Search Result
Results for "
peripheral selectivity
" in MedChemExpress (MCE) Product Catalog:
2
Biochemical Assay Reagents
30
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-B0468
-
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Isoproterenol hydrochloride
|
Adrenergic Receptor
Endogenous Metabolite
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Cardiovascular Disease
Endocrinology
|
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Isoprenaline (Isoproterenol) hydrochloride is a non-selective, orally active β-adrenergic receptor agonist. Isoprenaline has potent peripheral vasodilator, bronchodilator, and cardiac stimulating activities. Isoprenaline can be used for the research of bradycardia and bronchial asthma .
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- HY-17043
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- HY-B0233
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PN 200-110
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Calcium Channel
Autophagy
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Cardiovascular Disease
Neurological Disease
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Isradipine (PN 200-110) is an orally active and blood-brain barrier permeability L-type calcium channel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease .
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- HY-B0311
-
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(S)-(-)-Carbidopa
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Aryl Hydrocarbon Receptor
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Neurological Disease
Cancer
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Carbidopa ((S)-(-)-Carbidopa), a peripheral decarboxylase inhibitor, can be used for the research of Parkinson's disease. Carbidopa is a selective aryl hydrocarbon receptor (AhR) modulator. Carbidopa inhibits pancreatic cancer cell and tumor growth .
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- HY-13331
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Cortexolone 17 alpha-propionate; Cortexolone 17α-propionate; CB-03-01
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Androgen Receptor
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Endocrinology
|
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Clascoterone (Cortexolone 17 alpha-propionate;Cortexolone 17α-propionate;CB-03-01) is a new topical and peripherally selective androgen antagonist.
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- HY-103210
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Neurotoxin DSP 4 hydrochloride
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Adrenergic Receptor
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Neurological Disease
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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 .
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- HY-108353
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- HY-17609
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CR-845; FE-202845
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Opioid Receptor
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Neurological Disease
Inflammation/Immunology
|
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Difelikefalin (CR-845) is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease .
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- HY-101381
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AF-DX 116
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mAChR
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Neurological Disease
Metabolic Disease
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Otenzepad (AF-DX 116) is a selective and competitive M2 muscarinic acetylcholine receptor antagonist, with IC50 values of 640 nM and 386 nM for rabbit peripheral lung and rat heart, respectively .
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- HY-B0362A
-
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Phentolamine methanesulfonate
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Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
Cancer
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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 .
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- HY-107319
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- HY-B0311A
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(S)-(-)-Carbidopa monohydrate
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Aryl Hydrocarbon Receptor
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Neurological Disease
Cancer
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Carbidopa ((S)-(-)-Carbidopa) monohydrate, a peripheral decarboxylase inhibitor, can be used for the research of Parkinson's disease. Carbidopa monohydrate is a selective aryl hydrocarbon receptor (AhR) modulator. Carbidopa monohydrate inhibits pancreatic cancer cell and tumor growth .
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- HY-B0347
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|
Calcium Channel
Reactive Oxygen Species (ROS)
Caspase
Apoptosis
|
Cardiovascular Disease
|
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Lacidipine is an orally active and highly selective L-type calcium channel blocker that acts on smooth muscle calcium channels, primarily dilates peripheral arteries, reduces peripheral resistance, and has long-lasting anti-hypertensive activity. Lacidipine protects HKCs from apoptosis induced by ATP depletion and recovery by modulating the caspase-3 pathway. Lacidipine can be used in studies of hypertension, atherosclerosis and acute kidney injury (AKI) .
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- HY-111791
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HDAC
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Cancer
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ACY-1083 is a selective and brain-penetrating HDAC6 inhibitor with an IC50 of 3 nM and is 260-fold more selective for HDAC6 than all other classes of HDAC isoforms. ACY-1083 effectively reverses chemotherapy-induced peripheral neuropathy .
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- HY-157131
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TRP Channel
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Neurological Disease
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TRPV2-selective blocker 1 is a TRPV2-selective blocker that inhibits calcium influx and ionic currents. TRPV2-selective blocker 1 exhibits an IC50 of 6.3 μM against rat TRPV2, and shows no activity against TRPV1, TRPV3 or TRPV4 channels. TRPV2-selective blocker 1 attenuates macrophage phagocytosis, LPS-induced macrophage migration, and calcium microdomains generated by peripheral TRPV2. TRPV2-selective blocker 1 is non-cytotoxic and can be used to investigate the function of TRPV2 during immune processes .
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- HY-18977
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KML29
3 Publications Verification
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MAGL
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Metabolic Disease
Inflammation/Immunology
|
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KML29 is an extremely selective, orally active and irreversible MAGL inhibitor, with IC50 values of 15 nM, 43 nM and 5.9 nM for mouse, rat and human MAGL, respectively. KML29 exhibits minimal cross-reactivity toward other central and peripheral serine hydrolases, including no detectable activity against FAAH .
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- HY-101176
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Melatonin Receptor
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Cancer
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2-Iodomelatonin is a potent agonist of melatonin receptor 1 (MT1) with a Ki value of 28 pM, it is more 5-fold selective for MT1 over MT2 . 2-iodomelatonin can be used to identify, characterize and localize melatonin binding sites in the brain and peripheral tissues .
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- HY-101096
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MK-8998; CX-8998; JZP385
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Calcium Channel
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Neurological Disease
Cancer
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Suvecaltamide (MK-8998) is a selective T-type calcium channel inhibitor with oral efficacy. Suvecaltamide exhibits no cytotoxicity in myeloma cell lines and does not affect the antitumor efficacy of Bortezomib (BTZ). Suvecaltamide reverses BTZ-induced peripheral neuropathy (CIPN) in mouse and rat models, and helps inhibit myeloma growth .
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- HY-16100
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Fatty Acid Synthase (FASN)
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Metabolic Disease
Cancer
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BI 99179, a chemical probe, is a potent and selective type I fatty acid synthase (FAS) inhibitor with an IC50 of 79 nM. BI 99179 is a tool compound suitable for the in vivo validation of FAS as a target for lipid metabolism related diseases. BI 99179 exhibits significant exposure (both peripheral and central) upon oral administration in rats .
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- HY-100798
-
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GABA Receptor
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Neurological Disease
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Phaclofen is a selective GABAB receptor antagonist. Phaclofen is a peripheral and central baclofen antagonist. Phaclofen maybe a potential compound in determining the physiological significance of central and peripheral bicuculline-insensitive receptors with which GABA and (-)-baclofen interact .
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- HY-P3609
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CR 665
2 Publications Verification
JNJ 38488502; FE 200665
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Opioid Receptor
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Neurological Disease
|
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CR 665 (JNJ 38488502) is a peripherally selective κ-opioid agonist. CR 665 can activate the kappa opioid receptor with EC50 value of 10.9 nM. CR 665 can be used for the research of peripheral pain .
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- HY-107384A
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EMD-61753 hydrochloride
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Opioid Receptor
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Neurological Disease
Metabolic Disease
Inflammation/Immunology
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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) .
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- HY-173527
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Mitochondrial Metabolism
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Metabolic Disease
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PSSI-51 is an orally active, peripherally selective inhibitor of succinyl-CoA:3-ketoacid-CoA transferase (SCOT). PSSI-51 inhibits SCOT activity in peripheral tissues (such as muscle and kidney) but does not affect SCOT activity in brain tissue. PSSI-51 reduces ketone body oxidation by inhibiting SCOT, thereby improving obesity-related hyperglycemia. PSSI-51 can be used in the study of type 2 diabetes (T2D) and has the potential to improve obesity-related metabolic disorders .
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- HY-B1032
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(±)-Dropropizine; UCB-196
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Histamine Receptor
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Neurological Disease
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Dropropizine ((±)-Dropropizine; UCB-196) is an orally effective, peripherally selective antitussive that inhibits the activity of peripheral receptors and afferent nerves in the respiratory tract. Dropropizine acts on the cough reflex pathway, does not pass the blood-brain barrier, and has no central nervous system side effects. Dropropizine mainly regulates the level of sensory neuropeptides and inhibits the afferent signal transmission of the cough reflex, thereby alleviating the symptoms of dry cough, and has both mild local anesthetic and antihistamine activity. Dropropizine is mainly used for symptomatic research on dry cough caused by respiratory diseases .
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- HY-19721
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- HY-B0010B
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(±)Formoterol
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Adrenergic Receptor
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Inflammation/Immunology
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Formoterol ((±)Formoterol) is an orally active β2-selective agonist. Formoterol potently relaxes the peripheral airways through stimulating the beta 2-adrenoceptors selectively as is the case in the central airways and that it significantly inhibits IgE-mediated slow reactive substance of anaphylaxis (SRS-A) release through beta-adrenoceptor stimulation .
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- HY-B1298
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Adrenergic Receptor
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Neurological Disease
Endocrinology
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Methoxamine hydrochloride is a selective alpha1-adrenergic receptor agonist. Methoxamine hydrochloride causes vasoconstriction and increased peripheral vascular resistance . Methoxamine hydrochloride significantly increased the overflow of ATP, ADP and AMP, but not adenosine, by a prazosin-sensitive mechanism in the rabbit pulmonary artery .
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- HY-17043S1
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- HY-131879
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Sodium Channel
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Neurological Disease
|
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NS383 is a potent and uniquely selective inhibitor of rat ASICs containing 1a and/or 3 subunits. NS383 inhibits H(+)-activated currents recorded from rat homomeric ASIC1a, ASIC3, and heteromeric ASIC1a+3 with IC50 values ranging from 0.61 to 2.2 μM. NS383 is well tolerated and capable of reversing pathological painlike behaviors, presumably via peripheral actions, but possibly also via actions within central pain circuits .
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- HY-108229
-
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6β-Hydroxynaltrexone
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Drug Metabolite
Opioid Receptor
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Neurological Disease
|
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6β-Naltrexol (6β-Hydroxynaltrexone), the primary metabolite of Naltrexone, is a peripherally selective opioid antagonist. 6β-Naltrexol selectively inhibits gastrointestinal opioid effects in human subjects and inhibits Morphine-induced slowing of gastrointestinal transit .
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- HY-153963
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Oxytocin Receptor
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Endocrinology
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PF-06655075 is a novel andnon–brain-penetrant oxytocin receptor agonist with increased selectivity for the oxytocin receptor and significantly increased pharmacokinetic stability. PF-06655075 can be used as a tool compound to further explore the role of peripheral oxytocin in behavioral response .
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- HY-17043R
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- HY-108229S
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6β-Hydroxynaltrexone-d3
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Isotope-Labeled Compounds
Opioid Receptor
Drug Metabolite
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Neurological Disease
|
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6β-Naltrexol-d3 (6β-Hydroxynaltrexone-d3) is deuterium labeled 6β-Naltrexol. 6β-Naltrexol (6β-Hydroxynaltrexone), the primary metabolite of Naltrexone, is a peripherally selective opioid antagonist. 6β-Naltrexol selectively inhibits gastrointestinal opioid effects in human subjects and inhibits Morphine-induced slowing of gastrointestinal transit .
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- HY-155089
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MAP3K
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Neurological Disease
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IACS-52825 is a potent and selective DLK inhibitor with Kd of 1.3 nM, useful for the study of chemotherapy-induced peripheral neuropathy .
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- HY-14790
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(S,S)-(+)-Reboxetine
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Adrenergic Receptor
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Neurological Disease
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Esreboxetine ((S,S)-Reboxetine) is a selective norepinephrine reuptake inhibitor with activity in increasing urethral resistance. Esreboxetine has been reported to be effective in patients with stress urinary incontinence in a Phase IIa clinical study, achieving this effect by increasing urethral closure. The mechanism of action of esreboxetine involves inhibition of norepinephrine transporters in the central and peripheral nervous systems. The peripheral selectivity of esreboxetine helps it significantly increase urethral resistance without penetrating the brain .
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- HY-128038
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Opioid Receptor
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Neurological Disease
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N-Desmethyl-loperamide is a major metabolite of loperamide, a drug that selectively activates peripheral μopioid receptors with a Ki value of 0.16 nM. N-Desmethyl-loperamide is a substrate of the ATP-dependent efflux transporter P-glycoprotein .
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- HY-116018
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Phospholipase
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Neurological Disease
Inflammation/Immunology
Cancer
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FKGK11 is a potent and selective inhibitor of GVIA iPLA2 (Group VIA calcium-independent phospholipase A2). FKGK11 can be used for the research of ovarian cancer and neurological disorders such as peripheral nerve injury and multiple sclerosis .
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- HY-108353A
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- HY-101610
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- HY-B0311AS
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(S)-(-)-Carbidopa-d3 monohydrate
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Aryl Hydrocarbon Receptor
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Neurological Disease
Cancer
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Carbidopa-d3 (monohydrate) is the deuterium labeled Carbidopa monohydrate. Carbidopa ((S)-(-)-Carbidopa) monohydrate, a peripheral decarboxylase inhibitor, can be used for the research of Parkinson's disease. Carbidopa monohydrate is a selective aryl hydrocarbon receptor (AhR) modulator. Carbidopa monohydrate inhibits pancreatic cancer cell and tumor growth .
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- HY-B1298A
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Adrenergic Receptor
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Cardiovascular Disease
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Methoxamine is a selective alpha1-adrenergic receptor agonist. Methoxamine causes vasoconstriction and increased peripheral vascular resistance . Methoxamine hydrochloride significantly increased the overflow of ATP, ADP and AMP, but not adenosine, by a prazosin-sensitive mechanism in the rabbit pulmonary artery .
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- HY-157014
-
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Tryptophan Hydroxylase
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Cancer
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TPT-004 is a selective and oraly active tryptophan hydroxylases (TPH) inhibitor with IC50s of 77 nM and 16 nM for TPH1 and TPH2, repsectively. TPT-004 exhibits exceptional selectivity for TPH1 compared with other members of the AAAH family. TPT-004 shows efficacy peripheral serotonin attenuation and colorectal tumor growth in mice[1][2].
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- HY-19057
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MK-467; L-659066
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Adrenergic Receptor
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Cardiovascular Disease
Neurological Disease
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Vatinoxan (MK-467) is an alpha 2-adrenergic receptor antagonist. The peripheral selectivity of Vatinoxan determines that it has limited penetration across the blood-brain barrier and therefore has low concentrations in the central nervous system. Vatinoxan antagonizes alpha 2-adrenergic receptor receptors by binding to them, thereby reducing or preventing cardiovascular effects caused by α2-adrenergic agonists. Vatinoxan can be used in studies of cardiovascular effects, sedation and analgesia .
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- HY-103410
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EMD 45609 hydrochloride
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Dopamine Receptor
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Cardiovascular Disease
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Carmoxirole hydrochloride (EMD 45609 hydrochloride) is a selective, peripherally acting dopamine D2 receptor agonist and exhibits antihypertensive activities in vivo .
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- HY-P2898
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Biochemical Assay Reagents
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Neurological Disease
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Chondroitinase C degrades chondroitin sulfate glycosaminoglycans that inhibit axonal growth within the endoneurium of peripheral nerve. Chondroitinase C selectively enhances the axon growth-promoting properties of the endoneurial basal lamina .
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- HY-110065
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Cannabinoid Receptor
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Neurological Disease
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SER-601 is a potent and selective peripheral cannabinoid (CB2) receptor agonist with a Ki of 6.3 nM. SER-601 has analgesic and antidiabetic properties and can be used for relevant research .
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- HY-107384
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EMD-61753
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Opioid Receptor
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Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
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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) .
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- HY-403593
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- HY-13331R
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Cortexolone 17 alpha-propionate (Standard); Cortexolone 17α-propionate (Standard); CB-03-01 (Standard)
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Androgen Receptor
Reference Standards
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Endocrinology
|
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Clascoterone (Standard) is the analytical standard of Clascoterone. This product is intended for research and analytical applications. Clascoterone (Cortexolone 17 alpha-propionate;Cortexolone 17α-propionate;CB-03-01) is a new topical and peripherally selective androgen antagonist.
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- HY-B0347S1
-
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Apoptosis
Caspase
Calcium Channel
Reactive Oxygen Species (ROS)
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Cardiovascular Disease
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Lacidipine- 13C8 is the deuterium labeled Lacidipine . Lacidipine is an orally active and highly selective L-type calcium channel blocker that acts on smooth muscle calcium channels, primarily dilates peripheral arteries, reduces peripheral resistance, and has long-lasting anti-hypertensive activity. Lacidipine protects HKCs from apoptosis induced by ATP depletion and recovery by modulating the caspase-3 pathway. Lacidipine can be used in studies of hypertension, atherosclerosis and acute kidney injury (AKI) .
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- HY-U00363
-
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FK-480
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Cholecystokinin Receptor
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Endocrinology
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CHEMBL333994 (FK-480) is a potent and orally active Cholecystokinin A receptor (CCK-A receptor) antagonist, with an IC50 of 0.67 nM. CHEMBL333994 selectively antagonizes peripheral CCK receptors. CHEMBL333994 increases CCK mRNA level. CHEMBL333994 can be used for research of chronic pancreatitis .
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- HY-N6097
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- HY-122331
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- HY-122281
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Cannabinoid Receptor
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Others
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JTE 7-31 selectively acts on peripheral cannabinoid receptors, minimizing central nervous system side effects. They exhibit potent immunomodulatory, anti-inflammatory and anti-allergic properties, as well as inhibitory effects on nephritis .
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- HY-P5907
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Opioid Receptor
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Neurological Disease
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Helianorphin-19 is a potent and selective κ-opioid receptor (KOR) activator with a Ki of 21 nM and an EC50 of 45 nM. Helianorphin-19 exhibits strong KOR-specific peripheral analgesic activity in a mouse model of chronic visceral pain .
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- HY-P2696
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Transmembrane Glycoprotein
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Cardiovascular Disease
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EP 80317 is a selective CD36 ligand. EP 80317 protects the heart against damage and dysfunction elicited by myocardial ischaemia and reperfusion (MI/R), along with a transient reduction in peripheral lipolysis. EP 80317 can be used for the study of cardiovascular disease .
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- HY-B0311R
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(S)-(-)-Carbidopa (Standard)
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Aryl Hydrocarbon Receptor
Reference Standards
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Neurological Disease
Cancer
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Carbidopa (Standard) is the analytical standard of Carbidopa. This product is intended for research and analytical applications. Carbidopa ((S)-(-)-Carbidopa), a peripheral decarboxylase inhibitor, can be used for the research of Parkinson's disease. Carbidopa is a selective aryl hydrocarbon receptor (AhR) modulator. Carbidopa inhibits pancreatic cancer cell and tumor growth .
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- HY-B0311AR
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(S)-(-)-Carbidopa monohydrate (Standard)
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Reference Standards
Aryl Hydrocarbon Receptor
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Neurological Disease
Cancer
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Carbidopa (monohydrate) (Standard) is the analytical standard of Carbidopa (monohydrate). This product is intended for research and analytical applications. Carbidopa ((S)-(-)-Carbidopa) monohydrate, a peripheral decarboxylase inhibitor, can be used for the research of Parkinson's disease. Carbidopa monohydrate is a selective aryl hydrocarbon receptor (AhR) modulator. Carbidopa monohydrate inhibits pancreatic cancer cell and tumor growth .
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- HY-13331S2
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Cortexolone 17 alpha-propionate-d5-1; Cortexolone 17α-propionate-d5-1; CB-03-01-d5-1
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Isotope-Labeled Compounds
Androgen Receptor
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Endocrinology
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Clascoterone-d5-1 (Cortexolone 17 alpha-propionate-d5-1) is deuterium labeled Clascoterone. Clascoterone (Cortexolone 17 alpha-propionate;Cortexolone 17α-propionate;CB-03-01) is a new topical and peripherally selective androgen antagonist .
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- HY-B0233R
-
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PN 200-110 (Standard)
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Reference Standards
Calcium Channel
Autophagy
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Cardiovascular Disease
Neurological Disease
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Isradipine (Standard) is the analytical standard of Isradipine. This product is intended for research and analytical applications. Isradipine (PN 200-110) is an orally active L-type calcium channel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease .
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- HY-B0233S2
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PN 200-110-d7
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Calcium Channel
Autophagy
Isotope-Labeled Compounds
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Cardiovascular Disease
Neurological Disease
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Isradipine-d7 is deuterated labeled Isradipine (HY-B0233). Isradipine (PN 200-110) is an orally active L-type calcium channel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease .
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- HY-145884
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Btk
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Inflammation/Immunology
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BTK-IN-8 is a potent and 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) .
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- HY-101616
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- HY-118209
-
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Dopamine Receptor
5-HT Receptor
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Neurological Disease
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L-646462 is an antagonist of dopamine and 5-HT, with selectivity for the peripheral system (the central/peripheral activity ratio of L-646462 is 143). L-646462 can be used in research related to nausea, vomiting, and associated neurological disorders .
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- HY-105112
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- HY-119605
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GABA Receptor
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Neurological Disease
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DAA-1097 is an orally active and selective agonist for the peripheral benzodiazepine receptor (PBR). DAA-1097 has anxiolytic effects .
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- HY-B0233S1
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PN 200-110-d6
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Calcium Channel
Autophagy
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Neurological Disease
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Isradipine-d6 is the deuterium labeled Isradipine . Isradipine (PN 200-110) is an orally active L-type calcium channel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease .
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- HY-106147
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Opioid Receptor
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Neurological Disease
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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 .
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- HY-106045
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CI 914 free base
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Phosphodiesterase (PDE)
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Cardiovascular Disease
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Imazodan is a selective inhibitor for phosphodiesterase III (PDE III), which increases myocardial contractility by blocking the cAMP degradation, and improves the contractile function of heart. Imazodan serves also as a peripheral vasodilator .
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- HY-106147B
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Opioid Receptor
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Neurological Disease
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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 .
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- HY-129787
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Cannabinoid Receptor
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Neurological Disease
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PF-03550096 is an orally active synthetic cannabinoid (CB) that selectively targets peripheral CB2 receptors with a Ki value of 7.9 nM. PF-03550096 has analgesic activity .
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- HY-B0233S
-
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Isotope-Labeled Compounds
Calcium Channel
Autophagy
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Cardiovascular Disease
Neurological Disease
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Isradipine-d3 (PN 200-110-d3) is the deuterium labeled Isradipine. Isradipine (PN 200-110) is an orally active L-type calcium channel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease .
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- HY-103410R
-
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EMD 45609 hydrochloride (Standard)
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Reference Standards
Dopamine Receptor
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Cardiovascular Disease
|
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Carmoxirole (hydrochloride) (Standard) is the analytical standard of Carmoxirole (hydrochloride). This product is intended for research and analytical applications. Carmoxirole hydrochloride (EMD 45609 hydrochloride) is a selective, peripherally acting dopamine D2 receptor agonist and exhibits antihypertensive activities in vivo .
|
-
- HY-N2304A
-
|
|
Opioid Receptor
|
Inflammation/Immunology
|
|
Methyl-6-alpha-Naltrexol is a metabolite of Methylnaltrexone (MNTX). Methylnaltrexone is a selective mu-opioid receptor antagonist and functions as a peripherally acting receptor antagonist in tissues of the gastrointestinal tract .
|
-
- HY-120927
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Alvimopan metabolite is a μ opioid receptor antagonist with activity that selectively interacts with μ peripheral receptors. Alvimopan metabolite can be used as a potential inhibitory drug to alleviate the side effects caused by opioids. Alvimopan metabolite was identified as a highly selective μ opioid receptor antagonist during research and development .
|
-
- HY-125881
-
|
|
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-17609C
-
|
CR-845 acetate; FE-202845 acetate
|
Opioid Receptor
|
Neurological Disease
|
|
Difelikefalin (CR-845; FE-202845) acetate is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin acetate produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease .
|
-
- HY-106045A
-
|
CI 914
|
Phosphodiesterase (PDE)
|
Cardiovascular Disease
|
|
Imazodan hydrochloride is the hydrochloride form of Imazodan (HY-106045). Imazodan hydrochloride is a selective inhibitor for phosphodiesterase III (PDE III), which increases myocardial contractility by blocking the cAMP degradation, and improves the contractile function of heart. Imazodan hydrochloride serves also as a peripheral vasodilator .
|
-
- HY-B0311D
-
|
(S)-(-)-Carbidopa hydrochloride
|
Aryl Hydrocarbon Receptor
|
Cancer
|
|
Carbidopa hydrochloride ((S)-(-)-Carbidopa hydrochloride) is a drug used to inhibit Parkinson's disease, which has the activity of inhibiting the peripheral metabolism of levodopa. Carbidopa hydrochloride can increase the proportion of peripheral levodopa penetrating the blood-brain barrier, thereby enhancing its effect on the central nervous system. Carbidopa hydrochloride has also been found to be an aryl hydrocarbon receptor (AhR) ligand with anticancer activity, which can inhibit the growth of pancreatic cancer cells and tumors. The selective AhR regulation properties of carbidopa hydrochloride provide potential prospects for its clinical application .
|
-
- HY-B0347S3
-
|
|
Calcium Channel
Caspase
Reactive Oxygen Species (ROS)
Apoptosis
Isotope-Labeled Compounds
|
Cardiovascular Disease
|
|
Lacidipine- 13C4 is 13C labeled Lacidipine (HY-B0347). Lacidipine is an orally active and highly selective L-type calcium channel blocker that acts on smooth muscle calcium channels, primarily dilates peripheral arteries, reduces peripheral resistance, and has long-lasting anti-hypertensive activity. Lacidipine protects HKCs from apoptosis induced by ATP depletion and recovery by modulating the caspase-3 pathway. Lacidipine can be used in studies of hypertension, atherosclerosis and acute kidney injury (AKI) .
|
-
- HY-B0347R
-
|
|
Reference Standards
Calcium Channel
Reactive Oxygen Species (ROS)
Caspase
Apoptosis
|
Cardiovascular Disease
|
|
Lacidipine (Standard) is the analytical standard of Lacidipine. This product is intended for research and analytical applications. Lacidipine is an orally active and highly selective L-type calcium channel blocker that acts on smooth muscle calcium channels, primarily dilates peripheral arteries, reduces peripheral resistance, and has long-lasting anti-hypertensive activity. Lacidipine protects HKCs from apoptosis induced by ATP depletion and recovery by modulating the caspase-3 pathway. Lacidipine can be used in studies of hypertension, atherosclerosis and acute kidney injury (AKI) .
|
-
- HY-154832
-
|
|
Calcium Channel
|
Cardiovascular Disease
|
|
Cav 3.2 inhibitor 4 (compound 21) is a potent, peripherally restricted, selective T-type calcium channel (Cav3.2) inhibitor, with an IC50 of 0.6 μM. Cav 3.2 inhibitor 4 can be used for the research of atrial fibrillation .
|
-
- HY-118064
-
|
LY-368975
|
Dopamine Receptor
|
Neurological Disease
|
|
(R)-Thionisoxetine is a potent and selective inhibitor of central and peripheral norepinephrine (NE) uptake. (R)-thionisoxetine prevented hypothalamic NE depletion by 6-hydroxydopamine with an ED50 of 0.21 mg/kg. (R)-Thionisoxetine can be used for the research of a variety of diseases including depression and urinary incontinence .
|
-
- HY-120554
-
|
|
Potassium Channel
|
Cardiovascular Disease
|
|
RWJ 29009 is a highly selective ATP-sensitive potassium channel agonist. RWJ 29009 activates potassium channel in vascular smooth muscle cells, promoting potassium efflux and membrane hyperpolarization to induce coronary and peripheral vasodilation. RWJ 29009 is promising for research of cardiovascular diseases such as acute myocardial ischemia and hypertension .
|
-
- HY-121704
-
|
|
iGluR
|
Neurological Disease
|
|
SR 57227A Free base is a highly selective compound for both peripheral and central 5-HT3 receptors and acts as an inhibitor of NMDA receptor-mediated responses in rat cortical pyramidal cells, demonstrating antidepressant-like effects in rats while reducing isolation-induced aggressive behavior.
|
-
- HY-N2998R
-
|
|
Reference Standards
β-glucuronidase
|
Metabolic Disease
|
|
Carbidopa (monohydrate) (Standard) is the analytical standard of Carbidopa (monohydrate). This product is intended for research and analytical applications. Carbidopa ((S)-(-)-Carbidopa) monohydrate, a peripheral decarboxylase inhibitor, can be used for the research of Parkinson's disease. Carbidopa monohydrate is a selective aryl hydrocarbon receptor (AhR) modulator. Carbidopa monohydrate inhibits pancreatic cancer cell and tumor growth .
|
-
- HY-13331S1
-
|
Cortexolone 17 alpha-propionate-d6; Cortexolone 17α-propionate-d6; CB-03-01-d6
|
Isotope-Labeled Compounds
Androgen Receptor
|
Endocrinology
|
|
Clascoterone-d6 (Cortexolone 17 alpha-propionate-d6) is deuterium labeled Clascoterone. Clascoterone (Cortexolone 17 alpha-propionate;Cortexolone 17α-propionate;CB-03-01) is a new topical and peripherally selective androgen antagonist .
|
-
- HY-B0311S1
-
|
(S)-(-)-Carbidopa-d3
|
Aryl Hydrocarbon Receptor
Isotope-Labeled Compounds
|
Neurological Disease
|
|
Carbidopa-d3-1 is the deuterium labeled Carbidopa (HY-B0311). Carbidopa, a peripheral decarboxylase inhibitor, can be used for the research of Parkinson's disease. Carbidopa is a selective aryl hydrocarbon receptor (AhR) modulator. Carbidopa inhibits pancreatic cancer cell and tumor growth .
|
-
- HY-17043S
-
-
- HY-118064A
-
|
LY-368975 hydrochloride
|
Monoamine Transporter
|
Neurological Disease
|
|
(R)-Thionisoxetine hydrochloride (LY-368975 hydrochloride) is a potent and selective central and peripheral norepinephrine (NE) uptake inhibitor. (R)-Thionisoxetine hydrochloride prevents 6-hydroxydopamine-induced hypothalamic NE depletion with an ED50 of 0.21 mg/kg. (R)-Thionisoxetine hydrochloride can be used in the study of a variety of diseases, including depression and urinary incontinence .
|
-
- HY-B0098B
-
|
(R)-UK 33274
|
Adrenergic Receptor
|
Metabolic Disease
|
|
(R)-Doxazosin ((R)-UK 33274) is an isomer of Doxazosin, a selective and orally active a1-adrenoceptor agonist. Doxazosin can be used for systemic antihypertensive and ocular hypotensive. Doxazosin exerts its antihypertensive effect by reducing total peripheral resistance by selective postsynaptic a1-blockade, without reducing cardiac output. Doxazosin can significantly lower both standing and supine blood pressure .
|
-
- HY-144126
-
|
|
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-B0468S
-
|
Isoproterenol-d7 hydrochloride
|
Isotope-Labeled Compounds
Endogenous Metabolite
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Isoprenaline-d7 (hydrochloride) is a deuterated labeled Isoprenaline (hydrochloride) . Isoprenaline (Isoproterenol) hydrochloride is a non-selective, orally active β-adrenergic receptor agonist. Isoprenaline has potent peripheral vasodilator, bronchodilator, and cardiac stimulating activities. Isoprenaline can be used for the research of bradycardia and bronchial asthma .
|
-
- HY-150728
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
AChE-IN-22 (compound 10q) is a selective acetylcholinesterase (AChE) inhibitor against AChE and BuChE with the IC50 values of 0.88 μM and 10 μM, respectively. AChE-IN-22 can bind to both the CAS (catalytic active site) and PAS (peripheral anionic site) of AChE and has the potential for the research of Alzheimer's disease .
|
-
- HY-112481
-
|
|
|
Inflammation/Immunology
|
|
IKK2-IN-5 is a selective IKK-2 inhibitor with an IC50 of 0.025 μM. IKK2-IN-5 inhibits the production of TNF-α in LPS (HY-D1056)-stimulated human peripheral blood mononuclear cells. IKK2-IN-5 exhibits extremely low cytotoxicity against human peripheral blood mononuclear cells .
|
-
- HY-107319R
-
|
Almitrine bismesylate (Standard); Almitrine bismethanesulfonate (Standard); Almitrine dimesylate (Standard)
|
Reference Standards
Potassium Channel
|
Cardiovascular Disease
Neurological Disease
|
|
Almitrine mesylate (Standard) (Almitrine bismesylate (Standard)) is the analytical standard of Almitrine mesylate (HY-107319). This product is intended for research and analytical applications. Almitrine mesylate, a peripheral chemoreceptor agonist, inhibits selectively the Ca2+-dependent K+ channel.
|
-
- HY-P2696A
-
|
|
Transmembrane Glycoprotein
|
Cardiovascular Disease
|
|
EP 80317 acetate is a selective CD36 ligand. EP 80317 acetate protects the heart against damage and dysfunction elicited by myocardial ischaemia and reperfusion (MI/R), along with a transient reduction in peripheral lipolysis. EP 80317 acetate can be used for the study of cardiovascular disease .
|
-
- HY-103210R
-
|
Neurotoxin DSP 4 hydrochloride (Standard)
|
Adrenergic Receptor
Reference Standards
|
Neurological Disease
|
|
DSP-4 hydrochloride (Standard) is the analytical standard of DSP-4 hydrochloride (HY-103210). This product is intended for research and analytical applications. 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-107384AR
-
|
EMD-61753 hydrochloride (Standard)
|
Reference Standards
Opioid Receptor
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
Asimadoline hydrochloride (Standard) (EMD-61753 hydrochloride (Standard)) is the analytical standard of Asimadoline (hydrochloride) (HY-107384A). This product is intended for research and analytical applications. 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-186066
-
|
|
HCN Channel
|
Neurological Disease
|
|
HCN2-IN-2 (Compound 35), azaindazole derivative, is a selective HCN2 inhibitor with an IC50 of 145 nM. HCN2-IN-2 inhibits HCN2 channel activity blocks abnormal firing of peripheral nociceptive neurons. HCN2-IN-2 can be used for the research of pain .
|
-
- HY-B0715
-
|
BL-191; PTX; Oxpentifylline
|
Phosphodiesterase (PDE)
Autophagy
HIV
|
Cardiovascular Disease
Cancer
|
|
Pentoxifylline (BL-191), a haemorheological agent, is an orally active non-selective phosphodiesterase (PDE) inhibitor, with immune modulation, anti-inflammatory, hemorheological, anti-fibrinolytic and anti-proliferation effects. Pentoxifylline can be used for the research of peripheral vascular disease, cerebrovascular disease and a number of other conditions involving a defective regional microcirculation .
|
-
- HY-B0468R
-
|
Isoproterenol hydrochloride (Standard)
|
Reference Standards
Adrenergic Receptor
Endogenous Metabolite
|
Cardiovascular Disease
Endocrinology
|
|
Isoprenaline (hydrochloride) (Standard) is the analytical standard of Isoprenaline (hydrochloride). This product is intended for research and analytical applications. Isoprenaline (Isoproterenol) hydrochloride is a non-selective, orally active β-adrenergic receptor agonist. Isoprenaline has potent peripheral vasodilator, bronchodilator, and cardiac stimulating activities. Isoprenaline can be used for the research of bradycardia and bronchial asthma .
|
-
- HY-12717AS
-
|
|
Isotope-Labeled Compounds
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 .
|
-
- HY-138568
-
|
|
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-129406
-
|
|
Drug Derivative
|
Cardiovascular Disease
|
|
AF 698 is a phthalate derivative of Apovincamine (HY-135743) that can be used as a peripheral vasodilator with selective vasomotor effects on cerebral microvascular circulation. AF 698 has better vasodilator effect than Vincamine (HY-B1021), but there is no significant difference in the protective effect of the two drugs against hypobaric hypoxia-induced lethality in mice .
|
-
- HY-23188
-
|
Loratidine-d5-1; SCH 29851-d5-1
|
Isotope-Labeled Compounds
|
Others
|
|
Loratadine-d5-1 is a deuterated labeled Loratadine (HY-17043). Loratadine (SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. Loratadine has anti-dengue-virus (DENV) activity. Loratadine can inhibit immunologic release of inflammatory mediators.
|
-
- HY-183204
-
|
|
nAChR
|
Neurological Disease
|
|
TC-2559 is an orally active, selective central nervous system Nicotinic acetylcholine receptor agonist with a Ki value of 5 nM. TC-2559 activates central nervous system receptors selectively over peripheral nervous system receptors. TC-2559 improves scopolamine (HY-N0296)-induced cognitive impairment and enhances radial arm maze performance. TC-2559 can be used in the research of neurodegenerative diseases .
|
-
- HY-146662
-
|
|
PGE synthase
|
Inflammation/Immunology
|
|
HPGDS inhibitor 3 is an orally active and highly potent peripherally restricted hematopoietic prostaglandin D synthase (H-PGDS) inhibitor with IC50 value of 9.4 nM and EC50 of 42 nM, respectively. HPGDS inhibitor 3 exhibits good selectivity, good pharmacokinetic parameters in mouse, rat, and dog, and no CNS toxicity. HPGDS inhibitor 3 has anti-inflammatory activity .
|
-
- HY-17609S
-
|
CR-845-d5; FE-202845-d5
|
Isotope-Labeled Compounds
Opioid Receptor
|
Neurological Disease
|
|
Difelikefalin-d5 (CR-845-d5) is deuterium labeled Difelikefalin. Difelikefalin (CR-845; FE-202845) is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease .
|
-
- HY-17043S2
-
-
- HY-113826
-
|
|
Lipoxygenase
|
Others
|
|
L-656224 is an orally active, potent and selective inhibitor of leukotriene biosynthesis in intact rat and human leukocytes and CXBG mastocytoma cells (IC50 values, 18-240 nM) and of human leukocyte and porcine leukocyte 5-lipoxygenase (IC50, 4 x 10 -7 M). L-656224 is promising for research of asthma and peripheral analgesic agents .
|
-
- HY-107322A
-
|
Mepirodipine; YM-09730-5 Free base
|
Calcium Channel
|
Cardiovascular Disease
|
|
Barnidipine (Mepirodipine) is an L-type calcium antagonist (CaA) with high affinity for [ 3H] initrendipine binding sites (Ki = 0.21 nmol/L), has selective action against CaA receptors. Barnidipine is an orally effective antihypertensive agent that can reduce the level of platelet-derived growth factor B-chain mRNA and peripheral vascular resistance .
|
-
- HY-107322
-
|
Mepirodipine hydrochloride; YM-09730-5
|
Calcium Channel
|
Cardiovascular Disease
|
|
Barnidipine (Mepirodipine) hydrochloride is an L-type calcium antagonist (CaA) with high affinity for [ 3H] initrendipine binding sites (Ki = 0.21 nmol/L, has selective action against CaA receptors. Barnidipine hydrochloride is an orally active antihypertensive agent that can reduce the level of platelet-derived growth factor B-chain mRNA and peripheral vascular resistance .
|
-
- HY-153963A
-
|
|
Oxytocin Receptor
|
Endocrinology
|
|
PF-06655075 (TFA) is the TFA form of PF-06655075 (HY-153963). PF-06655075 is a novel andnon–brain-penetrant oxytocin receptor agonist with increased selectivity for the oxytocin receptor and significantly increased pharmacokinetic stability. PF-06655075 can be used as a tool compound to further explore the role of peripheral oxytocin in behavioral response .
|
-
- HY-17043S3
-
-
- HY-17609S1
-
|
CR-845-d5 hydrochloride; FE-202845-d5 hydrochloride
|
Isotope-Labeled Compounds
Opioid Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
Difelikefalin-d5 (CR-845-d5) hydrochloride is the deuterium labeled Difelikefalin (HY-17609). Difelikefalin (CR-845) is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease .
|
-
- HY-P10746
-
|
|
Neurokinin Receptor
|
Metabolic Disease
|
|
EB1002 is a highly selective, long-acting NK2R agonist. EB1002 exerts central appetite suppression, increases peripheral energy expenditure and enhances insulin sensitivity, which effectively reduces body weight, improves glucose and lipid metabolism, with favorable safety profiles. EB1002 can be used for research on diseases such as obesity and type 2 diabetes .
|
-
- HY-U00363A
-
|
(rac)-FK-480
|
Cholecystokinin Receptor
Drug Isomer
|
Inflammation/Immunology
|
|
(rac)-CHEMBL333994 is the racemate of CHEMBL333994 (HY-U00363). CHEMBL333994 is a potent and orally active Cholecystokinin A receptor (CCK-A receptor) antagonist, with an IC50 of 0.67 nM. CHEMBL333994 selectively antagonizes peripheral CCK receptors. CHEMBL333994 increases CCK mRNA level. CHEMBL333994 can be used for research of chronic pancreatitis .
|
-
- HY-B0362AR
-
|
Phentolamine methanesulfonate (Standard)
|
Reference Standards
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
Cancer
|
|
Phentolamine (mesylate) (Standard) is the analytical standard of Phentolamine (mesylate). This product is intended for research and analytical applications. 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-B0715S
-
|
BL-191-d6; PTX-d6; Oxpentifylline-d6
|
Phosphodiesterase (PDE)
Autophagy
HIV
|
Cardiovascular Disease
Cancer
|
|
Pentoxifylline-d6 is the deuterium labeled Pentoxifylline. Pentoxifylline (BL-191), a haemorheological agent, is an orally active non-selective phosphodiesterase (PDE) inhibitor, with immune modulation, anti-inflammatory, hemorheological, anti-fibrinolytic and anti-proliferation effects. Pentoxifylline can be used for the research of peripheral vascular disease, cerebrovascular disease and a number of other conditions involving a defective regional microcirculation .
|
-
- HY-B0715S2
-
|
BL-191-d5; PTX-d5; Oxpentifylline-d5
|
Phosphodiesterase (PDE)
Autophagy
HIV
|
Cardiovascular Disease
Cancer
|
|
Pentoxifylline-d5 is the deuterium labeled Pentoxifylline. Pentoxifylline (BL-191), a haemorheological agent, is an orally active non-selective phosphodiesterase (PDE) inhibitor, with immune modulation, anti-inflammatory, hemorheological, anti-fibrinolytic and anti-proliferation effects. Pentoxifylline can be used for the research of peripheral vascular disease, cerebrovascular disease and a number of other conditions involving a defective regional microcirculation .
|
-
- HY-120622
-
|
|
Src
|
Cancer
|
|
BMS-243117 is a potent, and selective benzothiazole based p56 Lck inhibitor with an IC50 of 4 nM. BMS-243117 inhibits anti-CD3/anti-CD28 induced PBL (human peripheral blood T-cells) proliferation with an IC50 of 1.1 μM. BMS-243117 binds in an extended conformation to the ATP-binding site of Lck .
|
-
- HY-107322S
-
|
Mepirodipine-d5 hydrochloride; YM-09730-5-d5 hydrochloride
|
Isotope-Labeled Compounds
Calcium Channel
|
Cardiovascular Disease
|
|
Barnidipine-d5 (hydrochloride) is the deuterium labeled Barnidipine hydrochloride. Barnidipine hydrochloride (Mepirodipine hydrochloride) is an L-type calcium antagonist (CaA) with high affinity for [3H] initrendipine binding sites (Ki=0.21 nmol/l), has selective action against CaA receptors .Barnidipine hydrochloride (Mepirodipine hydrochloride) is an antihypertensive agent and acts by the reduction of peripheral vascular resistance secondary to its vasodilatory action .
|
-
- HY-111011
-
|
JNJ 38488502 acetate; FE 200665 acetate
|
Opioid Receptor
|
Neurological Disease
|
|
CR 665 (JNJ 38488502) acetate is a kappa-opioid agonist that may effectively treat visceral pain by activating receptors on afferent nerves within the gut. CR 665 acetate exhibits peripheral selectivity, differentiating its pharmacokinetic profile from that of non-selective opioids like oxycodone. CR 665 acetate has demonstrated a beneficial effect on visceral pain tolerance thresholds without the delayed analgesic response characteristic of opioids that penetrate the brain. CR 665 acetate is proposed for use in managing postoperative pain due to its pain-relieving properties.
|
-
- HY-156131
-
|
ADL 2-1294
|
Opioid Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
Loperamide (ADL 2-1294) is selective and orally active μ opioid receptor agonist with Ki valuess of 3, 48 and 1156 nM against μ, δ and κ opioid receptor, respectively. Loperamide produces antinociception and antihyperalgesia. Loperamide exhibits peripheral selectivity, enhancing fluid, electrolyte, and glucose absorption, reversing PGE2 (HY-101952)- and Cholera toxin (HY-P1446)-induced intestinal secretion, and reducing intestinal motility. Loperamide can be used for the researches of inflammatory pain and protracted diarrhoea .
|
-
- HY-171846
-
|
|
TRP Channel
|
Neurological Disease
Inflammation/Immunology
|
|
LY3526318 is an orally active, selective TRPA1 antagonist (IC50=5-6μM). LY3526318 blocks TRPA1 channels, inhibits pain signal transduction mediated by the channel, and exerts analgesic activity. LY3526318 is mainly used in the research of chronic pain-related fields, such as diabetic peripheral neuropathy, chronic low back pain, and pain caused by osteoarthritis .
|
-
- HY-B0002B
-
|
GR 38032; SN 307
|
5-HT Receptor
|
Neurological Disease
|
|
Ondansetron (GR 38032; SN 307) is a highly selective 5-HT3 receptor antagonist with an IC50 value of 103 pM. Ondansetron exerts its antiemetic effect by antagonizing 5-HT receptors located in localized neurons in the peripheral and central nervous systems. Ondansetron can inhibit nausea and vomiting induced by chemotherapy and radiotherapy .
|
-
- HY-10061
-
|
AZD-3355
|
GABA Receptor
|
Metabolic Disease
|
|
Lesogaberan (AZD-3355) is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptors. The affinity (Kis) of Lesogaberan for rat GABAB and GABAA receptors, as measured by displacement of [ 3H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action .
|
-
- HY-156278
-
|
|
Apoptosis
Autophagy
|
Cancer
|
|
FB49 is a highly selective inhibitor of Bcl-2-associated athanogene 3 (BAG3), with the Ki of 45 μM. FB49 inhibits the cell growth in human tumoral cells, but has no toxicity in human peripheral mononuclear cells. FB49 block cell cycle in G1 phase and to induce apoptosis as well as autophagy in medulloblastoma HD-MB03 treated cells .
|
-
- HY-B0002
-
|
GR 38032 hydrochloride; SN 307 hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
|
Ondansetron (GR 38032; SN 307) hydrochloride is a highly selective 5-HT3 receptor antagonist with an IC50 value of 103 pM. Ondansetron hydrochloride exerts its antiemetic effect by antagonizing 5-HT receptors located in localized neurons in the peripheral and central nervous systems. Ondansetron hydrochloride can inhibit nausea and vomiting induced by chemotherapy and radiotherapy .
|
-
- HY-10061B
-
|
AZD-3355 hydrochloride
|
GABA Receptor
|
Metabolic Disease
|
|
Lesogaberan (AZD-3355) hydrochloride is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptor. The affinity (Kis) of Lesogaberan hydrochloride for rat GABAB and GABAA receptors, as measured by displacement of [ 3H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan hydrochloride inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action .
|
-
- HY-156730
-
|
|
Molecular Glues
STAT
|
Cancer
|
|
KT-333 is a molecular glues that degrades STAT3 protein. KT-333 mediates the selective degradation of STAT3 through the ubiquitin-proteasome system by binding to STAT3 protein and E3 ubiquitin ligase von Hippel-Lindau protein (VHL). KT-333 has strong selectivity for STAT3 protein degradation and good antitumor activity. KT-333 can be used in the study of hematologic malignancies such as large granular lymphocytic leukemia (LGL-L), peripheral T-cell lymphoma (PTCL), and cutaneous T-cell lymphoma (CTCL) .
|
-
- HY-147907
-
|
|
Adenosine Receptor
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Adenosine receptor inhibitor 1 is a potent and selective adenosine receptor (AR) inhibitor with Ki values of >1000, 68.5, >1000, >1000 nM for A1AR, A2AAR, A2BAR, A3AR, respectively. Adenosine receptor inhibitor 1 shows antinociceptive activity, anti-inflammatory effect and peripheral analgesic effect. Adenosine receptor inhibitor 1 has the potential for the research of cancer or neurodegenerative diseases .
|
-
- HY-101096R
-
|
MK-8998 (Standard); CX-8998 (Standard); JZP385 (Standard)
|
Calcium Channel
Reference Standards
|
Neurological Disease
Cancer
|
|
Suvecaltamide (Standard) is the analytical standard of Suvecaltamide (HY-101096). This product is intended for research and analytical applications. Suvecaltamide (MK-8998) is a selective T-type calcium channel inhibitor with oral efficacy. Suvecaltamide exhibits no cytotoxicity in myeloma cell lines and does not affect the antitumor efficacy of Bortezomib (BTZ). Suvecaltamide reverses BTZ-induced peripheral neuropathy (CIPN) in mouse and rat models, and helps inhibit myeloma growth .
|
-
- HY-183566
-
|
|
Sodium Channel
|
Neurological Disease
|
|
MK-5661 is an orally potent NaV1.8 voltage-gated sodium channel inhibitor with an EC50 of 4.3 nM. MK-5661 selectively inhibits peripheral nociceptive signaling mediators. MK-5661 reduces capsaicin-induced spontaneous nociceptive behaviors in humanized rats and attenuates capsaicin-induced skin flushing responses in rhesus monkeys. MK-5661 is applicable for pain-related research .
|
-
- HY-10061A
-
|
AZD-3355 napadisylate
|
GABA Receptor
|
Metabolic Disease
|
|
Lesogaberan (AZD-3355) napadisylate is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptors. The affinity (Kis) of Lesogaberan napadisylate for rat GABAB and GABAA receptors, as measured by displacement of [ 3H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan napadisylate inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action .
|
-
- HY-101176R
-
|
|
Reference Standards
Melatonin Receptor
|
Cancer
|
|
2-Iodomelatonin (Standard) is the analytical standard of 2-Iodomelatonin. This product is intended for research and analytical applications. 2-Iodomelatonin is a potent agonist of melatonin receptor 1 (MT1) with a Ki value of 28 pM, it is more 5-fold selective for MT1 ?over MT2 . 2-iodomelatonin can be used to identify, characterize and localize melatonin binding sites in the brain and peripheral tissues .
|
-
- HY-B0715R
-
|
BL-191 (Standard); PTX (Standard); Oxpentifylline (Standard)
|
HIV
Autophagy
Phosphodiesterase (PDE)
Reference Standards
|
Cardiovascular Disease
Cancer
|
|
Pentoxifylline (Standard) is the analytical standard of Pentoxifylline. This product is intended for research and analytical applications. Pentoxifylline (BL-191), a haemorheological agent, is an orally active non-selective phosphodiesterase (PDE) inhibitor, with immune modulation, anti-inflammatory, hemorheological, anti-fibrinolytic and anti-proliferation effects. Pentoxifylline can be used for the research of peripheral vascular disease, cerebrovascular disease and a number of other conditions involving a defective regional microcirculation .
|
-
- HY-118250A
-
|
|
Toll-like Receptor (TLR)
IFNAR
TNF Receptor
|
Inflammation/Immunology
|
|
GSK2245035 maleate is a highly potent and selective intranasal Toll-Like receptor 7 (TLR7) agonist with preferential Type-1 interferon (IFN)-stimulating properties. GSK2245035 maleate has pEC50s of 9.3 and 6.5 for IFNα and TFNα. GSK2245035 maleate effectively suppresses allergen-induced Th2 cytokine production in human peripheral blood cell cultures. GSK2245035 maleate is used for asthma .
|
-
- HY-118250
-
|
|
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-183578
-
|
|
LPL Receptor
|
Inflammation/Immunology
|
|
TYY-31 is an orally active, selective S1PR1 agonist with an EC50 of 1.13 pM. TYY-31 promotes the phosphorylation of ERK1/2. TYY-31 exerts anti-inflammatory and immunosuppressive effects, ameliorates DSS-induced colitis in mice, and reduces peripheral blood lymphocyte counts in mice in a dose-dependent manner. TYY-31 can be used for the research of ulcerative colitis .
|
-
- HY-B0002A
-
|
GR 38032 hydrochloride dihydrate; SN 307 hydrochloride dihydrate
|
5-HT Receptor
|
Neurological Disease
|
|
Ondansetron (GR 38032; SN 307) hydrochloride dehydrate is a highly selective 5-HT3 receptor antagonist with an IC50 value of 103 pM. Ondansetron hydrochloride dehydrate exerts its antiemetic effect by antagonizing 5-HT receptors located in localized neurons in the peripheral and central nervous systems. Ondansetron hydrochloride dehydrate can inhibit nausea and vomiting induced by chemotherapy and radiotherapy .
|
-
- HY-182777
-
|
|
HDAC
NO Synthase
TNF Receptor
Interleukin Related
|
Neurological Disease
Inflammation/Immunology
|
|
HDAC6-IN-80 is an orally active, selective HDAC6 inhibitor with an IC50 of 8.5 nM. HDAC6-IN-80 inhibits lipopolysaccharide-induced microglial activation, reduces the levels of iNOS, COX-2, TNF-α and IL-6, and alleviates sensory hypersensitivity behaviors. HDAC6-IN-80 can be used for the research of inflammatory pain and chemotherapy-induced peripheral neuropathy .
|
-
- HY-156730B
-
|
|
Molecular Glues
STAT
|
Cancer
|
|
KT-333 diammonium is a molecular glues that degrades STAT3 protein. KT-333 diammonium mediates the selective degradation of STAT3 through the ubiquitin-proteasome system by binding to STAT3 protein and E3 ubiquitin ligase von Hippel-Lindau protein (VHL). KT-333 diammonium has strong selectivity for STAT3 protein degradation and good antitumor activity. KT-333 diammonium can be used in the study of hematologic malignancies such as large granular lymphocytic leukemia (LGL-L), peripheral T-cell lymphoma (PTCL), and cutaneous T-cell lymphoma (CTCL) .
|
-
- HY-107322AS1
-
|
Mepirodipine-d5; YM-09730-5-d5 Free base
|
Isotope-Labeled Compounds
|
Others
|
|
Barnidipine-d5 is the deuterium-labeled Barnidipine (HY-107322A). Barnidipine-d5 (Mepirodipine) is an L-type calcium antagonist (CaA) with high affinity for [ 3H] initrendipine binding sites (Ki=0.21 nmol/l), has selective action against CaA receptors . Barnidipine-d5 (Mepirodipine) is an antihypertensive agent and acts by the reduction of peripheral vascular resistance secondary to its vasodilatory action .
|
-
- HY-B0715S3
-
|
BL-191-d3; PTX-d3; Oxpentifylline-d3
|
Isotope-Labeled Compounds
Autophagy
Phosphodiesterase (PDE)
HIV
|
Cardiovascular Disease
Cancer
|
|
Pentoxifylline-d3 (BL-191-d3) is deuterium labeled Pentoxifylline. Pentoxifylline (BL-191), a haemorheological agent, is an orally active non-selective phosphodiesterase (PDE) inhibitor, with immune modulation, anti-inflammatory, hemorheological, anti-fibrinolytic and anti-proliferation effects. Pentoxifylline can be used for the research of peripheral vascular disease, cerebrovascular disease and a number of other conditions involving a defective regional microcirculation .
|
-
- HY-B1021
-
|
|
Free Fatty Acid Receptor
|
Cardiovascular Disease
Metabolic Disease
|
|
Vincamine is a monoterpenoid indole alkaloid extracted from the Madagascar periwinkle. Vincamine is a peripheral vasodilator and exerts a selective vasoregulator action on the brain microcapilar circulation . Vincamine is a GPR40 agonist and acts as a β-cell protector by ameliorating β-cell dysfunction and promoting glucose-stimulated insulin secretion (GSIS). Vincamine improves glucose homeostasis in vivo, and has the potential for the type 2 diabetes mellitus (T2DM) research .
|
-
- HY-P10965
-
|
ZT002
|
GLP Receptor
|
Metabolic Disease
|
|
Zovaglutide (ZT002) is a long-acting, selective GLP-1 receptor agonist. Zovaglutide enhances albumin binding capacity via dual fatty acid chain modification. Zovaglutide exerts metabolic effects through central and peripheral GLP-1 pathways, thereby promoting satiety, reducing caloric intake and enhancing glucose-dependent insulin secretion, with no activity against GIP or glucagon receptors. Zovaglutide can be used in research on type 2 diabetes or obesity .
|
-
- HY-P5869
-
|
|
Calcium Channel
Sodium Channel
|
Neurological Disease
|
|
Kurtoxin is a selective Cav3 (T-type) voltage-gated Ca 2+ channel gating inhibitor with a Kd of 15 nM for Cav3.1 (α1G T-type) Ca 2+ channel. Kurtoxin can interact with high affinity with native neuronal high-threshold L-type, N-type, and P-type Ca 2+ channels in central and peripheral neurons. Kurtoxin also shows cross-reactivity with voltage-gated Na + channel .
|
-
- HY-19969
-
|
|
Interleukin Related
|
Inflammation/Immunology
|
|
YM-90709 is a novel IL-5 inhibitor which selectively blocks the binding of IL-5 to the IL-5 receptor (IL-5R).YM-90709 potently inhibits the binding of [ 125I]-IL-5 to IL-5R on human peripheral eosinophils and eosinophilic HL-60 clone 15 cells with IC50 values of 1.0 and 0.57 μM .
|
-
- HY-156730A
-
|
|
Molecular Glues
STAT
|
Cancer
|
|
KT-333 ammonium (Compound A) is a molecular glues that degrades STAT3 protein. KT-333 ammonium mediates the selective degradation of STAT3 through the ubiquitin-proteasome system by binding to STAT3 protein and E3 ubiquitin ligase von Hippel-Lindau protein (VHL). KT-333 ammonium has strong selectivity for STAT3 protein degradation and good antitumor activity. KT-333 ammonium can be used in the study of hematologic malignancies such as large granular lymphocytic leukemia (LGL-L), peripheral T-cell lymphoma (PTCL), and cutaneous T-cell lymphoma (CTCL) .
|
-
- HY-P1106
-
|
|
CRFR
|
Cardiovascular Disease
|
|
K41498 is a highly selective CRF 2 receptor antagonist, with a Ki of 0.66 nM for human CRF2α receptor and a Ki of 0.62 nM for human CRF2β receptor. K41498 inhibits cAMP accumulation in cells expressing CRF2. K41498 antagonizes the hypotensive response induced by systemic administration of urocortin in conscious rats. K41498 undergoes radioiodination without loss of activity and serves for autoradiographic studies of native CRF2 receptors in rat brain and peripheral tissues .
|
-
- HY-13106
-
|
EMA401; PD-126055; (S)-EMA400
|
Angiotensin Receptor
|
Cardiovascular Disease
Neurological Disease
Endocrinology
|
|
Olodanrigan (EMA401) is a highly selective, orally active, peripherally restricted angiotensin II type 2 receptor (AT2R) antagonist. It is under development as a neuropathic pain therapeutic agent. Olodanrigan (EMA401) analgesic action appears to involve inhibition of augmented AngII/AT2R induced p38 and p42/p44 MAPK activation, and hence inhibition of DRG neuron hyperexcitability and sprouting of DRG neurons .
|
-
- HY-180320
-
|
|
LRRK2
|
Neurological Disease
|
|
Lu AF58786 is a potent and selective LRRK2 inhibitor with an IC50 of 12 nM. Lu AF58786 also exhibits inhibition activity against LRRK2 G2019S and LRRK2 A2016T with IC50s of 19 and 93 nM. Lu AF58786 inhibits phosphorylation of LRRK2, Rab10 and Rab12 in human peripheral blood mononuclear cells. Lu AF58786 can be used for parkinson’s disease research .
|
-
- HY-107322R
-
|
Mepirodipine hydrochloride (Standard); YM-09730-5 (Standard)
|
Reference Standards
Calcium Channel
|
Cardiovascular Disease
|
|
Barnidipine hydrochloride (Standard) (Mepirodipine hydrochloride (Standard)) is the analytical standard of Barnidipine (hydrochloride) (HY-107322). This product is intended for research and analytical applications. Barnidipine (Mepirodipine) hydrochloride is an L-type calcium antagonist (CaA) with high affinity for [3H] initrendipine binding sites (Ki = 0.21 nmol/L, has selective action against CaA receptors. Barnidipine hydrochloride is an orally active antihypertensive agent that can reduce the level of platelet-derived growth factor B-chain mRNA and peripheral vascular resistance .
|
-
- HY-13106A
-
|
EMA401 sodium; PD-126055 sodium
|
Angiotensin Receptor
|
Neurological Disease
Endocrinology
|
|
Olodanrigan (EMA401) sodium is a highly selective, orally active, peripherally restricted angiotensin II type 2 receptor (AT2R) antagonist. Olodanrigan sodium is under development as a neuropathic pain therapeutic agent. Olodanrigan sodium analgesic action appears to involve inhibition of augmented AngII/AT2R induced p38 and p42/p44 MAPK activation, and hence inhibition of DRG neuron hyperexcitability and sprouting of DRG neurons .
|
-
- HY-P1220
-
|
|
Sodium Channel
|
Neurological Disease
|
|
Huwentoxin-IV is a potent and selective sodium channel blocker, inhibits neuronal Nav1.7, Nav1.2, Nav1.3 and Nav1.4 with IC50s of 26, 150, 338 and 400 nM, respectively. Huwentoxin-IV preferentially blocks peripheral nerve subtype Nav1.7 by binding neurotoxin receptor site 4. Huwentoxin-IV has analgesic effects on animal models of inflammatory and neuropathic pain .
|
-
- HY-P1220A
-
|
|
Sodium Channel
|
Neurological Disease
|
|
Huwentoxin-IV TFA is a potent and selective sodium channel blocker, inhibits neuronal Nav1.7, Nav1.2, Nav1.3 and Nav1.4 with IC50s of 26, 150, 338 and 400 nM, respectively. Huwentoxin-IV TFA preferentially blocks peripheral nerve subtype Nav1.7 by binding neurotoxin receptor site 4. Huwentoxin-IV TFA has analgesic effects on animal models of inflammatory and neuropathic pain .
|
-
- HY-B0002BS1
-
|
GR 38032-d3; SN 307-d3
|
5-HT Receptor
Isotope-Labeled Compounds
|
Neurological Disease
|
|
Ondansetron-d3 is the deuterium labeled Ondansetron (HY-B0002B ). Ondansetron (GR 38032; SN 307) is a highly selective 5-HT3 receptor antagonist with an IC50 value of 103 pM. Ondansetron exerts its antiemetic effect by antagonizing 5-HT receptors located in localized neurons in the peripheral and central nervous systems. Ondansetron can inhibit nausea and vomiting induced by chemotherapy and radiotherapy .
|
-
- HY-P1106A
-
|
|
CFTR
|
Cardiovascular Disease
|
|
K41498 TFA is a highly selective CRF 2 receptor antagonist, with a Ki of 0.66 nM for human CRF2α receptor and a Ki of 0.62 nM for human CRF2β receptor. K41498 TFA inhibits cAMP accumulation in cells expressing CRF2. K41498 TFA antagonizes the hypotensive response induced by systemic administration of urocortin in conscious rats. K41498 TFA undergoes radioiodination without loss of activity and serves for autoradiographic studies of native CRF2 receptors in rat brain and peripheral tissues .
|
-
- HY-17436
-
|
|
Calcium Channel
|
Cardiovascular Disease
Cancer
|
|
Clevidipine is a selective, short-acting L-type calcium channel antagonist with an IC50 of 7.1 nM. Clevidipine can competitively bind to calcium channels and exert rapid vasoselective vasodilation by blocking the influx of extracellular calcium ions, thereby reducing peripheral vascular resistance and effectively controlling acute severe hypertension. Clevidipine can also protect the myocardium from reperfusion injury by promoting the release of nitric oxide (NO). Clevidipine can be used in the research of acute hypertension, perioperative blood pressure management, and myocardial ischemia-reperfusion injury .
|
-
- HY-10061BR
-
|
AZD-3355 hydrochloride (Standard)
|
GABA Receptor
Reference Standards
|
Metabolic Disease
|
|
Lesogaberan (hydrochloride) (Standard) is the analytical standard of Lesogaberan (hydrochloride) (HY-10061B). This product is intended for research and analytical applications. Lesogaberan (AZD-3355) hydrochloride is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptor. The affinity (Kis) of Lesogaberan hydrochloride for rat GABAB and GABAA receptors, as measured by displacement of [3H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan hydrochloride inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action .
|
-
- HY-B0002BS
-
|
GR 38032-d5; SN 307-d5
|
5-HT Receptor
Isotope-Labeled Compounds
|
Neurological Disease
|
|
Ondansetron-d5 is the deuterium labeled Ondansetron (HY-B0002B). Ondansetron (GR 38032; SN 307) is a highly selective 5-HT3 receptor antagonist with an IC50 value of 103 pM. Ondansetron exerts its antiemetic effect by antagonizing 5-HT receptors located in localized neurons in the peripheral and central nervous systems. Ondansetron can inhibit nausea and vomiting induced by chemotherapy and radiotherapy .
|
-
- HY-B0002BR
-
|
GR 38032 (Standard); SN 307 (Standard)
|
Reference Standards
5-HT Receptor
|
Neurological Disease
Cancer
|
|
Ondansetron (Standard) is the analytical standard of Ondansetron (HY-B0002B). This product is intended for research and analytical applications. Ondansetron (GR 38032; SN 307) is a highly selective 5-HT3 receptor antagonist with an IC50 value of 103 pM. Ondansetron exerts its antiemetic effect by antagonizing 5-HT receptors located in localized neurons in the peripheral and central nervous systems. Ondansetron can inhibit nausea and vomiting induced by chemotherapy and radiotherapy .
|
-
- HY-B1021R
-
|
|
Reference Standards
Free Fatty Acid Receptor
|
Cardiovascular Disease
Metabolic Disease
|
|
Vincamine (Standard) is the analytical standard of Vincamine. This product is intended for research and analytical applications. Vincamine is a monoterpenoid indole alkaloid extracted from the Madagascar periwinkle. Vincamine is a peripheral vasodilator and exerts a selective vasoregulator action on the brain microcapilar circulation . Vincamine is a GPR40 agonist and acts as a β-cell protector by ameliorating β-cell dysfunction and promoting glucose-stimulated insulin secretion (GSIS). Vincamine improves glucose homeostasis in vivo, and has the potential for the type 2 diabetes mellitus (T2DM) research .
|
-
- HY-N18471
-
|
5,7-DHP
|
Monoamine Oxidase
5-HT Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
5,7-Dihydroxytryptamine (5,7-DHP) is an autofluorescent (λex≈365 nm), selective neurotoxin and a transport substrate for MAO-A and 5-HT. 5,7-Dihydroxytryptamine can specifically target and damage central and peripheral 5-HTergic neurons, while affecting 5-HT-related pathways and neurotransmitter balance. 5,7-Dihydroxytryptamine can be used to establish 5-HTergic neuron injury models for studies on neural development, neurodegenerative diseases, as well as mechanisms related to platelet function and retinal neurons .
|
-
- HY-B0002BS2
-
|
GR 38032-13C,d3; SN 307-13C,d3
|
Isotope-Labeled Compounds
5-HT Receptor
|
Neurological Disease
|
|
Ondansetron- 13C,d3 is the 13C- and deuterium labeled Ondansetron (HY-B0002B). Ondansetron (GR 38032; SN 307) is a highly selective 5-HT3 receptor antagonist with an IC50 value of 103 pM. Ondansetron exerts its antiemetic effect by antagonizing 5-HT receptors located in localized neurons in the peripheral and central nervous systems. Ondansetron can inhibit nausea and vomiting induced by chemotherapy and radiotherapy .
|
-
- HY-110206
-
|
|
Cannabinoid Receptor
|
Metabolic Disease
|
|
AM6545 is a highly selective, brain-free (peripherally active) CB1 receptor antagonist (Ki=1.7 nM). AM6545 inhibits endocannabinoid signaling by competitively antagonizing CB1 receptors, inhibiting CB1-mediated appetite stimulation and inflammatory responses without affecting cAMP levels. AM6545 significantly reduces food intake and body weight in mice, while improving metabolic syndrome-related renal impairment (such as proteinuria, fibrosis) and insulin resistance. AM6545 can be used in the study of obesity and its complications .
|
-
- HY-P10587
-
|
JNJ-77242113; JNJ-2113; PN-235
|
Interleukin Related
STAT
IFNAR
|
Inflammation/Immunology
|
|
Icotrokinra (JNJ-77242113) is an orally available, selective antagonist of the IL-23 receptor. Icotrokinra inhibits IL-23-induced STAT3 phosphorylation in peripheral blood mononuclear cells (IC50=5.6 pM) and inhibits IL-23-induced interferon IFN-γ production in NK cells with an IC50 of 18.4 pM. Icotrokinra exhibits anti-inflammatory activity in a rat TNBS-induced colitis model. Icotrokinra can be used in the study of psoriasis, psoriatic arthritis, and inflammatory bowel disease .
|
-
- HY-163746
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
BuChE-IN-11 (Compound 3b-1) is an selective BuChE inhibitor with an IC50 of 0.44 μM for hBuChE. BuChE-IN-11 has high blood-brain barrier permeability and exhibits strong antioxidant activity due to its free radical scavenging properties. BuChE-IN-11 interacts with the choline binding site, acetyl binding site, and peripheral anionic site, exhibiting submicromolar BuChE inhibitory activity and preventing β-amyloid (Aβ) self-aggregation. BuChE-IN-11 holds promise for research in the field of Alzheimer's disease .
|
-
- HY-P10587A
-
|
JNJ-77242113 acetate; JNJ-2113 acetate; PN-235 acetate
|
Interleukin Related
STAT
IFNAR
|
Inflammation/Immunology
|
|
Icotrokinra (JNJ-77242113) acetate is an orally available, selective antagonist of the IL-23 receptor. Icotrokinra acetate inhibits IL-23-induced STAT3 phosphorylation in peripheral blood mononuclear cells (IC50=5.6 pM) and inhibits IL-23-induced interferon IFN-γ production in NK cells with an IC50 of 18.4 pM. Icotrokinra acetate exhibits anti-inflammatory activity in a rat TNBS-induced colitis model. Icotrokinra acetate can be used in the study of psoriasis, psoriatic arthritis, and inflammatory bowel disease .
|
-
- HY-123497
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
R116031 is a selective Neurokinin-1 (NK-1) receptor antagonist with a Ki of 0.45 nM for human NK-1 receptor. R116031 inhibits Substance P (HY-P0201)-induced peripheral effects (skin reactions and plasma extravasation in guinea pigs) and a central effect (thumping in gerbils).R116031 labeled with 3H significantly accumulate in the striatum, olfactory tubercule, olfactory bulb and locus coeruleus in gerbils models. R116031 can be used as a positron emission tomography (PET) ligand for PET imaging .
|
-
- HY-P992450
-
|
|
TNF Receptor
|
Cancer
|
|
REGN6569 is a fully human IgG1 monoclonal antibody targeting glucocorticoid-induced tumor necrosis factor receptor-related protein (GITR) with high specificity for GITR. REGN6569 exerts stronger in vitro antibody-dependent cell-mediated cytotoxicity (ADCC) against regulatory T cells expressing GITR. REGN6569 selectively depletes regulatory T cells via antibody-dependent cell-mediated cytotoxicity and increases the proportion of proliferative natural killer (NK) cells in peripheral blood. REGN6569 is applicable for advanced solid malignancies. Isotype control: HY-P99001 .
|
-
- HY-14280A
-
|
|
COMT
|
Neurological Disease
Cancer
|
|
Entacapone sodium salt is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone sodium salt inhibits COMT from rat brain, erythrocytes and liver with IC50 values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone sodium salt is selective for COMT over other catecholamine metabolizing enzymes, including MAO-A, MAO-B, phenolsulphotransferase M (PST-M) and PST-P (IC50s>50 µM). Entacapone sodium salt can be used for the research of Parkinson's disease . Entacapone sodium salt serves as as a inhibit of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders .
|
-
- HY-183301
-
|
|
Toll-like Receptor (TLR)
|
Cardiovascular Disease
|
|
TLR2/1 agonist-1 is a selective agonist of the TLR2/1 heterodimer. TLR2/1 agonist-1 acts as a hematopoietic recovery inducer to accelerate the recovery of peripheral blood cells. TLR2/1 agonist-1 serves as a G-CSF production inducer to increase serum G-CSF levels. TLR2/1 agonist-1 exhibits radioprotective effects in mice exposed to radiation. TLR2/1 agonist-1 can be used in studies related to acute radiation syndrome .
|
-
- HY-N18471A
-
|
5,7-DHP hydrobromide
|
Monoamine Oxidase
5-HT Receptor
|
Neurological Disease
|
|
5,7-Dihydroxytryptamine (5,7-DHT) hydrobromide is an autofluorescent (Ex ≈ 365 nm), selective neurotoxin and a transport substrate for MAO-A and 5-HT. 5,7-Dihydroxytryptamine hydrobromide can specifically target and damage central and peripheral 5-HTergic neurons, while affecting 5-HT-related pathways and neurotransmitter balance. 5,7-Dihydroxytryptamine hydrobromide can be used to establish 5-HTergic neuron injury models for studies on neural development, neurodegenerative diseases, as well as mechanisms related to platelet function and retinal neurons .
|
-
- HY-110391
-
|
VUF 2274
|
CCR
|
Neurological Disease
Inflammation/Immunology
|
|
BX-513 is a highly potent and selective CCR1 antagonist. BX-513 effectively inhibits the binding of radiolabeled MIP-1α and RANTES to CCR1, with Ki values of 40 nM and 60 nM, respectively. BX-513 suppresses MIP-1α-induced extracellular acidification, MIP-1α- and RANTES-induced intracellular calcium mobilization, as well as MIP-1α- and RANTES-induced migration of peripheral blood mononuclear cells. BX-513 can be used for the research of rheumatoid arthritis and multiple sclerosis .
|
-
- HY-142240
-
|
HSK16149
|
Calcium Channel
|
Neurological Disease
|
|
Crisugabalin is an orally active, selective ligand for the α2δ subunit of voltage-gated calcium channels, with a target IC50 of 3.96 nM in rats. Crisugabalin inhibits the binding of [ 3H]gabapentin to the α2δ subunit, reduces calcium influx, decreases neuronal excitability, and impairs nociceptive transmission. Crisugabalin alleviates mechanical allodynia, neuropathic pain and inflammatory pain in rats, and reduces phase II pain behaviors. Crisugabalin can be used in research related to chronic pain, neuropathic pain, diabetic neuropathy, fibromyalgia, inflammatory pain, diabetic peripheral neuropathy and postherpetic neuralgia.
|
-
- HY-136208
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
TAN-452 is an orally active, selective peripherally acting δ-opioid receptor (DOR) antagonist with a Ki of 0.47 nM and a Kb of 0.21 nM. TAN-452 is an antagonist for μ-opioid receptor (MOR; Ki=36.56 nM and Kb=9.43 nM) and κ-opioid receptor (KOR; Ki=5.31 nM and Kb=7.18 nM). TAN-452, a derivative of Naltrindole, demonstrates low brain penetrability and attenuates morphine-induced side effects without affecting pain control .
|
-
- HY-176192
-
|
|
Toll-like Receptor (TLR)
NF-κB
p38 MAPK
ERK
IKK
TNF Receptor
Interleukin Related
|
Inflammation/Immunology
|
|
SMU-14a is a selective Toll-like receptor 3 (TLR3) inhibitor wirh an IC50 of 0.18 μM. SMU-14a reduces phosphorylation of p65, ERK, and TBK1 via NF-κB, MAPK, and IRF3 signaling pathways. SMU-14a inhibits IL-6 secretion in mouse peritoneal macrophages, downregulates TNF-α in human peripheral blood monocytes and decreases serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels. SMU-14a can be used for the research of acute hepatitis .
|
-
- HY-14280
-
|
|
COMT
|
Neurological Disease
Cancer
|
|
Entacapone is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone inhibits COMT from rat brain, erythrocytes and liver with IC50 values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone is selective for COMT over other catecholamine metabolizing enzymes, including MAO-A, MAO-B, phenolsulphotransferase M (PST-M) and PST-P (IC50s>50 μM). Entacapone can be used for the research of Parkinson's disease . Entacapone serves as a inhibitor of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders .
|
-
- HY-P990197
-
|
|
L-Selectin
|
Metabolic Disease
Inflammation/Immunology
|
|
Anti-Mouse MAdCAM-1 Antibody (MECA-367) is an anti-mouse MAdCAM-1 IgG2a monoclonal antibody. Anti-Mouse MAdCAM-1 Antibody (MECA-367) significantly inhibits the migration of pig peripheral blood lymphocytes (PBL) by blocking the function of MAdCAM-1. Anti-Mouse MAdCAM-1 Antibody (MECA-367) selectively inhibits B cell migration to exacerbate inflammation. Anti-Mouse MAdCAM-1 Antibody (MECA-367) can be used for researches on inflammation, metabolic conditions and xenotransplantation such as colitis and diabetes .
|
-
- HY-N18471B
-
|
5,7-DHP creatinine sulfate
|
Monoamine Oxidase
5-HT Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
5,7-Dihydroxytryptamine creatinine sulfate (5,7-DHT) is an autofluorescent (Ex ≈ 365 nm), selective neurotoxin and a transport substrate for MAO-A and 5-HT. 5,7-Dihydroxytryptamine creatinine sulfate can specifically target and damage central and peripheral 5-HTergic neurons, while affecting 5-HT-related pathways and neurotransmitter balance. 5,7-Dihydroxytryptamine creatinine sulfate can be used to establish 5-HTergic neuron injury models for studies on neural development, neurodegenerative diseases, as well as mechanisms related to platelet function and retinal neurons .
|
-
- HY-125387
-
|
|
Src
|
Inflammation/Immunology
|
|
TOP1210 is a narrow-spectrum tyrosine kinase inhibitor with potent inhibitory activity against P38α, Src, and Syk kinases. TOP1210 effectively reduced proinflammatory cytokines released by peripheral blood monocytes, primary macrophages, HT29 cells, inflammatory cells in ulcerative colitis (UC) biopsies, and myofibroblasts isolated from inflamed colonic UC mucosa. TOP1210 showed significant anti-inflammatory effects in cell experiments and UC biopsies, superior to some selective kinase inhibitors. The multi-kinase inhibition of TOP1210 provides the possibility of obtaining a wider range of therapeutic effects, especially in the regulation of autoimmune responses .
|
-
- HY-B0197
-
|
GR-85548A
|
5-HT Receptor
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
|
|
Naratriptan is an orally active and selective 5-HT1B/1D receptor agonist. Naratriptan is peripherally active and has good oral bioavailability, inducing cranial artery vasoconstriction by activating 5-HT1B/1D receptors (EC50=0.11 μM for dog basilar artery). Naratriptan also inhibits trigeminal nerve-mediated dural neurogenic plasma extravasation and reduces sterile inflammation. Naratriptan is mainly used in the research of acute migraine, targeting cranial vascular and neuroinflammatory mechanisms .
|
-
- HY-137055
-
|
|
Others
|
Others
|
|
PF-3774076 is a highly central nervous system (CNS) penetrant, potent, and selective human α1A-adrenoceptor partial agonist. It exhibits good potency and selectivity in multiple binding and functional assays. PF-3774076 increases peak urethral pressure in anesthetized female dogs in a dose-dependent manner via a central mechanism. PF-3774076 affects both the proximal and distal portions of the urethra in vivo. These properties suggest that PF-3774076 may have significant benefit in the treatment of stress urinary incontinence (SUI) as a CNS-penetrant α1A receptor partial agonist. However, despite its partial agonism and selectivity for α1A receptors, PF-3774076 failed to provide adequate safety differences in in vivo models of cardiovascular function. This may be due to the simultaneous activation of both peripheral and central α1A receptors. These data suggest that while central α1A partial agonists may have significant benefit in the treatment of SUI, this class of agents may have difficulty achieving the desired urethral selectivity without affecting cardiovascular function.
|
-
- HY-A0144A
-
|
|
Adrenergic Receptor
AMPK
Akt
|
Cardiovascular Disease
|
|
Etilefrine hydrochloride is a sympathetic nerve agonist and AMPK activator that selectively targets α1/β1 adrenergic receptors. Etilefrine hydrochloride stimulates α1 adrenergic receptors, leading to contraction of vascular smooth muscle and increased peripheral resistance. Etilefrine hydrochloride also stimulates β1 receptors to enhance myocardial contractility and increase heart rate, thereby increasing blood pressure and improving cardiac output. Etilefrine hydrochloride also bidirectionally regulates the AMPK/Akt pathway and modulates the phosphorylation levels. Etilefrine hydrochloride can be used in cardiovascular research, such as postural hypotension, chylothorax, and improving low cardiac output .
|
-
- HY-A0144
-
|
|
Adrenergic Receptor
AMPK
Akt
|
Cardiovascular Disease
|
|
Etilefrine is a sympathetic nerve agonist and AMPK activator that selectively targets α1/β1 adrenergic receptors. Etilefrine stimulates α1 adrenergic receptors, leading to contraction of vascular smooth muscle and increased peripheral resistance. Etilefrine also stimulates β1 receptors to enhance myocardial contractility and increase heart rate, thereby increasing blood pressure and improving cardiac output. Etilefrine also bidirectionally regulates the AMPK/Akt pathway and modulates the phosphorylation levels. Etilefrine can be used in cardiovascular research, such as postural hypotension, chylothorax, and improving low cardiac output .
|
-
- HY-B0197A
-
|
GR-85548A hydrochloride
|
5-HT Receptor
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
|
|
Naratriptan (GR-85548A) hydrochloride is a selective 5-HT1B/1D receptor agonist. Naratriptan hydrochloride is peripherally active and has good oral bioavailability, inducing cranial artery vasoconstriction by activating 5-HT1B/1D receptors (EC50=0.11 μM for dog basilar artery). Naratriptan hydrochloride also inhibits trigeminal nerve-mediated dural neurogenic plasma extravasation and reduces sterile inflammation. Naratriptan hydrochloride is mainly used in the research of acute migraine, targeting cranial vascular and neuroinflammatory mechanisms .
|
-
- HY-14280S
-
|
|
COMT
|
Neurological Disease
|
|
Entacapone-d10 is the deuterium labeled Entacapone. Entacapone is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone inhibits COMT from rat brain, erythrocytes and liver with IC50 values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone is selective for COMT over other catecholamine metabolizing enzymes, including MAO-A, MAO-B, phenolsulphotransferase M (PST-M) and PST-P (IC50s>50 μM). Entacapone can be used for the research of Parkinson's disease . Entacapone serves as a inhibitor of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders .
|
-
- HY-13224A
-
|
|
Endogenous Metabolite
|
Cancer
|
|
AZD4877 hydrochloride is a synthetic dynein inhibitor with potential anti-tumor activity. AZD4877 selectively inhibits the microtubule dynein KSP (also known as kinesin-5 or Eg5), which may lead to inhibition of mitotic spindle assembly. The action of AZD4877 may activate the spindle assembly checkpoint, leading to cell cycle arrest at the mitotic stage. AZD4877 may induce cell death in actively dividing tumor cells. AZD4877 may be less likely to cause peripheral neuropathy associated with microtubule-targeted compounds as it is not involved in post-mitotic processes. AZD4877 is essential for the formation of bipolar spindles and the proper segregation of sister chromosomes .
|
-
- HY-14280R
-
|
|
Reference Standards
COMT
|
Neurological Disease
Cancer
|
|
Entacapone (Standard) is the analytical standard of Entacapone. This product is intended for research and analytical applications. Entacapone is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone inhibits COMT from rat brain, erythrocytes and liver with IC50 values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone is selective for COMT over other catecholamine metabolizing enzymes, including MAO-A, MAO-B, phenolsulphotransferase M (PST-M) and PST-P (IC50s>50 µM). Entacapone can be used for the research of Parkinson's disease . Entacapone serves as a inhibitor of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders .
|
-
- HY-15322
-
|
P505-15; PRT-2607; BIIB-057
|
Syk
Apoptosis
Caspase
|
Inflammation/Immunology
Cancer
|
|
PRT062607 (P505-15; PRT-2607) is an orally active ATP-competitive Syk inhibitor with an IC50 value of 1 nM, and exhibits at least 80-fold selectivity over other kinases. PRT062607 blocks B cell antigen receptor-mediated activation, Fcε receptor 1-mediated basophil degranulation and microglial phagocytosis, and induces caspase-dependent apoptosis and microglial death. PRT062607 inhibits tumor growth and peripheral nerve injury-induced mechanical allodynia, and prevents neuronal loss. PRT062607 can be used in research related to rheumatoid arthritis, chronic lymphocytic leukemia, non-Hodgkin's lymphoma, neurodegenerative diseases and neuropathic pain .
|
-
- HY-A0144R
-
|
|
Adrenergic Receptor
AMPK
Akt
Reference Standards
|
Cardiovascular Disease
|
|
Etilefrine (Standard) is the analytical standard of Etilefrine. This product is intended for research and analytical applications. Etilefrine is a sympathetic nerve agonist and AMPK activator that selectively targets α1/β1 adrenergic receptors. Etilefrine stimulates α1 adrenergic receptors, leading to contraction of vascular smooth muscle and increased peripheral resistance. Etilefrine also stimulates β1 receptors to enhance myocardial contractility and increase heart rate, thereby increasing blood pressure and improving cardiac output. Etilefrine also bidirectionally regulates the AMPK/Akt pathway and modulates the phosphorylation levels. Etilefrine can be used in cardiovascular research, such as postural hypotension, chylothorax, and improving low cardiac output .
|
-
- HY-177338
-
|
|
STING
Cyclic GMP-AMP Synthase
IFNAR
TNF Receptor
Interleukin Related
|
Inflammation/Immunology
Cancer
|
|
STING agonist-45 is a selective STING agonist (EC50 = 0.28 μM). STING agonist-45 activates the innate immune response through the cGAS-STING pathway, upregulating key markers such as p-TBK1 and IRF3. STING agonist-45 exhibits robust STING activation in human peripheral blood mononuclear cells (PBMCs), inducing the production of type I interferons (such as IFN-β) and downstream cytokines (such as TNF-α and IL-6). STING agonist-45 enhances anti-tumor immunity, inhibits tumor growth, and increases CD8 + T cell infiltration in mouse models. STING agonist-45 is promising for the study of STING-related diseases .
|
-
- HY-A0144AR
-
|
|
Reference Standards
AMPK
Adrenergic Receptor
Akt
|
Cardiovascular Disease
|
|
Etilefrine hydrochloride (Standard) is the analytical standard of Etilefrine hydrochloride (HY-A0144A). This product is intended for research and analytical applications. Etilefrine hydrochloride is a sympathetic nerve agonist and AMPK activator that selectively targets α1/β1 adrenergic receptors. Etilefrine hydrochloride stimulates α1 adrenergic receptors, leading to contraction of vascular smooth muscle and increased peripheral resistance. Etilefrine hydrochloride also stimulates β1 receptors to enhance myocardial contractility and increase heart rate, thereby increasing blood pressure and improving cardiac output. Etilefrine hydrochloride also bidirectionally regulates the AMPK/Akt pathway and modulates the phosphorylation levels. Etilefrine hydrochloride can be used in cardiovascular research, such as postural hypotension, chylothorax, and improving low cardiac output .
|
-
- HY-126031
-
|
|
DAGL
|
Inflammation/Immunology
|
|
(R)-KT109 is a peripherally restricted serine hydrolase inhibitor that cannot cross the blood-brain barrier. (R)-KT109 irreversibly inhibits ABHD6, DAGLα and DAGLβ via carbamoylation of the active-site serine. (R)-KT109 exerts selective inhibitory effects on serine hydrolases in mouse brains, with pIC50 values of 8.6, 9.1 and 8.2 against human ABHD6, DAGLα and DAGLβ, respectively. (R)-KT109 effectively reduces the levels of 2-arachidonoylglycerol, arachidonic acid, eicosanoids and TNF-α. (R)-KT109 is widely used in studies of metabolic syndrome-related diseases and neuroinflammation .
|
-
- HY-B0197S
-
|
GR-85548A-d3-1
|
5-HT Receptor
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
|
|
Naratriptan-d3 (GR-85548A-d3) is the deuterium labeled Naratriptan (HY-B0197). Naratriptan is a selective 5-HT1B/1D receptor agonist. Naratriptan is peripherally active and has good oral bioavailability, inducing cranial artery vasoconstriction by activating 5-HT1B/1D receptors (EC50=0.11 μM for dog basilar artery). Naratriptan also inhibits trigeminal nerve-mediated dural neurogenic plasma extravasation and reduces sterile inflammation. Naratriptan is mainly used in the research of acute migraine, targeting cranial vascular and neuroinflammatory mechanisms .
|
-
- HY-B0197AR
-
|
GR-85548A hydrochloride (Standard)
|
Reference Standards
5-HT Receptor
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
|
|
Naratriptan (GR-85548A) hydrochloride (Standard) is the analytical standard of Naratriptan hydrochloride (HY-B0197A). This product is intended for research and analytical applications. Naratriptan is a selective 5-HT1B/1D receptor agonist. Naratriptan is peripherally active and has good oral bioavailability, inducing cranial artery vasoconstriction by activating 5-HT1B/1D receptors (EC50=0.11 μM for dog basilar artery). Naratriptan also inhibits trigeminal nerve-mediated dural neurogenic plasma extravasation and reduces sterile inflammation. Naratriptan is mainly used in the research of acute migraine, targeting cranial vascular and neuroinflammatory mechanisms .
|
-
- HY-B0197AS
-
|
GR-85548A d3
|
5-HT Receptor
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
|
|
Naratriptan-d3 (GR-85548A-d3) is the deuterium labeled Naratriptan hydrochloride (HY-B0197A). Naratriptan hydrochloride is a selective 5-HT1B/1D receptor agonist. Naratriptan hydrochloride is peripherally active and has good oral bioavailability, inducing cranial artery vasoconstriction by activating 5-HT1B/1D receptors (EC50=0.11 μM for dog basilar artery). Naratriptan hydrochloride also inhibits trigeminal nerve-mediated dural neurogenic plasma extravasation and reduces sterile inflammation. Naratriptan hydrochloride is mainly used in the research of acute migraine, targeting cranial vascular and neuroinflammatory mechanisms .
|
-
- HY-186072
-
|
|
NOD-like Receptor (NLR)
Interleukin Related
Cytochrome P450
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
NT-0527 is a selective, orally active, and brain-permeable NLRP3 inflammasome inhibitor. NT-0527 can specifically block the formation of the NLRP3 inflammasome, resulting in the reduction in the maturation and release of IL-1β, exhibit inhibition on CYP2C19. NT-0527 displays anti-inflammatory activity in the mouse LPS (HY-D1056) /ATP (HY-B2176)-induced peritonitis model. NT-0527 can be used for the research of neuroinflammatory disorders (Parkinson's disease, Alzheimer's disease, amyotrophic lateral sclerosis) and peripheral inflammatory disorders (type II diabetes, atherosclerosis, gout, etc.) associated with NLRP3 inflammasome .
|
-
- HY-P1723
-
Spexin
2 Publications Verification
Neuropeptide Q
|
Neuropeptide Y Receptor
Apoptosis
Ferroptosis
Autophagy
|
Cardiovascular Disease
Neurological Disease
|
|
Spexin (Neuropeptide Q) is a selective agonist of galanin receptors GAL2 and GAL3, and is a conserved peptide that functions as a neurotransmitter/neuromodulator and endocrine factor. Spexin can function through both central and peripheral actions. Spexin upregulates Beclin 1 to inhibit ferroptosis induced by excessive autophagy, reduces the uptake of long-chain fatty acids by adipocytes, and regulates energy metabolism by increasing lipid oxidation (e.g., reducing the respiratory exchange ratio in rodents). Spexin improves cardiac function in the Doxorubicin hydrochloride (HY-15142)-induced cardiotoxicity model, protects mitochondrial membrane potential, and reduces iron accumulation and lipid peroxidation. Spexin can be used to study obesity and its related metabolic disorders, cardiovascular diseases (e.g., cardioprotection), and side effects of tumor chemotherapy .
|
-
- HY-155297
-
|
FLA-136
|
Histamine Receptor
|
Cardiovascular Disease
|
|
Nebidrazine is a centrally-acting hypotensive agent compared to clonidine, demonstrating weaker cardiovascular effects in rats. It induces dose-dependent hypotension and bradycardia when administered intracerebroventricularly (i.c.v.), with significantly lower sedative potential than clonidine in conscious rats. Yohimbine attenuates the cardiovascular effects of both Nebidrazine and clonidine, suggesting involvement of central alpha-autoreceptors sensitive to yohimbine. Unlike clonidine, Nebidrazine does not affect peripheral alpha-adrenoceptors in pithed rats, indicating a selective central mechanism. Chemical sympathectomy reduces Nebidrazine's cardiovascular effects more than clonidine's, and metiamide diminishes responses to both drugs, implicating central histamine receptors. These findings highlight Nebidrazine's distinct pharmacological profile and potential therapeutic application in managing hypertension through central alpha-autoreceptor stimulation .
|
-
- HY-P1723A
-
|
Neuropeptide Q TFA
|
Neuropeptide Y Receptor
Apoptosis
Ferroptosis
Autophagy
|
Cardiovascular Disease
Metabolic Disease
|
|
Spexin (Neuropeptide Q) TFA is a selective agonist of galanin receptors GAL2 and GAL3, and is a conserved peptide that functions as a neurotransmitter/neuromodulator and endocrine factor. Spexin TFA can function through both central and peripheral actions. Spexin TFA upregulates Beclin 1 to inhibit ferroptosis induced by excessive autophagy, reduces the uptake of long-chain fatty acids by adipocytes, and regulates energy metabolism by increasing lipid oxidation (e.g., reducing the respiratory exchange ratio in rodents). Spexin TFA improves cardiac function in the Doxorubicin hydrochloride (HY-15142)-induced cardiotoxicity model, protects mitochondrial membrane potential, and reduces iron accumulation and lipid peroxidation. Spexin TFA can be used to study obesity and its related metabolic disorders, cardiovascular diseases (e.g., cardioprotection), and side effects of tumor chemotherapy .
|
-
- HY-P5640
-
|
|
Bacterial
Parasite
|
Infection
|
|
Tritrpticin is a porcine-derived antimicrobial peptide with properties such as membrane disruption and hemolysis. Tritrpticin disrupts the cell membranes of bacteria, fungi and Jurkat T cell leukemia cells and induces their death. Tritrpticin also enhances the efficacy of Metronidazole (HY-B0318) against *Trichomonas vaginalis*, reduces plasma endotoxin and inflammatory cytokine levels, restricts bacterial growth in blood and visceral tissues, decreases the mortality rate of septic shock in rats and enhances the therapeutic effect of ertapenem. Tritrpticin exhibits selective cytotoxicity against Jurkat T cell leukemia cells, while showing low toxicity to normal peripheral blood mononuclear cells and red blood cells, and can serve as a template for antimicrobial peptide design. Tritrpticin can be applied to research related to bacterial infections, fungal infections, trichomoniasis, septic shock and leukemia .
|
-
- HY-179047
-
|
|
Toll-like Receptor (TLR)
MyD88
IKK
p38 MAPK
ERK
TNF Receptor
Interleukin Related
|
Inflammation/Immunology
Cancer
|
|
SMU-L11-R is a selective TLR7 agonist with an EC50 of 0.012 μM for human TLR7. SMU-L11-R specifically activates TLR7, recruits MyD88, and triggers MAPK/NF-κB pathways, leading to TNF-α/IL-1β/IL-6 secretion in both mouse and human peripheral blood mononuclear cells. SMU-L11-R promotes M1-like macrophage polarization. SMU-L11-R exhibits excellent synergistic anti-tumor effects with PD-L1 inhibitors by upregulating CD8 +T cells. SMU-L11-R shows potential in colorectal cancer studies .
|
-
- HY-14977
-
|
|
LPL Receptor
|
Inflammation/Immunology
|
|
CS-0777-P, the phosphorylated form of CS-0777, acts as a potent and selective modulator of the S1P receptor-1 (S1P1). It exhibits approximately 320-fold higher agonist activity for human S1P1 compared to S1P3, with an EC50 of 1.1 nM. In pharmacological studies, CS-0777-P demonstrated significant effects in vitro as an S1P1 and S1P3 agonist, leading to lowered peripheral blood lymphocyte counts and suppressive effects on experimental autoimmune encephalomyelitis (EAE) in rats. Pharmacokinetic studies in rats revealed rapid lymphocyte count reductions following oral administration, making CS-0777 a promising candidate currently undergoing clinical trials for the treatment of multiple sclerosis (MS) .
|
-
- HY-118917
-
|
|
IMPDH
|
Inflammation/Immunology
|
|
VX-148 is an orally active immunosuppressant, which is a non-competitive inosine-5'-monophosphate dehydrogenase (IMPDH) inhibitor with Ki values for IMPDH Ⅱ and IMPDH Ⅰ of 6 and 14 nM respectively. VX-148 can significantly inhibit the proliferation of human peripheral blood mononuclear cells (PBMC) stimulated by T-cell mitogen (PHA) or B-cell mitogen (SPAS). VX-148 has high selectivity for lymphocytes (such as L1210, Jurkat T cells, and Raji B cells), but has no significant toxicity to non-lymphoid cells. VX-148 can inhibit antibody responses in mouse models and significantly prolong the survival time of transplanted skin in allogeneic skin transplantation models. VX-148 can be used in the research of autoimmune diseases (such as rheumatoid arthritis, psoriasis) and organ transplantation anti-rejection .
|
-
- HY-14604
-
|
SR57746A; SR57746 hydrochloride
|
5-HT Receptor
Dopamine Receptor
Trk Receptor
PKC
ERK
Akt
JNK
|
Neurological Disease
Metabolic Disease
|
|
Xaliproden (SR57746) hydrochloride (SR57746A) is an orally active, highly selective 5-HT1A receptor agonist. Xaliproden hydrochloride activates pertussis toxin-sensitive G protein-coupled signaling cascades, as well as the PKC, ERK1/ERK2, Akt and p21 Ras/MEK-1 pathways. Xaliproden hydrochloride also downregulates the JNK/p66/c-Jun signaling pathway, induces phosphorylation of the shc adaptor protein, regulates extracellular dopamine and 5-HT levels, and induces [ 35S]GTPγS labeling in rat brain structures rich in 5-HT1A receptors. Xaliproden hydrochloride exerts neurotrophic, neuroprotective, renoprotective, anti-inflammatory, anti-apoptotic, anti-fibrotic and analgesic effects. Xaliproden hydrochloride also enhances NGF-induced neurite outgrowth, promotes motor neuron survival, attenuates renal tubular injury and inhibits chemotherapy-induced mechanical allodynia, without activating or altering NGF-induced TrkA receptor activation. Xaliproden hydrochloride can be used in the research of motor neuron disease, diabetic nephropathy, chemotherapy-induced peripheral neuropathy, amyotrophic lateral sclerosis, Alzheimer's disease, acute tonic nociceptive pain, inflammatory pain, depression and anxiety .
|
-
- HY-119820
-
|
SR57746A free base
|
Akt
Dopamine Receptor
Trk Receptor
5-HT Receptor
PKC
JNK
ERK
|
Neurological Disease
|
|
Xaliproden (SR57746) free base is an orally active, highly selective 5-HT1A receptor agonist. Xaliproden free base activates pertussis toxin-sensitive G protein-coupled signaling cascades, as well as the PKC, ERK1/ERK2, Akt and p21 Ras/MEK-1 pathways. Xaliproden free base also downregulates the JNK/p66/c-Jun signaling pathway, induces phosphorylation of the shc adaptor protein, regulates extracellular dopamine and 5-HT levels, and induces [ 35S]GTPγS labeling in rat brain structures rich in 5-HT1A receptors. Xaliproden free base exerts neurotrophic, neuroprotective, renoprotective, anti-inflammatory, anti-apoptotic, anti-fibrotic and analgesic effects. Xaliproden free base also enhances NGF-induced neurite outgrowth, promotes motor neuron survival, attenuates renal tubular injury and inhibits chemotherapy-induced mechanical allodynia, without activating or altering NGF-induced TrkA receptor activation. Xaliproden free base can be used in the research of motor neuron disease, diabetic nephropathy, chemotherapy-induced peripheral neuropathy, amyotrophic lateral sclerosis, Alzheimer's disease, acute tonic nociceptive pain, inflammatory pain, depression and anxiety .
|
-
- HY-14604R
-
|
SR57746A (Standard); SR57746 hydrochloride (Standard)
|
Reference Standards
Akt
Dopamine Receptor
Trk Receptor
5-HT Receptor
PKC
JNK
ERK
|
Neurological Disease
Cancer
|
|
Xaliproden (hydrochloride) (Standard) is the analytical standard of Xaliproden (hydrochloride). This product is intended for research and analytical applications. Xaliproden (SR57746) hydrochloride (SR57746A) is an orally active, highly selective 5-HT1A receptor agonist. Xaliproden hydrochloride activates pertussis toxin-sensitive G protein-coupled signaling cascades, as well as the PKC, ERK1/ERK2, Akt and p21 Ras/MEK-1 pathways. Xaliproden hydrochloride also downregulates the JNK/p66/c-Jun signaling pathway, induces phosphorylation of the shc adaptor protein, regulates extracellular dopamine and 5-HT levels, and induces [ 35S]GTPγS labeling in rat brain structures rich in 5-HT1A receptors. Xaliproden hydrochloride exerts neurotrophic, neuroprotective, renoprotective, anti-inflammatory, anti-apoptotic, anti-fibrotic and analgesic effects. Xaliproden hydrochloride also enhances NGF-induced neurite outgrowth, promotes motor neuron survival, attenuates renal tubular injury and inhibits chemotherapy-induced mechanical allodynia, without activating or altering NGF-induced TrkA receptor activation. Xaliproden hydrochloride can be used in the research of motor neuron disease, diabetic nephropathy, chemotherapy-induced peripheral neuropathy, amyotrophic lateral sclerosis, Alzheimer's disease, acute tonic nociceptive pain, inflammatory pain, depression and anxiety .
|
-
| Cat. No. |
Product Name |
Type |
-
- HY-A0144A
-
|
|
Biochemical Assay Reagents
|
|
Etilefrine hydrochloride is a sympathetic nerve agonist and AMPK activator that selectively targets α1/β1 adrenergic receptors. Etilefrine hydrochloride stimulates α1 adrenergic receptors, leading to contraction of vascular smooth muscle and increased peripheral resistance. Etilefrine hydrochloride also stimulates β1 receptors to enhance myocardial contractility and increase heart rate, thereby increasing blood pressure and improving cardiac output. Etilefrine hydrochloride also bidirectionally regulates the AMPK/Akt pathway and modulates the phosphorylation levels. Etilefrine hydrochloride can be used in cardiovascular research, such as postural hypotension, chylothorax, and improving low cardiac output .
|
-
- HY-A0144AR
-
|
|
Biochemical Assay Reagents
|
|
Etilefrine hydrochloride (Standard) is the analytical standard of Etilefrine hydrochloride (HY-A0144A). This product is intended for research and analytical applications. Etilefrine hydrochloride is a sympathetic nerve agonist and AMPK activator that selectively targets α1/β1 adrenergic receptors. Etilefrine hydrochloride stimulates α1 adrenergic receptors, leading to contraction of vascular smooth muscle and increased peripheral resistance. Etilefrine hydrochloride also stimulates β1 receptors to enhance myocardial contractility and increase heart rate, thereby increasing blood pressure and improving cardiac output. Etilefrine hydrochloride also bidirectionally regulates the AMPK/Akt pathway and modulates the phosphorylation levels. Etilefrine hydrochloride can be used in cardiovascular research, such as postural hypotension, chylothorax, and improving low cardiac output .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P10587
-
|
JNJ-77242113; JNJ-2113; PN-235
|
Interleukin Related
STAT
IFNAR
|
Inflammation/Immunology
|
|
Icotrokinra (JNJ-77242113) is an orally available, selective antagonist of the IL-23 receptor. Icotrokinra inhibits IL-23-induced STAT3 phosphorylation in peripheral blood mononuclear cells (IC50=5.6 pM) and inhibits IL-23-induced interferon IFN-γ production in NK cells with an IC50 of 18.4 pM. Icotrokinra exhibits anti-inflammatory activity in a rat TNBS-induced colitis model. Icotrokinra can be used in the study of psoriasis, psoriatic arthritis, and inflammatory bowel disease .
|
-
- HY-P10746
-
|
|
Neurokinin Receptor
|
Metabolic Disease
|
|
EB1002 is a highly selective, long-acting NK2R agonist. EB1002 exerts central appetite suppression, increases peripheral energy expenditure and enhances insulin sensitivity, which effectively reduces body weight, improves glucose and lipid metabolism, with favorable safety profiles. EB1002 can be used for research on diseases such as obesity and type 2 diabetes .
|
-
- HY-17609
-
|
CR-845; FE-202845
|
Opioid Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
Difelikefalin (CR-845) is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease .
|
-
- HY-P1723
-
Spexin
2 Publications Verification
Neuropeptide Q
|
Neuropeptide Y Receptor
Apoptosis
Ferroptosis
Autophagy
|
Cardiovascular Disease
Neurological Disease
|
|
Spexin (Neuropeptide Q) is a selective agonist of galanin receptors GAL2 and GAL3, and is a conserved peptide that functions as a neurotransmitter/neuromodulator and endocrine factor. Spexin can function through both central and peripheral actions. Spexin upregulates Beclin 1 to inhibit ferroptosis induced by excessive autophagy, reduces the uptake of long-chain fatty acids by adipocytes, and regulates energy metabolism by increasing lipid oxidation (e.g., reducing the respiratory exchange ratio in rodents). Spexin improves cardiac function in the Doxorubicin hydrochloride (HY-15142)-induced cardiotoxicity model, protects mitochondrial membrane potential, and reduces iron accumulation and lipid peroxidation. Spexin can be used to study obesity and its related metabolic disorders, cardiovascular diseases (e.g., cardioprotection), and side effects of tumor chemotherapy .
|
-
- HY-P3609
-
CR 665
2 Publications Verification
JNJ 38488502; FE 200665
|
Opioid Receptor
|
Neurological Disease
|
|
CR 665 (JNJ 38488502) is a peripherally selective κ-opioid agonist. CR 665 can activate the kappa opioid receptor with EC50 value of 10.9 nM. CR 665 can be used for the research of peripheral pain .
|
-
- HY-153963
-
|
|
Oxytocin Receptor
|
Endocrinology
|
|
PF-06655075 is a novel andnon–brain-penetrant oxytocin receptor agonist with increased selectivity for the oxytocin receptor and significantly increased pharmacokinetic stability. PF-06655075 can be used as a tool compound to further explore the role of peripheral oxytocin in behavioral response .
|
-
- HY-P1106A
-
|
|
CFTR
|
Cardiovascular Disease
|
|
K41498 TFA is a highly selective CRF 2 receptor antagonist, with a Ki of 0.66 nM for human CRF2α receptor and a Ki of 0.62 nM for human CRF2β receptor. K41498 TFA inhibits cAMP accumulation in cells expressing CRF2. K41498 TFA antagonizes the hypotensive response induced by systemic administration of urocortin in conscious rats. K41498 TFA undergoes radioiodination without loss of activity and serves for autoradiographic studies of native CRF2 receptors in rat brain and peripheral tissues .
|
-
- HY-P1106
-
|
|
CRFR
|
Cardiovascular Disease
|
|
K41498 is a highly selective CRF 2 receptor antagonist, with a Ki of 0.66 nM for human CRF2α receptor and a Ki of 0.62 nM for human CRF2β receptor. K41498 inhibits cAMP accumulation in cells expressing CRF2. K41498 antagonizes the hypotensive response induced by systemic administration of urocortin in conscious rats. K41498 undergoes radioiodination without loss of activity and serves for autoradiographic studies of native CRF2 receptors in rat brain and peripheral tissues .
|
-
- HY-P1220A
-
|
|
Sodium Channel
|
Neurological Disease
|
|
Huwentoxin-IV TFA is a potent and selective sodium channel blocker, inhibits neuronal Nav1.7, Nav1.2, Nav1.3 and Nav1.4 with IC50s of 26, 150, 338 and 400 nM, respectively. Huwentoxin-IV TFA preferentially blocks peripheral nerve subtype Nav1.7 by binding neurotoxin receptor site 4. Huwentoxin-IV TFA has analgesic effects on animal models of inflammatory and neuropathic pain .
|
-
- HY-P5640
-
|
|
Bacterial
Parasite
|
Infection
|
|
Tritrpticin is a porcine-derived antimicrobial peptide with properties such as membrane disruption and hemolysis. Tritrpticin disrupts the cell membranes of bacteria, fungi and Jurkat T cell leukemia cells and induces their death. Tritrpticin also enhances the efficacy of Metronidazole (HY-B0318) against *Trichomonas vaginalis*, reduces plasma endotoxin and inflammatory cytokine levels, restricts bacterial growth in blood and visceral tissues, decreases the mortality rate of septic shock in rats and enhances the therapeutic effect of ertapenem. Tritrpticin exhibits selective cytotoxicity against Jurkat T cell leukemia cells, while showing low toxicity to normal peripheral blood mononuclear cells and red blood cells, and can serve as a template for antimicrobial peptide design. Tritrpticin can be applied to research related to bacterial infections, fungal infections, trichomoniasis, septic shock and leukemia .
|
-
- HY-P10965
-
|
ZT002
|
GLP Receptor
|
Metabolic Disease
|
|
Zovaglutide (ZT002) is a long-acting, selective GLP-1 receptor agonist. Zovaglutide enhances albumin binding capacity via dual fatty acid chain modification. Zovaglutide exerts metabolic effects through central and peripheral GLP-1 pathways, thereby promoting satiety, reducing caloric intake and enhancing glucose-dependent insulin secretion, with no activity against GIP or glucagon receptors. Zovaglutide can be used in research on type 2 diabetes or obesity .
|
-
- HY-P5907
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Helianorphin-19 is a potent and selective κ-opioid receptor (KOR) activator with a Ki of 21 nM and an EC50 of 45 nM. Helianorphin-19 exhibits strong KOR-specific peripheral analgesic activity in a mouse model of chronic visceral pain .
|
-
- HY-P2696
-
|
|
Transmembrane Glycoprotein
|
Cardiovascular Disease
|
|
EP 80317 is a selective CD36 ligand. EP 80317 protects the heart against damage and dysfunction elicited by myocardial ischaemia and reperfusion (MI/R), along with a transient reduction in peripheral lipolysis. EP 80317 can be used for the study of cardiovascular disease .
|
-
- HY-P1220
-
|
|
Sodium Channel
|
Neurological Disease
|
|
Huwentoxin-IV is a potent and selective sodium channel blocker, inhibits neuronal Nav1.7, Nav1.2, Nav1.3 and Nav1.4 with IC50s of 26, 150, 338 and 400 nM, respectively. Huwentoxin-IV preferentially blocks peripheral nerve subtype Nav1.7 by binding neurotoxin receptor site 4. Huwentoxin-IV has analgesic effects on animal models of inflammatory and neuropathic pain .
|
-
- HY-P10587A
-
|
JNJ-77242113 acetate; JNJ-2113 acetate; PN-235 acetate
|
Interleukin Related
STAT
IFNAR
|
Inflammation/Immunology
|
|
Icotrokinra (JNJ-77242113) acetate is an orally available, selective antagonist of the IL-23 receptor. Icotrokinra acetate inhibits IL-23-induced STAT3 phosphorylation in peripheral blood mononuclear cells (IC50=5.6 pM) and inhibits IL-23-induced interferon IFN-γ production in NK cells with an IC50 of 18.4 pM. Icotrokinra acetate exhibits anti-inflammatory activity in a rat TNBS-induced colitis model. Icotrokinra acetate can be used in the study of psoriasis, psoriatic arthritis, and inflammatory bowel disease .
|
-
- HY-P1723A
-
|
Neuropeptide Q TFA
|
Neuropeptide Y Receptor
Apoptosis
Ferroptosis
Autophagy
|
Cardiovascular Disease
Metabolic Disease
|
|
Spexin (Neuropeptide Q) TFA is a selective agonist of galanin receptors GAL2 and GAL3, and is a conserved peptide that functions as a neurotransmitter/neuromodulator and endocrine factor. Spexin TFA can function through both central and peripheral actions. Spexin TFA upregulates Beclin 1 to inhibit ferroptosis induced by excessive autophagy, reduces the uptake of long-chain fatty acids by adipocytes, and regulates energy metabolism by increasing lipid oxidation (e.g., reducing the respiratory exchange ratio in rodents). Spexin TFA improves cardiac function in the Doxorubicin hydrochloride (HY-15142)-induced cardiotoxicity model, protects mitochondrial membrane potential, and reduces iron accumulation and lipid peroxidation. Spexin TFA can be used to study obesity and its related metabolic disorders, cardiovascular diseases (e.g., cardioprotection), and side effects of tumor chemotherapy .
|
-
- HY-153963A
-
|
|
Oxytocin Receptor
|
Endocrinology
|
|
PF-06655075 (TFA) is the TFA form of PF-06655075 (HY-153963). PF-06655075 is a novel andnon–brain-penetrant oxytocin receptor agonist with increased selectivity for the oxytocin receptor and significantly increased pharmacokinetic stability. PF-06655075 can be used as a tool compound to further explore the role of peripheral oxytocin in behavioral response .
|
-
- HY-P5869
-
|
|
Calcium Channel
Sodium Channel
|
Neurological Disease
|
|
Kurtoxin is a selective Cav3 (T-type) voltage-gated Ca 2+ channel gating inhibitor with a Kd of 15 nM for Cav3.1 (α1G T-type) Ca 2+ channel. Kurtoxin can interact with high affinity with native neuronal high-threshold L-type, N-type, and P-type Ca 2+ channels in central and peripheral neurons. Kurtoxin also shows cross-reactivity with voltage-gated Na + channel .
|
-
- HY-P2696A
-
|
|
Transmembrane Glycoprotein
|
Cardiovascular Disease
|
|
EP 80317 acetate is a selective CD36 ligand. EP 80317 acetate protects the heart against damage and dysfunction elicited by myocardial ischaemia and reperfusion (MI/R), along with a transient reduction in peripheral lipolysis. EP 80317 acetate can be used for the study of cardiovascular disease .
|
| Cat. No. |
Product Name |
Target |
Research Area |
Image |
-
- HY-P990197
-
|
|
L-Selectin
|
Metabolic Disease
Inflammation/Immunology
|
|
Anti-Mouse MAdCAM-1 Antibody (MECA-367) is an anti-mouse MAdCAM-1 IgG2a monoclonal antibody. Anti-Mouse MAdCAM-1 Antibody (MECA-367) significantly inhibits the migration of pig peripheral blood lymphocytes (PBL) by blocking the function of MAdCAM-1. Anti-Mouse MAdCAM-1 Antibody (MECA-367) selectively inhibits B cell migration to exacerbate inflammation. Anti-Mouse MAdCAM-1 Antibody (MECA-367) can be used for researches on inflammation, metabolic conditions and xenotransplantation such as colitis and diabetes .
|
-
(5)
-
- HY-P992450
-
|
|
TNF Receptor
|
Cancer
|
|
REGN6569 is a fully human IgG1 monoclonal antibody targeting glucocorticoid-induced tumor necrosis factor receptor-related protein (GITR) with high specificity for GITR. REGN6569 exerts stronger in vitro antibody-dependent cell-mediated cytotoxicity (ADCC) against regulatory T cells expressing GITR. REGN6569 selectively depletes regulatory T cells via antibody-dependent cell-mediated cytotoxicity and increases the proportion of proliferative natural killer (NK) cells in peripheral blood. REGN6569 is applicable for advanced solid malignancies. Isotype control: HY-P99001 .
|
-
(5)
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-B0468
-
-
-
- HY-B0715
-
|
BL-191; PTX; Oxpentifylline
|
Classification of Application Fields
Disease Research Fields
Cancer
|
Phosphodiesterase (PDE)
Autophagy
HIV
|
|
Pentoxifylline (BL-191), a haemorheological agent, is an orally active non-selective phosphodiesterase (PDE) inhibitor, with immune modulation, anti-inflammatory, hemorheological, anti-fibrinolytic and anti-proliferation effects. Pentoxifylline can be used for the research of peripheral vascular disease, cerebrovascular disease and a number of other conditions involving a defective regional microcirculation .
|
-
-
- HY-108353
-
-
-
- HY-B1021
-
-
-
- HY-108353A
-
-
-
- HY-N6097
-
-
-
- HY-B0468R
-
-
-
- HY-N2998R
-
-
-
- HY-B1021R
-
-
-
- HY-N18471
-
|
5,7-DHP
|
Structural Classification
Alkaloids
Animals
Indole Alkaloids
Source Classification
|
Monoamine Oxidase
5-HT Receptor
|
|
5,7-Dihydroxytryptamine (5,7-DHP) is an autofluorescent (λex≈365 nm), selective neurotoxin and a transport substrate for MAO-A and 5-HT. 5,7-Dihydroxytryptamine can specifically target and damage central and peripheral 5-HTergic neurons, while affecting 5-HT-related pathways and neurotransmitter balance. 5,7-Dihydroxytryptamine can be used to establish 5-HTergic neuron injury models for studies on neural development, neurodegenerative diseases, as well as mechanisms related to platelet function and retinal neurons .
|
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-17043S1
-
|
|
|
Loratadine-d5 is the deuterium labeled Loratadine. Loratadine (SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. Loratadine has anti-dengue-virus (DENV) activity. Loratadine can inhibit immunologic release of inflammatory mediators.
|
-
-
- HY-108229S
-
|
|
|
6β-Naltrexol-d3 (6β-Hydroxynaltrexone-d3) is deuterium labeled 6β-Naltrexol. 6β-Naltrexol (6β-Hydroxynaltrexone), the primary metabolite of Naltrexone, is a peripherally selective opioid antagonist. 6β-Naltrexol selectively inhibits gastrointestinal opioid effects in human subjects and inhibits Morphine-induced slowing of gastrointestinal transit .
|
-
-
- HY-14280S
-
|
|
|
Entacapone-d10 is the deuterium labeled Entacapone. Entacapone is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone inhibits COMT from rat brain, erythrocytes and liver with IC50 values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone is selective for COMT over other catecholamine metabolizing enzymes, including MAO-A, MAO-B, phenolsulphotransferase M (PST-M) and PST-P (IC50s>50 μM). Entacapone can be used for the research of Parkinson's disease . Entacapone serves as a inhibitor of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders .
|
-
-
- HY-B0311AS
-
|
|
|
Carbidopa-d3 (monohydrate) is the deuterium labeled Carbidopa monohydrate. Carbidopa ((S)-(-)-Carbidopa) monohydrate, a peripheral decarboxylase inhibitor, can be used for the research of Parkinson's disease. Carbidopa monohydrate is a selective aryl hydrocarbon receptor (AhR) modulator. Carbidopa monohydrate inhibits pancreatic cancer cell and tumor growth .
|
-
-
- HY-B0715S2
-
|
|
|
Pentoxifylline-d5 is the deuterium labeled Pentoxifylline. Pentoxifylline (BL-191), a haemorheological agent, is an orally active non-selective phosphodiesterase (PDE) inhibitor, with immune modulation, anti-inflammatory, hemorheological, anti-fibrinolytic and anti-proliferation effects. Pentoxifylline can be used for the research of peripheral vascular disease, cerebrovascular disease and a number of other conditions involving a defective regional microcirculation .
|
-
-
- HY-B0002BS
-
|
|
|
Ondansetron-d5 is the deuterium labeled Ondansetron (HY-B0002B). Ondansetron (GR 38032; SN 307) is a highly selective 5-HT3 receptor antagonist with an IC50 value of 103 pM. Ondansetron exerts its antiemetic effect by antagonizing 5-HT receptors located in localized neurons in the peripheral and central nervous systems. Ondansetron can inhibit nausea and vomiting induced by chemotherapy and radiotherapy .
|
-
-
- HY-B0347S1
-
|
|
|
Lacidipine- 13C8 is the deuterium labeled Lacidipine . Lacidipine is an orally active and highly selective L-type calcium channel blocker that acts on smooth muscle calcium channels, primarily dilates peripheral arteries, reduces peripheral resistance, and has long-lasting anti-hypertensive activity. Lacidipine protects HKCs from apoptosis induced by ATP depletion and recovery by modulating the caspase-3 pathway. Lacidipine can be used in studies of hypertension, atherosclerosis and acute kidney injury (AKI) .
|
-
-
- HY-17609S1
-
|
|
|
Difelikefalin-d5 (CR-845-d5) hydrochloride is the deuterium labeled Difelikefalin (HY-17609). Difelikefalin (CR-845) is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease .
|
-
-
- HY-107322S
-
|
|
|
Barnidipine-d5 (hydrochloride) is the deuterium labeled Barnidipine hydrochloride. Barnidipine hydrochloride (Mepirodipine hydrochloride) is an L-type calcium antagonist (CaA) with high affinity for [3H] initrendipine binding sites (Ki=0.21 nmol/l), has selective action against CaA receptors .Barnidipine hydrochloride (Mepirodipine hydrochloride) is an antihypertensive agent and acts by the reduction of peripheral vascular resistance secondary to its vasodilatory action .
|
-
-
- HY-107322AS1
-
|
|
|
Barnidipine-d5 is the deuterium-labeled Barnidipine (HY-107322A). Barnidipine-d5 (Mepirodipine) is an L-type calcium antagonist (CaA) with high affinity for [ 3H] initrendipine binding sites (Ki=0.21 nmol/l), has selective action against CaA receptors . Barnidipine-d5 (Mepirodipine) is an antihypertensive agent and acts by the reduction of peripheral vascular resistance secondary to its vasodilatory action .
|
-
-
- HY-13331S2
-
|
|
|
Clascoterone-d5-1 (Cortexolone 17 alpha-propionate-d5-1) is deuterium labeled Clascoterone. Clascoterone (Cortexolone 17 alpha-propionate;Cortexolone 17α-propionate;CB-03-01) is a new topical and peripherally selective androgen antagonist .
|
-
-
- HY-12717AS
-
|
|
|
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 .
|
-
-
- HY-17609S
-
|
|
|
Difelikefalin-d5 (CR-845-d5) is deuterium labeled Difelikefalin. Difelikefalin (CR-845; FE-202845) is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease .
|
-
-
- HY-B0715S
-
|
|
|
Pentoxifylline-d6 is the deuterium labeled Pentoxifylline. Pentoxifylline (BL-191), a haemorheological agent, is an orally active non-selective phosphodiesterase (PDE) inhibitor, with immune modulation, anti-inflammatory, hemorheological, anti-fibrinolytic and anti-proliferation effects. Pentoxifylline can be used for the research of peripheral vascular disease, cerebrovascular disease and a number of other conditions involving a defective regional microcirculation .
|
-
-
- HY-B0197AS
-
|
|
|
Naratriptan-d3 (GR-85548A-d3) is the deuterium labeled Naratriptan hydrochloride (HY-B0197A). Naratriptan hydrochloride is a selective 5-HT1B/1D receptor agonist. Naratriptan hydrochloride is peripherally active and has good oral bioavailability, inducing cranial artery vasoconstriction by activating 5-HT1B/1D receptors (EC50=0.11 μM for dog basilar artery). Naratriptan hydrochloride also inhibits trigeminal nerve-mediated dural neurogenic plasma extravasation and reduces sterile inflammation. Naratriptan hydrochloride is mainly used in the research of acute migraine, targeting cranial vascular and neuroinflammatory mechanisms .
|
-
-
- HY-B0233S2
-
|
|
|
Isradipine-d7 is deuterated labeled Isradipine (HY-B0233). Isradipine (PN 200-110) is an orally active L-type calcium channel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease .
|
-
-
- HY-B0233S1
-
|
|
|
Isradipine-d6 is the deuterium labeled Isradipine . Isradipine (PN 200-110) is an orally active L-type calcium channel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease .
|
-
-
- HY-B0233S
-
|
|
|
Isradipine-d3 (PN 200-110-d3) is the deuterium labeled Isradipine. Isradipine (PN 200-110) is an orally active L-type calcium channel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease .
|
-
-
- HY-B0347S3
-
|
|
|
Lacidipine- 13C4 is 13C labeled Lacidipine (HY-B0347). Lacidipine is an orally active and highly selective L-type calcium channel blocker that acts on smooth muscle calcium channels, primarily dilates peripheral arteries, reduces peripheral resistance, and has long-lasting anti-hypertensive activity. Lacidipine protects HKCs from apoptosis induced by ATP depletion and recovery by modulating the caspase-3 pathway. Lacidipine can be used in studies of hypertension, atherosclerosis and acute kidney injury (AKI) .
|
-
-
- HY-13331S1
-
|
|
|
Clascoterone-d6 (Cortexolone 17 alpha-propionate-d6) is deuterium labeled Clascoterone. Clascoterone (Cortexolone 17 alpha-propionate;Cortexolone 17α-propionate;CB-03-01) is a new topical and peripherally selective androgen antagonist .
|
-
-
- HY-B0311S1
-
|
|
|
Carbidopa-d3-1 is the deuterium labeled Carbidopa (HY-B0311). Carbidopa, a peripheral decarboxylase inhibitor, can be used for the research of Parkinson's disease. Carbidopa is a selective aryl hydrocarbon receptor (AhR) modulator. Carbidopa inhibits pancreatic cancer cell and tumor growth .
|
-
-
- HY-17043S
-
|
|
|
Loratadine-d4 is the deuterium labeled Loratadine. Loratadine (SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. Loratadine has anti-dengue-virus (DENV) activity. Loratadine can inhibit immunologic release of inflammatory mediators.
|
-
-
- HY-B0468S
-
|
|
|
Isoprenaline-d7 (hydrochloride) is a deuterated labeled Isoprenaline (hydrochloride) . Isoprenaline (Isoproterenol) hydrochloride is a non-selective, orally active β-adrenergic receptor agonist. Isoprenaline has potent peripheral vasodilator, bronchodilator, and cardiac stimulating activities. Isoprenaline can be used for the research of bradycardia and bronchial asthma .
|
-
-
- HY-23188
-
|
|
|
Loratadine-d5-1 is a deuterated labeled Loratadine (HY-17043). Loratadine (SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. Loratadine has anti-dengue-virus (DENV) activity. Loratadine can inhibit immunologic release of inflammatory mediators.
|
-
-
- HY-17043S2
-
|
|
|
Loratadine-d4-1 (Loratidine-d4-1) is deuterium labeled Loratadine. Loratadine (SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. Loratadine has anti-dengue-virus (DENV) activity. Loratadine can inhibit immunologic release of inflammatory mediators .
|
-
-
- HY-17043S3
-
|
|
|
Loratadine- 13C6 (SCH 29851- 13C6) is 13C labeled Loratadine. Loratadine (SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. Loratadine has anti-dengue-virus (DENV) activity. Loratadine can inhibit immunologic release of inflammatory mediators.
|
-
-
- HY-B0715S3
-
|
|
|
Pentoxifylline-d3 (BL-191-d3) is deuterium labeled Pentoxifylline. Pentoxifylline (BL-191), a haemorheological agent, is an orally active non-selective phosphodiesterase (PDE) inhibitor, with immune modulation, anti-inflammatory, hemorheological, anti-fibrinolytic and anti-proliferation effects. Pentoxifylline can be used for the research of peripheral vascular disease, cerebrovascular disease and a number of other conditions involving a defective regional microcirculation .
|
-
-
- HY-B0002BS1
-
|
|
|
Ondansetron-d3 is the deuterium labeled Ondansetron (HY-B0002B ). Ondansetron (GR 38032; SN 307) is a highly selective 5-HT3 receptor antagonist with an IC50 value of 103 pM. Ondansetron exerts its antiemetic effect by antagonizing 5-HT receptors located in localized neurons in the peripheral and central nervous systems. Ondansetron can inhibit nausea and vomiting induced by chemotherapy and radiotherapy .
|
-
-
- HY-B0002BS2
-
|
|
|
Ondansetron- 13C,d3 is the 13C- and deuterium labeled Ondansetron (HY-B0002B). Ondansetron (GR 38032; SN 307) is a highly selective 5-HT3 receptor antagonist with an IC50 value of 103 pM. Ondansetron exerts its antiemetic effect by antagonizing 5-HT receptors located in localized neurons in the peripheral and central nervous systems. Ondansetron can inhibit nausea and vomiting induced by chemotherapy and radiotherapy .
|
-
-
- HY-B0197S
-
|
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Naratriptan-d3 (GR-85548A-d3) is the deuterium labeled Naratriptan (HY-B0197). Naratriptan is a selective 5-HT1B/1D receptor agonist. Naratriptan is peripherally active and has good oral bioavailability, inducing cranial artery vasoconstriction by activating 5-HT1B/1D receptors (EC50=0.11 μM for dog basilar artery). Naratriptan also inhibits trigeminal nerve-mediated dural neurogenic plasma extravasation and reduces sterile inflammation. Naratriptan is mainly used in the research of acute migraine, targeting cranial vascular and neuroinflammatory mechanisms .
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- HY-125387
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Alkynes
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TOP1210 is a narrow-spectrum tyrosine kinase inhibitor with potent inhibitory activity against P38α, Src, and Syk kinases. TOP1210 effectively reduced proinflammatory cytokines released by peripheral blood monocytes, primary macrophages, HT29 cells, inflammatory cells in ulcerative colitis (UC) biopsies, and myofibroblasts isolated from inflamed colonic UC mucosa. TOP1210 showed significant anti-inflammatory effects in cell experiments and UC biopsies, superior to some selective kinase inhibitors. The multi-kinase inhibition of TOP1210 provides the possibility of obtaining a wider range of therapeutic effects, especially in the regulation of autoimmune responses .
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