activates ERK, Akt, and Rac signaling pathways and induces S1P1 internalization and recycling. SEW2871 reduces lymphocyte numbers in blood. SEW2871 can be used for the research of diabetes, Alzheimer’s disease, liver fibrosis, and inflammatory responses.
|
-
- HY-15978
-
|
P7C3-A20
|
Others
|
Neurological Disease
|
|
P7C3-A20 is a derivative of P7C3 with potent proneurogenic and neuroprotective activity. P7C3-A20 exerts an antidepressant-like effect. P7C3-A20 can cross the blood-brain barrier and therefore has the potential for brain injury treatment.
|
-
- HY-106224B
-
|
Orexin A (human, rat, mouse) (acetate)
Hypocretin-1 (human, rat, mouse) (acetate)
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
Orexin A (Hypocretin-1) (human, rat, mouse) acetate is a hypothalamic neuropeptide with analgesic properties (crosses the blood-brain barrier). Orexin A (human, rat, mouse) acetate is also an OX1R agonist that induces the expression of BDNF and TH proteins in SH-SY5Y cells in a time- and dose-dependent manner. Orexin A (human, rat, mouse) acetate can be used in studies of appetite regulation, neurodegenerative diseases and modulation of injurious messaging.
|
-
- HY-B0683S
-
|
Limaprost-d3
|
PGE synthase
|
Inflammation/Immunology
Cardiovascular Disease
|
|
Limaprost-d3 (17α,20-dimethyl-δ2-PGE1-d3) is the deuterium labeled Limaprost. Limaprost (OP1206) is a PGE1 analogue and a potent and orally active vasodilator. Limaprost increases blood flow and inhibits platelet aggregation. Limaprost pain relief, has antianginal effects, and can be used for ischaemic symptoms research[1][2].
|
-
- HY-125881
-
|
ASP1126
|
LPL Receptor
|
Inflammation/Immunology
|
|
ASP1126 is a selective and orally active sphingosine-1-phosphate (S1P) agonist, with EC50 values of 7.12 nM, 517 nM for hS1P1 and hS1P3, respectively. ASP1126 decreases the number of peripheral lymphocytes, naive T cells, central memory T cells and effector memory T cells in the peripheral blood. ASP1126 has the potential to be applied in clinical transplantation with improved safety profile.
|
-
- HY-18555
-
|
TMPA
|
AMPK
|
Cancer
Metabolic Disease
Inflammation/Immunology
|
|
TMPA is a high-affinity Nur77 antagonist that binds to Nur77 leading to the release and shuttling of LKB1 in the cytoplasm to activate AMPKα. TMPA effectively lowers blood glucose and attenuates insulin resistance in type II db/db, high-fat diet and streptozotocin-induced diabetic mice. TMPA reduces RICD (restimulation-induced cell death) in human T cells, can also be used in studies of cancer and T-cell apoptosis dysregulation.
|
-
- HY-B1126S
-
|
Orphenadrine-d3 hydrochloride
|
iGluR
|
Neurological Disease
|
|
Orphenadrine-d3 (hydrochloride) is the deuterium labeled Orphenadrine hydrochloride[1]. Orphenadrine hydrochloride is an orally active and non-competitive NMDA receptor antagonist (crosses the blood-brain barrier) with a Ki of 6.0 μM. Orphenadrine hydrochloride relieves stiffness, pain and discomfort due to muscle strains, sprains or other injuries. Orphenadrine hydrochloride is also used to relieve tremors associated with parkinson's disease. Orphenadrine citrate has good neuroprotective properties, can be used in studies of neurodegenerative diseases[2][3].
|
-
- HY-144825
-
|
Chol-CTPP
|
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
Chol-CTPP is a ligand with dual targeting effect on blood-brain barrier (BBB) and glioma cells. Lip-CTPP can be gained by Chol-CTPP and another mitochondria targeting ligand (Chol-TPP). Lip-CTPP is a promising potential carrier to exert the anti-glioma effect of doxorubicin (DOX) and lonidamine (LND) collaboratively. Lip-CTPP elevates the inhibition rate of tumor cell proliferation, migration and invasion, promote apoptosis and necrosis, and interfere with mitochondrial function.
|
-
- HY-107732
-
|
JNJ-5207787
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
JNJ-5207787 is a nonpeptidic, selective and penetrate the blood-brain barrier neuropeptide Y Y2 receptor (Y2) antagonist. JNJ-5207787 inhibits the binding of peptide YY (PYY) with pIC50s of 7.0 and 7.1 for human Y2 receptor and rat Y2 receptor, respectively. JNJ-5207787 is >100-fold selective versus human Y1, Y4, and Y5 receptors.
|
-
- HY-148502
-
|
VU6019650
|
mAChR
|
Neurological Disease
|
|
VU6019650 is a potent and selective orthosteric antagonist of M5 mAChR (IC50=36 nM), can be used for opioid use disorder (OUD) relief. VU6019650 can cross blood brain barrier, potentially modulates the mesolimbic dopaminergic reward circuitry. VU6019650 blocks Oxotremorine M iodide (HY-101372A) induced increases of neuronal firing rates of midbrain dopamine neurons in the ventral tegmental area (VTA).
|
-
- HY-147327
-
|
N-Formylsarcolysine
|
Others
|
Cancer
|
|
N-Formylsarcolysine has antitumor activity, and inhibits leukemia by increasing the Hb and erythrocyte levels and decreasing the number of leukocytes. N-Formylsarcolysine also involves in glioblastoma and other diseases research.
|
-
- HY-17355S
-
|
Pramipexole-d7 dihydrochloride
|
Dopamine Receptor
|
Neurological Disease
|
|
Pramipexole-d7 (dihydrochloride) is the deuterium labeled Pramipexole dihydrochloride. Pramipexole dihydrochloride is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole dihydrochloride can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS)[1][2][3].
|
-
- HY-146398
-
|
AMPK activator 6
|
AMPK
|
Metabolic Disease
|
|
AMPK activator 6 (Compound GC) reduces lipid content and activates the AMPK pathway in HepG2 and 3T3-L1 cells. AMPK activator 6 significantly suppresses the increase in triglyceride (TG) , total cholesterol (TC), low-density lipoprotein-C (LDL-C), and other biochemical indices in blood serum. AMPK activator 6 can be used for the research of non-alcoholic fatty liver disease (NAFLD) and metabolic syndrome.
|
-
- HY-B0410S1
-
|
Pramipexole-d5
|
Dopamine Receptor
|
Neurological Disease
|
|
Pramipexole-d5 is the deuterium labeled Pramipexole[1]. Pramipexole is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS)[2][3][4].
|
-
- HY-146468
-
-
- HY-15425
-
|
PF-543
Sphingosine Kinase 1 Inhibitor II
|
SphK
LPL Receptor
Apoptosis
Autophagy
|
Cancer
Inflammation/Immunology
Cardiovascular Disease
|
|
PF-543 (Sphingosine Kinase 1 Inhibitor II) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM. PF-543 is >100-fold selectivity for SPHK1 over SPHK2. PF-543 is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 induces apoptosis, necrosis, and autophagy.
|
-
- HY-15425B
-
|
PF-543 hydrochloride
Sphingosine Kinase 1 Inhibitor II hydrochloride
|
SphK
LPL Receptor
Apoptosis
Autophagy
|
Cancer
Inflammation/Immunology
Cardiovascular Disease
|
|
PF-543 hydrochloride (Sphingosine Kinase 1 Inhibitor II hydrochloride) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM. PF-543 hydrochloride is >100-fold selectivity for SPHK1 over SPHK2. PF-543 hydrochloride is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 hydrochloride induces apoptosis, necrosis, and autophagy.
|
-
- HY-121618
-
|
α-Thujone
|
GABA Receptor
Reactive Oxygen Species
Parasite
Apoptosis
Autophagy
|
Cancer
Infection
Neurological Disease
|
|
α-Thujone is a monoterpene isolated from Thuja occidentalis essential oil with potent anti-tumor activities. α-Thujone is a reversible modulator of the GABA type A receptor and the IC50 for α-Thujone is 21 μM in suppressing the GABA-induced currents. α-Thujone induces ROS accumulation-dependent cytotoxicity, also induces cell apoptosis and autophagy. α-Thujone has antinociceptive, insecticidal, and anthelmintic activity, and easily penetrates the blood-brain barrier.
|
-
- HY-17355S1
-
|
Pramipexole-d5 dihydrochloride
|
Dopamine Receptor
|
Neurological Disease
|
|
Pramipexole-d5 (dihydrochloride) is deuterium labeled Pramipexole (dihydrochloride). Pramipexole dihydrochloride is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole dihydrochloride can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS)[1][2][3].
|
-
- HY-N3807
-
|
Enniatin B1
|
Acyltransferase
ERK
NF-κB
|
Cancer
Infection
Cardiovascular Disease
|
|
Enniatin B1 is a Fusarium mycotoxin. Enniatin B1 inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 73 μM in an enzyme assay using rat liver microsomes. Enniatin B1 crosss the blood-brain barrier. Enniatin B1 decreases the activation of ERK (p44/p42). Enniatin B1 inhibits moderately TNF-α-induced NF-κB activation.
|
-
- HY-146725
-
|
FBPase-IN-1
|
FBPase
|
Metabolic Disease
|
|
FBPase-IN-1 is a potent FBPase (Fructose-1,6-bisphosphatase) inhibitor for Type 2 diabetes (T2D) study with an IC50 of 0.22 μM. FBPase-IN-1 can reduce blood glucose levels and ameliorate glucose tolerance. FBPase-IN-1 modifies the C128 site, regulates the N125-S124-S123 allosteric pathway of FBPase and affects the catalytic activity of FBPase.
|
-
- HY-B0688S2
-
|
Dapsone-13C12
4,4′-Diaminodiphenyl sulfone-13C12; DDS-13C12
|
Isotope-Labeled Compounds
Antibiotic
Parasite
Bacterial
Reactive Oxygen Species
|
Infection
Inflammation/Immunology
|
|
Dapsone- 13C12 is the 13C12 labeled Dapsone (HY-B0688). Dapsone (4,4′-Diaminodiphenyl sulfone) is an orally active and blood-brain penetrant sulfonamide antibiotic with bacteriostatic, antimycobacterial and antiprotozoal activities. Dapsone exerts effective antileprosy activity and inhibits folate synthesis in cell extracts of M. leprae. Dapsone is used for dermatologic disorder research, including leprosy, dermatitis herpetiformis, acne vulgaris et al.
|
-
- HY-12170
-
|
Prinomastat
AG3340; KB-R9896
|
MMP
Apoptosis
|
Cancer
|
|
Prinomastat (AG3340) is a broad spectrum, potent, orally active metalloproteinase (MMP) inhibitor with IC50s of 79, 6.3 and 5.0 nM for MMP-1, MMP-3 and MMP-9, respectively. Prinomastat inhibits MMP-2, MMP-3 and MMP-9 with Kis of 0.05 nM, 0.3 nM and 0.26 nM, respectively. Prinomastat crosses blood-brain barrier. Antitumor avtivity.
|
-
- HY-18862
-
|
PF-03715455
|
p38 MAPK
|
Inflammation/Immunology
|
|
PF-03715455 is a potent inhaled p38 MAPK inhibitor. PF-03715455 shows some selectivity for p38α over p38β with respective IC50 values of 0.88 and 23 nM. PF-03715455 potently inhibits LPS-induced TNFα production in human whole blood (IC50=1.7 nM). PF-03715455 has potential for the treatment of COPD (chronic obstructive pulmonary disease).
|
-
- HY-124569
-
|
NAB-14
|
iGluR
|
Neurological Disease
|
|
NAB-14 is a potent, selective, orally active and non-competitive GluN2C/2D antagonists with an IC50 of 580 nM for GluN1/GluN2D. NAB-14 shows >800-fold selective for recombinant GluN2C and GluN2D over GluN2A and GluN2B. NAB-14 can cross the blood-brain-barrier.
|
-
- HY-144765
-
|
NF-κB-IN-4
|
NF-κB
Apoptosis
|
Inflammation/Immunology
Neurological Disease
|
|
NF-κB-IN-4 (compound 17) is a potent and BBB-penetrated NF-κB pathway inhibitor with blood brain barrier (BBB) permeability. NF-κB-IN-4 exhibits potential anti-neuroinflammatory activity with low toxicity. NF-κB-IN-4 can block the activation and phosphorylation of IκBα, reduce expression of NLRP3, and thus inhibit NF-κB activation. NF-κB-IN-4 can be used for neuroinflammation related diseases research.
|
-
- HY-115925
-
|
SHP2-IN-9
|
SHP2
Phosphatase
|
Cancer
|
|
SHP2-IN-9 is a specific SHP2 inhibitor (IC50 =1.174 μM) with enhanced blood–brain barrier penetration. SHP2-IN-9 shows 85-fold more selective for SHP2 than SHP1. SHP2-IN-9 inhibits SHP2-mediated cell signal transduction and cancer cell proliferation, and inhibits the growth of cervix cancer tumors and glioblastoma growth in vivo.
|
-
- HY-12170A
-
|
Prinomastat hydrochloride
AG3340 hydrochloride; KB-R9896 hydrochloride
|
MMP
Apoptosis
|
Cancer
|
|
Prinomastat hydrochloride (AG3340 hydrochloride) is a broad spectrum, potent, orally active metalloproteinase (MMP) inhibitor with IC50s of 79, 6.3 and 5.0 nM for MMP-1, MMP-3 and MMP-9, respectively. Prinomastat hydrochloride inhibits MMP-2, MMP-3 and MMP-9 with Kis of 0.05 nM, 0.3 nM and 0.26 nM, respectively. Prinomastat hydrochloride can cross blood-brain barrier. Antitumor avtivity.
|
-
- HY-111640
-
|
3'-Azido-3'-deoxy-5-methylcytidine
|
HIV
Reverse Transcriptase
|
Infection
|
|
3'-Azido-3'-deoxy-5-methylcytidine (CS-92) is a potent xenotropic murine leukemia-related retrovirus (XMRV) inhibitor with a CC50 of 43.5 μM in MCF-7 cells. 3'-Azido-3'-deoxy-5-methylcytidine also inhibits HIV-1 reverse transcriptase with an EC50 of 0.06 μM in peripheral blood mononuclear (PBM) cells.
|
-
- HY-152148
-
|
JZP-MA-11
|
MAGL
|
Neurological Disease
|
|
JZP-MA-11 is a positron emission tomography (PET) ligand targeting the endocannabinoid α/β-hydrolase domain 6 (ABHD6) enzyme. JZP-MA-11 selectively inhibits ABHD6 with an IC50 value of 126 nM. JZP-MA-11 can cross the blood-brain barrier (BBB). [18F]JZP-MA-11 has the potential for preclinical evaluation targeting the brain ABHD6 in mice and nonhuman primate (NHP).
|
-
- HY-10046
-
|
Plerixafor
AMD 3100; JM3100; SID791
|
CXCR
HIV
|
Cancer
Infection
Endocrinology
Inflammation/Immunology
|
|
Plerixafor (AMD 3100) is a selective CXCR4 antagonist with an IC50 of 44 nM. Plerixafor, an immunostimulant and a hematopoietic stem cell (HSC) mobilizer, is an allosteric agonist of CXCR7. Plerixafor inhibits HIV-1 and HIV-2 replication with an EC50 of 1-10 nM.
|
-
- HY-115983
-
|
DMUP
|
Apoptosis
|
Cancer
|
|
DMUP is a potent CD47-SIRPα axis inhibitor. DMUP induces apoptosis and increases the macrophage phagocytosis in A549 cells. DMUP decreases the expression of CD47 and SIRPα protein. DMUP shows antitumor activity.
|
-
- HY-150096
-
-
- HY-P99167
-
|
Lucatumumab
HCD122
|
TNF Receptor
|
Cancer
|
|
Lucatumumab (HCD122) is a fully human anti-CD40 antagonist monoclonal antibody, which blocks CD40/CD40L-mediated signaling. Lucatumumab efficiently mediates antibody-dependent cell-mediated cytotoxicity (ADCC) and clearance of tumor cells, can be used for refractory lymphomas, CLL and multiple myeloma research.
|
-
- HY-B0263S
-
-
- HY-141899
-
|
MK-6884
|
mAChR
|
Neurological Disease
|
|
MK-6884 is a M4 muscarinic receptor positive allosteric modulator (PAM) with a Ki value of 0.19 nM. MK-6884 can be used for the research of the neurodegenerative diseases. MK-6884 can be conveniently radiolabeled with carbon-11 and as a positron emission tomography (PET) imaging agent.
|
-
- HY-N4314
-
|
Scutellarein tetramethyl ether
4',5,6,7-Tetramethoxyflavone
|
Bacterial
|
Infection
Inflammation/Immunology
|
|
Scutellarein tetramethyl ether (4',5,6,7-Tetramethoxyflavone) is a bioactive component of Siam weed extract. Scutellarein tetramethyl ether (4',5,6,7-Tetramethoxyflavone) exhibits anti-inflammatory activity through NF-κB pathway. Scutellarein tetramethyl ether (4',5,6,7-Tetramethoxyflavone) modulats of bacterial agent resistance via efflux pump inhibition. Scutellarein tetramethyl ether (4',5,6,7-Tetramethoxyflavone) can enhance blood coagulation.
|
-
- HY-D0958
-
|
Methylene blue hydrate
Basic Blue 9 hydrate; CI-52015 hydrate; Methylthioninium chloride hydrate
|
Guanylate Cyclase
Monoamine Oxidase
NO Synthase
Microtubule/Tubulin
|
Cancer
Infection
Inflammation/Immunology
|
|
Methylene blue (Basic Blue 9) hydrate is a guanylyl cyclase (sGC), monoamine oxidase A (MAO-A) and NO synthase (NOS) inhibitor. Methylene blue is a vasopressor and is often used as a dye in several medical procedures. Methylene blue hydrate through the nitric oxide syntase/guanylate cyclase signalling pathway to reduce prepulse inhibition. Methylene blue hydrate is a REDOX cycling compound and able to cross the blood-brain barrier. Methylene blue hydrate is a Tau aggregation inhibitor. Methylene blue hydrate reduces cerebral edema, attenuated microglial activation and reduced neuroinflammation.
|
-
- HY-153369
-
|
BAY-747
|
Guanylate Cyclase
|
Neurological Disease
Cardiovascular Disease
|
|
BAY-747 is an orally active and brain-penetrant stimulator of soluble guanylate cyclase (sGC). BAY-747 reverses L-NAME induced memory impairments and enhances cognition of rats in the object location task (OLT). BAY-747 also decreases blood pressure in both conscious normotensive and spontaneously hypertensive rats (SHR). BAY-747 improves function of the skeletal muscle associated with Duchenne muscular dystrophy (DMD) in mdx/mTRG2 mice model.
|
-
- HY-110155
-
|
LM11A-31 dihydrochloride
|
Neurotensin Receptor
|
Neurological Disease
|
|
LM11A-31 dihydrochloride, a non-peptide p75 NTR (neurotrophin receptor p75) modulator, is an orally active and potent proNGF (nerve growth factor) antagonist. LM11A-31 dihydrochloride is an amino acid derivative with high blood-brain barrier permeability and blocks p75-mediated cell death. M11A-31 dihydrochloride reverses cholinergic neurite dystrophy in Alzheimer's disease mouse models with mid- to late-stage disease progression.
|
-
- HY-106784A
-
|
(E)-Ajoene
|
Others
|
Neurological Disease
|
|
(E)-Ajoene is a oxygenated ajoene and organosulfur compound, which can be acquired via allicin decomposing. The polysulfides from garlic can be converted by human red blood cells into hydrogen sulfide (H2S) and allyl glutathione. (E)-Ajoene has been proved to show neuroprotective effects against ischemic damage. (E)-Ajoene is orally active to inhibit lipid peroxidation. (E)-Ajoene increases the number of cresyl violet-positive neurons and decreases the number of reactive gliosis in the CA1 region.
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- HY-15196
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TAK-285
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EGFR
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Cancer
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TAK-285 is a potent, selective, ATP-competitive and orally active HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, respectively. TAK-285 is >10-fold selectivity for HER1/2 than HER4, and less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc. TAK-285 has effective antitumor activity. TAK-285 can cross the blood-brain barrier (BBB).
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- HY-149211
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AChE/BChE-IN-12
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Cholinesterase (ChE)
Beta-secretase
Amyloid-β
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Neurological Disease
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AChE/BChE-IN-12 (compound 10b), a 3,5-dimethoxy analogue, is a potent AChE, BChE, and β-secretase-1 (BACE-1) inhibitor, with IC50 values of 2.57, 3.26, and 10.65 μM, respectively. AChE/BChE-IN-12 crosses the blood-brain barrier via passive diffusion and inhibits the self-aggregation of amyloid-β monomers. AChE/BChE-IN-12 can be used for Alzheimer’s disease (AD) research.
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- HY-17355S2
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Pramipexole-d7-1 dihydrochloride
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Dopamine Receptor
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Neurological Disease
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Pramipexole-d7-1 (dihydrochloride) is the deuterium labeled Pramipexole dihydrochloride[1]. Pramipexole dihydrochloride is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole dihydrochloride can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS)[2][3][4].
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- HY-147939
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AChE/BuChE-IN-3
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Cholinesterase (ChE)
Amyloid-β
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Cancer
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AChE/BuChE-IN-3 is a potent and blood-brain barrier (BBB) penetrant AChE and BuChE dual inhibitor with IC50s of 0.65 μM and 5.77 μM for AChE and BuChE. AChE/BuChE-IN-3 also inhibits Aβ1-42 aggregation. AChE/BuChE-IN-3 has effectively neuroprotective activities and nearly no toxicity on SH-SY5Y cells. AChE/BuChE-IN-3 can be used for researching Alzheimer's disease.
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- HY-15425A
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PF-543 Citrate
Sphingosine Kinase 1 Inhibitor II Citrate
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SphK
LPL Receptor
Apoptosis
Autophagy
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Cancer
Inflammation/Immunology
Cardiovascular Disease
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PF-543 Citrate (Sphingosine Kinase 1 Inhibitor II Citrate) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM. PF-543 Citrate is >100-fold selectivity for SPHK1 over SPHK2. PF-543 Citrate is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 Citrate induces apoptosis, necrosis, and autophagy.
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- HY-13750
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- HY-120475A
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