Search Result
Results for "
cardiovascular
" in MCE Product Catalog:
1827
Inhibitors & Agonists
6
Biochemical Assay Reagents
116
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
-
- HY-107337
-
-
- HY-135601
-
-
- HY-103314
-
-
- HY-N6617
-
-
- HY-14936
-
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Sofigatran
MCC-977
|
Thrombin
|
Cardiovascular Disease
|
|
Sofigatran (MCC-977) is an orally active factor IIa (thrombin) inhibitor, acts as an anticoagulant. Sofigatran is used for the research of cardiovascular disease.
|
-
- HY-14838
-
-
- HY-14838A
-
-
- HY-17464
-
-
- HY-132591
-
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Inclisiran
ALN-PCSsc
|
Ser/Thr Protease
|
Cardiovascular Disease
|
|
Inclisiran (ALN-PCSsc) is a double-stranded small interfering RNA (siRNA) molecule that inhibits the transcription of PCSK-9. Inclisiran can be used for hyperlipidemia and cardiovascular disease (CVD) research.
|
-
- HY-112094S
-
-
- HY-B0232
-
-
- HY-119515
-
|
Denopamine
(R)-(-)-Denopamine; TA-064
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Denopamine ((R)-(-)-Denopamine) is an orally active, selective β1-adrenergic agonist. Denopamine prolongs survival in a murine model of congestive heart failure induced by viral myocarditis: suppression of tumor necrosis factor-α production in the heart. Cardiovascular effects.
|
-
- HY-141552
-
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FC9402
|
Others
|
Cardiovascular Disease
|
|
FC9402 is a potent and selective sulfide quinone oxidoreductase (SQOR) inhibitor extracted from patent WO 2020/146636 A1. FC9402 attenuates TAC-induced cardiomyocyte hypertrophy and left ventricle (LV) fibrosis. FC9402 can be used for cardiovascular regulation.
|
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- HY-N7431
-
-
- HY-B0835
-
|
Fenobucarb
|
Apoptosis
|
Neurological Disease
Cardiovascular Disease
|
|
Fenobucarb is a carbamate insecticide. Fenobucarb induces zebrafish developmental neurotoxicity through pathways involved in inflammation, oxidative stress, degeneration and apoptosis. Fenobucarb is a possible risk factor to cardiovascular and cerebrovascular systems in animals.
|
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- HY-A0176
-
-
- HY-P1298
-
|
Sauvagine
|
CRFR
|
Endocrinology
Neurological Disease
Cardiovascular Disease
|
|
Sauvagine, a 40-amino-acid neuropeptide from the skin of the frog, is a mammalian CRF agonist. Sauvagine is effective at releasing ACTH from rat pituitary cells. Sauvagine possesses a number of pharmacological actions on diuresis, the cardiovascular system and endocrine glands.
|
-
- HY-123268
-
|
Ro 363
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Ro 363, an effective inotropic stimulant, is a potent and highly selective β1-adrenoceptor agonist. RO 363 is a cardiovascular modulator that reduces diastolic blood pressure and pronounces increases in myocardial contractility.
|
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- HY-123268A
-
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Ro 363 hydrochloride
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Ro 363 hydrochloride, an effective inotropic stimulant, is a potent and highly selective β1-adrenoceptor agonist. Ro 363 hydrochloride is a cardiovascular modulator that reduces diastolic blood pressure and pronounces increases in myocardial contractility.
|
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- HY-139486
-
|
AM-8123
|
Others
|
Cardiovascular Disease
|
|
AM-8123 is an orally active and potent APJ agonist. AM-8123 inhibits Forskolin-stimulated cAMP production and promotes Gα protein activation. AM-8123 can be used for the research of cardiovascular disease.
|
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- HY-110237
-
|
BX430
|
P2X Receptor
Calcium Channel
|
Cardiovascular Disease
|
|
BX430 is a potent and selective noncompetitive allosteric human P2X4 receptor channels antagonist with an IC50 of 0.54 μM. BX430 has species specificity. BX430 is used for chronic pain and cardiovascular disease.
|
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- HY-P1298A
-
|
Sauvagine TFA
|
CRFR
|
Endocrinology
Neurological Disease
Cardiovascular Disease
|
|
Sauvagine TFA, a 40-amino-acid neuropeptide from the skin of the frog, is a mammalian CRF agonist. Sauvagine TFA is effective at releasing ACTH from rat pituitary cells. Sauvagine TFA possesses a number of pharmacological actions on diuresis, the cardiovascular system and endocrine glands.
|
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- HY-16952A
-
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Bepridil hydrochloride hydrate
(±)-Bepridil hydrochloride hydrate; Org 5730 hydrochloride hydrate
|
Calcium Channel
|
Cardiovascular Disease
|
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Bepridil hydrochloride hydrate ((±)-Bepridil hydrochloride hydrate) is a non-selective, long-acting Ca + channel antagonist and Na +, K + channel inhibitor, with antianginal and type I antiarrhythmic effects. Bepridil hydrochloride hydrate also acts as a cardiac Na +/Ca2 + exchange (NCX1) inhibitor. Bepridil hydrochloride hydrate can be used for the research of cardiovascular disorders.
|
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- HY-W009749
-
|
L-Cystathionine
|
Endogenous Metabolite
Apoptosis
|
Cardiovascular Disease
|
|
L-Cystathionine is a nonprotein thioether and is a key amino acid associated with the metabolic state of sulfur-containing amino acids. L-Cystathionine protects against Homocysteine-induced mitochondria-dependent apoptosis of vascular endothelial cells (HUVECs). L-Cystathionine plays an important role in cardiovascular protection.
|
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- HY-N8086
-
-
- HY-N8087
-
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- HY-136584
-
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2,2,14,14-Tetramethyl-8-oxopentadecanedioic acid
|
Others
|
Metabolic Disease
Cardiovascular Disease
|
|
2,2,14,14-Tetramethyl-8-oxopentadecanedioic acid is a ketone compound extracted from patent WO2002030860A2, compound example II-9. 2,2,14,14-Tetramethyl-8-oxopentadecanedioic acid can be used for the research of cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders.
|
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- HY-N0728
-
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α-Linolenic acid
|
PI3K
Akt
|
Cancer
Cardiovascular Disease
|
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α-Linolenic acid, isolated from seed oils, is an essential fatty acid that cannot be synthesized by humans. α-Linolenic acid can affect the process of thrombotic through the modulation of PI3K/Akt signaling. α-Linolenic acid possess the anti-arrhythmic properties and is related to cardiovascular disease and cancer.
|
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- HY-W062836
-
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BAY 41-8543
|
Guanylate Cyclase
|
Cardiovascular Disease
|
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BAY 41-8543 is an orally active, nitric oxide (NO)-independent stimulator of soluble guanylyl cyclase (sGC). BAY 41-8543 has vasodilator activity in the pulmonary and systemic vascular beds in the rat. BAY 41-8543 has antiplatelet effects and has the potential for cardiovascular diseases research.
|
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- HY-121538
-
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CUDA
|
Epoxide Hydrolase
PPAR
|
Cardiovascular Disease
|
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CUDA is a potent inhibitor of soluble epoxide hydrolase (sEH), with IC50s of 11.1 nM and 112 nM for mouse sEH and human sEH, respectively. CUDA selectively increases peroxisome proliferator-activated receptor (PPAR) alpha activity. CUDA may be valuable for the research of cardiovascular disease.
|
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- HY-126415
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- HY-131981
-
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TP0586532
|
Bacterial
|
Infection
|
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TP0586532 is a non-hydroxamate LpxC inhibitor (IC50=0.101 μM). TP0586532 as a compound with a low cardiovascular risk that is effective against K. pneumoniae, including resistant strains.
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- HY-121392
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- HY-125990
-
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SLC13A5-IN-1
|
Sodium Channel
|
Metabolic Disease
Cardiovascular Disease
|
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SLC13A5-IN-1 is a selective sodium-citrate co-transporter (SLC13A5) inhibitor. SLC13A5-IN-1 completely blocks the uptake of 14C-citrate with an IC50 value of 0.022 μM in HepG2 cells. SLC13A5-IN-1 has the potential for the treatment of metabolic and/or cardiovascular diseases. SLC13A5-IN-1 is extracted from patent WO2018104220A1, Compound I-5.
|
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- HY-135773
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- HY-14406A
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- HY-U00398
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- HY-U00044
-
-
- HY-U00034
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- HY-135593
-
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LY88074 analog 1
|
Others
|
Endocrinology
|
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LY88074 analog 1 is a benzothiophene compound with nitrogen-containing non-basic side chains, Compound 26, extracted from patent EP0747380A1. LY88074 analog 1 is an agent for alleviating the symptoms of post-menopausal symptoms, such as osteoporosis, cardiovascular related pathological conditions, and estrogen-dependent cancer. LY88074 analog 1 can be used alone or in combination with estrogen or progestin.
|
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- HY-19504
-
-
- HY-19321
-
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- HY-121765
-
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Dacisteine
N,S-Diacetyl-L-cysteine
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Dacisteine (N,S-Diacetyl-L-cysteine) is a cysteine derivative and displays a less New Delhi metallo-beta-lactamase-1 (NDM-1) inhibitor with an IC50 value of 1000 μM. Dacisteine can be used for the treatment of cardiovascular and cerebrovascular diseases caused by platelet aggregation.
|
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- HY-70037
-
-
- HY-U00386
-
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- HY-17408
-
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- HY-70037A
-
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- HY-124063
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- HY-N5078
-
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- HY-W021162
-
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- HY-P1064
-
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Apelin-36(human)
|
HIV
|
Infection
Metabolic Disease
Cardiovascular Disease
|
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Apelin-36(human) is an endogenous orphan G protein-coupled receptor APJ agonist, with an EC50 of 20 nM. Apelin-36(human) shows high affinity to human APJ receptors expressed in HEK 293 cells (pIC50=8.61). Apelin-36 has been linked to two major types of biological activities: cardiovascular and metabolic. Apelin-36(human) inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ.
|
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- HY-U00191
-
-
- HY-P1064A
-
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Apelin-36(human) TFA
|
HIV
|
Infection
Metabolic Disease
Cardiovascular Disease
|
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Apelin-36(human) TFA is an endogenous orphan G protein-coupled receptor APJ agonist, with an EC50 of 20 nM. Apelin-36(human) TFA shows high affinity to human APJ receptors expressed in HEK 293 cells (pIC550=8.61). Apelin-36(human) TFA has been linked to two major types of biological activities: cardiovascular and metabolic. Apelin-36(human) TFA inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ.
|
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- HY-122537A
-
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Arotinolol
|
Adrenergic Receptor
5-HT Receptor
|
Cardiovascular Disease
|
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Arotinolol is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker. Arotinolol also shows potency for inhibiting the binding of the radioligand 125I-ICYP to 5HT1B-serotonergic receptor sites. Arotinolol is an antihypertensive agent for the treatment of a variety of cardiovascular pathologies as well as non-cardiovascular diseases.
|
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- HY-N1913
-
-
- HY-N4305
-
-
- HY-17503
-
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- HY-N6881
-
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Gypenoside XIII
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Others
|
Cardiovascular Disease
|
|
Gypenoside XIII is belonging to the gypenosides. Gypenosides, extracted from Gynostemma pentaphyllum, have various pharmacological properties and protect against cardiovascular diseases, especially atherosclerosis.
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- HY-109593
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- HY-109136
-
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Runcaciguat
|
Guanylate Cyclase
|
Cardiovascular Disease
|
|
Runcaciguat is an orally active stimulator of soluble guanylate cyclase, and is used in the research of cardiovascular and renal diseases combined with selective partial adenosine A1 receptor agonists.
|
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- HY-136576
-
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RP101075
|
LPL Receptor
Drug Metabolite
|
Inflammation/Immunology
|
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RP101075, an active metabolite of Ozanimod, is a potent, orally active S1PR (sphingosine-1-phosphate receptor 1) agonist, with an EC50 of 0.27 nM. RP101075 displays >100-fold selectivity over S1PR5 (EC50=5.9 nM) and >10000-fold over S1PR 2, 3, and 4. RP101075 displays superior cardiovascular safety profile.
|
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- HY-17503A
-
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- HY-N1362
-
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Salvianolic acid B
Lithospermic acid B
|
Autophagy
|
Cardiovascular Disease
|
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Salvianolic acid B is an active ingredient of Salvia miltiorrhiza, which has been widely applied in China for the management of various microcirculation-related disorders, such as cardiovascular disease, cerebrovascular disease, and diabetic vascular complication.
|
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- HY-N1370
-
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- HY-N0360
-
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Dihydrotanshinone I
|
SARS-CoV
|
Cardiovascular Disease
|
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Dihydrotanshinone I is a natural compound extracted from Salvia miltiorrhiza Bunge which has been widely used for treating cardiovascular diseases. Dihydrotanshinone I exhibits entry-blocking effect for MERS-CoV.
|
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- HY-N4271
-
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Protogracillin
|
Others
|
Cardiovascular Disease
|
|
Protogracillin is a steroidal saponin isolated from Dioscorea zingiberensis Wright (DZW). Steroidal saponins from DZW rhizomes have the potential to reduce the risk of cardiovascular diseases by anti-thrombotic action.
|
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- HY-106950
-
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Fosfructose
Diphosphofructose; Esafosfan; FDP
|
Endogenous Metabolite
|
Cardiovascular Disease
|
|
Fosfructose (Diphosphofructose;Esafosfan;FDP) is a cytoprotective natural sugar phosphate for the potential treatment of cardiovascular ischemia, sickle cell anemia and asthma. It acts by stimulating anaerobic glycolysis which generates adenosine triphosphate under ischemic conditions.
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- HY-N2174
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- HY-12124
-
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BBS-4
|
NO Synthase
|
Cardiovascular Disease
|
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BBS-4 is a potent and selective inducible nitric oxide synthase (NOS2) dimerization inhibitor, with an IC50 of 0.49 nM. BBS-4 can protect mice from the cardiovascular dysfunction of sepsis.
|
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- HY-106950A
-
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Fosfructose trisodium
Diphosphofructose trisodium; Esafosfan trisodium; FDP trisodium
|
Endogenous Metabolite
|
Cardiovascular Disease
|
|
Fosfructose trisodium (Diphosphofructose trisodium;Esafosfan trisodium;FDP trisodium) is a cytoprotective natural sugar phosphate for the potential treatment of cardiovascular ischemia, sickle cell anemia and asthma. It acts by stimulating anaerobic glycolysis which generates adenosine triphosphate under ischemic conditions.
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- HY-N0738
-
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- HY-N7513
-
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Homovanillyl alcohol
|
Drug Metabolite
|
Cardiovascular Disease
|
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Homovanillyl alcohol is a biological metabolite of Hydroxytyrosol. Hydroxytyrosol is a phenolic compound that is present in virgin olive oil (VOO) and wine. Homovanillyl alcohol protects red blood cells (RBCs) from oxidative injury and has protective effect on cardiovascular disease.
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- HY-N0534
-
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Vitexin-2"-O-rhamnoside
|
Others
|
Cardiovascular Disease
|
|
Vitexin-2"-O-rhamnoside, a main flavonoid glycoside of the leaves of Cratagus pinnatifida Bge, contributes to the protection against H2O2-mediated oxidative stress damage and has potential to treat cardiovascular system diseases.
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- HY-A0176S
-
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- HY-126293
-
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Apelin agonist 1
|
Others
|
Cardiovascular Disease
|
|
Apelin agonist 1 is an oral selective apelin agonist AM-2995, a agonist of the APJ (APLNR, angiotensin receptor like-1) receptor, may be used in the treatment of cardiovascular conditions. Apelin agonist 1 is extracted from patent WO 2018097944 (210.0), Example 210.0.
|
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- HY-124756
-
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SBI-425
|
Phosphatase
|
Cardiovascular Disease
|
|
SBI-425 is a potent, selective and oral bioavailable tissue-nonspecific alkaline phosphatase (TNAP) inhibitor. Long-term administration of SBI-425 effectively reaches and inhibits TNAP in the vasculature, improving cardiovascular parameters and survival at a dose that does not cause a detectable change in bone.
|
-
- HY-118284
-
|
Vicagrel
|
P2Y Receptor
|
Cardiovascular Disease
|
|
Vicagrel, an acetate derivative of Clopidogrel, is a P2Y12 platelet inhibitor potentially for the treatment of thrombosis, the substrate of carboxylesterase 2 (CES2). Vicagrel demonstrates a favorable safety profile and excellent anti-platelet activity, which could be an anti-platelet drug and for the unmet medical needs of cardiovascular diseases.
|
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- HY-129459
-
-
- HY-W011690
-
-
- HY-U00397
-
-
- HY-P1131
-
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M617
|
Neuropeptide Y Receptor
|
Cardiovascular Disease
|
|
M617 is a selective galanin receptor 1 (GAL1) agonist, with Kis of 0.23 and 5.71 nM for GAL1 and GAL2, respectively. M617, acting through its central GAL1, can promote GLUT4 expression and enhance GLUT4 content in the cardiac muscle of type 2 diabetic rats.
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- HY-N6256
-
-
- HY-W009749B
-
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DL-Cystathionine dihydrochloride
|
Apoptosis
|
Cardiovascular Disease
|
|
DL-Cystathionine dihydrochloride is a racemic melange of the L-Cystathionine dihydrochloride and D-Cystathionine dihydrochloride. L-Cystathionine dihydrochloride is a nonprotein thioether and is a key amino acid associated with the metabolic state of sulfur-containing amino acids. L-Cystathionine dihydrochloride protects against Homocysteine-induced mitochondria-dependent apoptosis of vascular endothelial cells (HUVECs). L-Cystathionine dihydrochloride plays an important role in cardiovascular protection.
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- HY-139572
-
-
- HY-N3307
-
-
- HY-B1416A
-
-
- HY-122778
-
|
δ-Tocotrienol
|
Others
|
Cancer
Neurological Disease
Cardiovascular Disease
|
|
δ-Tocotrienol is a Vitamin E in vegetables, fruits, seeds, nuts, grains and oils. Vitamin E has become well known for its role as an antioxidant, in lowering cholesterol and other lipids, as a neuroprotective and anticancer agent, and in cardiovascular disease protection.
|
-
- HY-103080
-
|
CMF019
|
Others
|
Cardiovascular Disease
|
|
CMF019 is a potent and small molecule agonist at Apelin receptor (APJ) with G protein bias. CMF019 binds to APJ with pKi values of 8.58, 8.49 and 8.71 for human, rat, and mouse, respectively. CMF019 mimics the beneficial cardiovascular actions of apelin in rodents. Apelin receptor (APJ) is a G protein-coupled receptor (GPCR) activated by the endogenous peptide apelin.
|
-
- HY-112233
-
|
O-304
|
AMPK
|
Metabolic Disease
Cardiovascular Disease
|
|
O-304 is a first-in-class, orally available pan-AMPK activator, which increases AMPK activity by suppressing the dephosphorylation of pAMPK. O-304 exhibits a great potential as a drug to treat type 2 diabetes (T2D) and associated cardiovascular complications .
|
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- HY-P1548
-
-
- HY-P1548B
-
-
- HY-P1548A
-
-
- HY-N0712
-
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Typhaneoside
|
Autophagy
|
Inflammation/Immunology
Cardiovascular Disease
|
|
Typhaneoside, extracted from Typha angustifolia L., Typhaneoside can inhibit the excessive autophagy of hypoxia/reoxygenation cells and increase the phosphorylation of Akt and mTOR. Typhaneoside has certain effects on the cardiovascular system, including lowering blood lipid levels, promoting antiatherosclerosis activities, as well as improving immune and coagulation function.
|
-
- HY-N6979
-
|
Crustecdysone
20-Hydroxyecdysone
|
Caspase
Autophagy
Endogenous Metabolite
|
Cardiovascular Disease
|
|
Crustecdysone (20-Hydroxyecdysone) is a naturally occurring ecdysteroid hormone isolated from Cyanotis arachnoides C.B.Clarke which controls the ecdysis (moulting) and metamorphosis of arthropods, it inhibits caspase activity and induces autophagy via the 20E nuclear receptor complex, EcR-USP. Crustecdysone exhibits regulatory or protective roles in the cardiovascular system. Crustecdysone is an active metabolite of Ecdysone (α-Ecdysone; HY-N0179)
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- HY-N1356
-
-
- HY-125976
-
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ML233
|
Others
|
Cardiovascular Disease
|
|
ML233 is a non-peptide based potent apelin receptor (APJ) agonist (EC50=3.7 μM). ML233 displays >21-fold selective over the closely related angiotensin 1 (AT1) receptor (>79 μM).
|
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- HY-118643
-
|
Cimlanod
BMS-986231; CXL-1427
|
Others
|
Cardiovascular Disease
|
|
Cimlanod (BMS-986231) is a second-generation Nitroxyl (HNO) donor for heart failure. Cimlanod (BMS-986231) delivers HNO via pH-dependent chemical breakdown when exposed to the neutral pH environment of the bloodstream. Cimlanod (BMS-986231) possesses positive lusitropic and inotropic as well as vasodilatory effects.
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- HY-N6934
-
-
- HY-121955
-
-
- HY-N0714
-
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Berbamine
|
NF-κB
Autophagy
|
Cancer
|
|
Berbamine is a natural compound extracted from traditional Chinese medicine Barberry with anti-tumor, immunomodulatory and cardiovascular effects. Berbamine is a calcium channel blocker.
|
-
- HY-B2163
-
|
Astaxanthin
|
PPAR
Reactive Oxygen Species
|
Cancer
Cardiovascular Disease
|
|
Astaxanthin, a red dietary carotenoid isolated from Haematococcus pluvialis, is a modulator of PPARγ and a potent antioxidant with antiproliferative, neuroprotective and anti-inflammatory activity. Astaxanthin has potential in the study of various diseases, such as cancers and Parkinson’s disease, cardiovascular disease. Due to its bright red colour, Astaxanthin could be used as a food colorant in animal feeds.
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- HY-N0655
-
-
- HY-108611
-
|
AACOCF3
Arachidonyl trifluoromethyl ketone
|
Phospholipase
|
Cardiovascular Disease
|
|
AACOCF3 (Arachidonyl trifluoromethyl ketone) is a cell-permeant trifluoromethyl ketone analog of arachidonic acid. AACOCF3 is a potent and selective slow binding inhibitor of the 85-kDa cytosolic phospholipase A2 (cPLA2). AACOCF3 blocks production of arachidonate and 12-hydroxyeicosatetraenoic acid by calcium ionophore-challenged platelets. AACOCF3 inhibits glucose-induced insulin secretion from isolated rat islets. AACOCF3 has the potential for the research of cardiovascular disease.
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-
- HY-125851
-
|
TP-008
|
ALK
|
Inflammation/Immunology
|
|
TP-008 is a potent, selective and orally active (Activin-Like Kinase 5) ALK5 inhibitor with pIC50 and pEC50 values of 7.6 and 6.63, respectively. TGFβRI-IN-2 can produce observed cardiac toxicity in vivo at high dose.
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-
- HY-115688
-
-
- HY-N0799
-
|
Protodioscin
|
Endogenous Metabolite
|
Cancer
|
|
Protodioscin, a major steroidal saponin in dioscoreae rhizome, has been shown to exhibit multiple biological actions, such as anti-hyperlipidemia, anti-cancer, sexual effects and cardiovascular properties.
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-
- HY-17557
-
|
Calcium N5-methyltetrahydrofolate
NSC173328
|
Antifolate
|
Cancer
|
|
Calcium N5-methyltetrahydrofolate(NSC173328) is the calcium salt of levomefolic acid, which has been proposed for treatment of cardiovascular disease and advanced cancers such as breast and colorectal cancers.
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-
- HY-N2007
-
|
Veratric acid
3,4-Dimethoxybenzoic acid
|
COX
Reactive Oxygen Species
|
Inflammation/Immunology
Cardiovascular Disease
|
|
Veratric acid (3,4-Dimethoxybenzoic acid) is an orally active phenolic compound derived from vegetables and fruits, has antioxidant and anti-inflammatory activities. Veratric acid also acts as a protective agent against hypertension-associated cardiovascular remodelling. Veratric acid reduces upregulated COX-2 expression, and levels of PGE2, IL-6 after UVB irradiation.
|
-
- HY-P1525
-
-
- HY-15556A
-
-
- HY-15556
-
-
- HY-13603
-
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Crolibulin
EPC2407
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Crolibulin (EPC2407) is a tubulin polymerization inhibitor, with potent apoptosis induction and cell growth inhibition. Crolibulin has anti-tumor activity. Crolibulin also has cardiovascular toxicity and neurotoxicity.
|
-
- HY-P1525A
-
-
- HY-109523
-
|
Cerivastatin sodium
|
HMG-CoA Reductase (HMGCR)
Ferroptosis
|
Cancer
Cardiovascular Disease
|
|
Cerivastatin sodium is a synthetic lipid-lowering agent and a highly potent, well-tolerated and orally active HMG-CoA reductase inhibitor, with a Ki of 1.3 nM/L. Cerivastatin sodium reduces low-density lipoprotein cholesterol levels. Cerivastatin sodium also inhibits proliferation and invasiveness of MDA-MB-231 cells, mainly by RhoA inhibition, and has anti-cancer effect.
|
-
- HY-100434
-
|
PD-161570
|
FGFR
PDGFR
EGFR
Src
TGF-β Receptor
|
Cancer
Cardiovascular Disease
|
|
PD-161570 is a potent and ATP-competitive human FGF-1 receptor inhibitor with an IC50 of 39.9 nM and a Ki of 42 nM. PD-161570 also inhibits the PDGFR, EGFR and c-Src tyrosine kinases with IC50 values of 310 nM, 240 nM, and 44 nM, respectively. PD-161570 inhibits PDGF-stimulated autophosphorylation and FGF-1 receptor phosphorylation with IC50s of 450 nM and 622 nM, respectively. PD-161570 is also a bone morphogenetic proteins (BMPs) and TGF-β signaling inhibitor.
|
-
- HY-129458
-
|
Cerivastatin
|
HMG-CoA Reductase (HMGCR)
Ferroptosis
|
Cancer
Cardiovascular Disease
|
|
Cerivastatin is a synthetic lipid-lowering agent and a highly potent, well-tolerated and orally active HMG-CoA reductase inhibitor, with a Ki of 1.3 nM/L. Cerivastatin reduces low-density lipoprotein cholesterol levels. Cerivastatin also inhibits proliferation and invasiveness of MDA-MB-231 cells, mainly by RhoA inhibition, and has anti-cancer effect.
|
-
- HY-P1065A
-
|
Apelin-36(rat, mouse) TFA
|
HIV
|
Infection
Metabolic Disease
Cardiovascular Disease
|
|
Apelin-36(rat, mouse) TFA is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-36(rat, mouse) TFA binds to APJ receptors with an IC50 of 5.4 nM, and potently inhibits cAMP production with an EC50 of 0.52 nM. Apelin-36(rat, mouse) TFA blocks entry of some HIV-1 and HIV-2 strains into NP-2/CD4 cells expressing APJ.
|
-
- HY-125911
-
|
Gossypin
|
NF-κB
|
Cancer
Inflammation/Immunology
Cardiovascular Disease
|
|
Gossypin is a flavone isolated from Hibiscus vitifolius and has antioxidant, antiinflammatory, anticancer, anticataract, antidiabetic, and hepatoprotective activities. Gossypin inhibits NF-κB and NF-κB-regulated gene expression. Gossypin inhibits RANKL-induced osteoclastogenesis both in mouse primary bone marrow cells and RAW 264.7 cells in vitro.
|
-
- HY-P1065
-
|
Apelin-36(rat, mouse)
|
HIV
|
Infection
Metabolic Disease
Cardiovascular Disease
|
|
Apelin-36(rat, mouse) is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-36(rat, mouse) binds to APJ receptors with an IC50 of 5.4 nM, and potently inhibits cAMP production with an EC50 of 0.52 nM. Apelin-36(rat, mouse) blocks entry of some HIV-1 and HIV-2 strains into NP-2/CD4 cells expressing APJ.
|
-
- HY-N0515
-
|
Ophiopogonin D
|
PPAR
NF-κB
Calcium Channel
|
Inflammation/Immunology
Cardiovascular Disease
|
|
Ophiopogonin D, isolated from the tubers of Ophiopogon japonicus, is a rare naturally occurring C29 steroidal glycoside. Ophiopogonin D is a CYP2J3 inducer that significantly inhibits Ang II induced NF-κB nuclear translocation, IκBα down-regulation, intracellular Ca 2+ overload and activation of pro-inflammatory cytokines by increasing the expression of CYP2J2/EETs and PPARα in human umbilical vein endothelial cells (HUVECs). Ophiopogonin D has been used to treat inflammatory and cardiovascular diseases for thousands of years.
|
-
- HY-N0393
-
|
Glabridin
|
PPAR
Reactive Oxygen Species
Bacterial
|
Cancer
Infection
Inflammation/Immunology
|
|
Glabridin is a natural isoflavan from Glycyrrhiza glabra, binds to and activates PPARγ, with an EC50 of 6115 nM. Glabridin exhibits antioxidant, anti-bacterial, anti-nephritic, anti-diabetic, anti-fungal, antitumor, anti-inflammatory, antiosteoporotic, cardiovascular protective, neuroprotective and radical scavenging activities.
|
-
- HY-115688A
-
|
(S)-TXNIP-IN-1
|
Others
|
Others
|
|
(S)-TXNIP-IN-1 is the less active S-enantiomer of TXNIP-IN-1 (HY-115688). TXNIP-IN-1 is a TXNIP-TRX complex inhibitor which can be used in the research of TXNIP-TRX complex associated metabolic disorder (diabetes), cardiovascular disease, or inflammatory disease
|
-
- HY-N1485
-
|
Cycloastragenol
Astramembrangenin; Cyclosieversigenin
|
Telomerase
|
Inflammation/Immunology
Neurological Disease
|
|
Cycloastragenol (Astramembrangenin), the active form of astragaloside IV, has anti-oxidant, anti-inflammatory, anti-aging, anti-apoptotic, and cardiovascular protective effects. Cycloastragenol is a potent telomerase activator and can lengthen telomeres. Cycloastragenol alleviates age-related bone loss and improves bone microstructure and biomechanical properties.
|
-
- HY-18260
-
|
Bisphenol A
|
Endogenous Metabolite
|
Endocrinology
|
|
Bisphenol A is a phenolic, organic synthetic compound widely used in the production of polycarbonate plastics and epoxy resins. Bisphenol A is a reproductive, developmental, and systemic toxicant, often classified as an endocrine-disrupting compound (EDC). Bisphenol A is associated with many diseases, including cardiovascular diseases, respiratory diseases, diabetes, kidney diseases, obesity, and reproductivedisorders.
|
-
- HY-103211
-
|
L748337
|
Adrenergic Receptor
|
Cancer
Metabolic Disease
Cardiovascular Disease
|
|
L748337 is a potent β3-adrenergic receptor antagonist and displays selectivity over β1 and β2 receptors. The Ki values of L748337 for β3-, β2- and β1-adrenoceptors are 4.0 nM, 204 nM and 390 nM, respectively. L748337 couples predominantly to Gi to activate MAPK signaling and increases phosphorylation of Erk1/2 with pEC50 value of 11.6. L748337 can be used for the research of cancer, nonalcoholic fatty liver disease (NAFLD), and cardiovascular related diseases.
|
-
- HY-13524
-
-
- HY-13524A
-
-
- HY-N7627
-
-
- HY-138944
-
-
- HY-B0351
-
|
Taurine
2-Aminoethanesulfonic acid
|
Autophagy
Endogenous Metabolite
|
Metabolic Disease
|
|
Taurine, a sulphur-containing amino acid and an organic osmolyte involved in cell volume regulation, provides a substrate for the formation of bile salts, and plays a role in the modulation of intracellular free calcium concentration. Taurine has the ability to activate autophagy in adipocytes.
|
-
- HY-P1066A
-
|
Apelin-17(human, bovine) TFA
|
HIV
|
Infection
|
|
Apelin-17(human, bovine) TFA is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-17(human, bovine) TFA binds to human APJ receptors expressed in HEK 293 cells (pIC50=9.02). Apelin-17(human, bovine) TFA inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ.
|
-
- HY-P1066
-
|
Apelin-17(human, bovine)
|
HIV
|
Infection
|
|
Apelin-17(human, bovine) is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-17(human, bovine) binds to human APJ receptors expressed in HEK 293 cells (pIC50=9.02). Apelin-17(human, bovine) inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ.
|
-
- HY-P1208
-
|
PG-931
|
Melanocortin Receptor
|
Inflammation/Immunology
|
|
PG-931, an analog of SHU 9119 (HY-P0227), is a potent melanocortin 4 (MC4) receptor (IC50=0.58 nM) agonist and is more selective than for the hMC3R (IC50=55 nM) or the hMC5R (IC50=2.4 nM). PG-931 can reverse haemorrhagic shock and prevent multiple organ damage in vivo.
|
-
- HY-P1208A
-
|
PG-931 TFA
|
Melanocortin Receptor
|
Inflammation/Immunology
|
|
PG-931 TFA, an analog of SHU 9119 (HY-P0227), is a potent melanocortin 4 (MC4) receptor (IC50=0.58 nM) agonist and is more selective than for the hMC3R (IC50=55 nM) or the hMC5R(IC50=2.4 nM). PG-931 TFA can reverse haemorrhagic shock and prevent multiple organ damage in vivo.
|
-
- HY-139560
-
-
- HY-139561
-
-
- HY-19762
-
-
- HY-15398
-
-
- HY-14728
-
|
Aleglitazar
R1439; RO0728804
|
PPAR
|
Metabolic Disease
|
|
Aleglitazar (R1439) is a potent dual PPARα/γ agonist, with IC50s of 38 nM and 19 nM for human PPARa and PPARγ, respectively. Aleglitazar can be used for the research of type II diabetes.
|
-
- HY-N6626
-
-
- HY-P1106
-
|
K41498
|
CRFR
|
Cardiovascular Disease
|
|
K41498 is a potent and highly selective CRF2 receptor antagonist with Ki values of 0.66 nM, 0.62 nM and 425 nM for human CRF2α, CRF2β and CRF1 receptors respectively. K41498 is an analogues of antisauvagine-30 (aSvg-30), inhibits sauvagine-stimulated cAMP accumulation in hCRF2α- and hCRF2β-expressing cells. K41498 can be used for hypotension study.
|
-
- HY-N5004
-
-
- HY-B0428
-
|
Ozagrel
OKY-046
|
Prostaglandin Receptor
|
Cardiovascular Disease
|
|
Ozagrel (OKY-046)is an anti-asthmatic agent and a thromboxane A2 (TXA2) synthase inhibitor. Ozagrel is an antiplatelet agent, which selectively inhibits human platelet aggregation with an IC50 of 53.12 μM.
|
-
- HY-135883
-
-
- HY-P3108
-
-
- HY-A0182A
-
-
- HY-15124
-
-
- HY-N5006
-
-
- HY-100380
-
-
- HY-111372A
-
|
(Rac)-Finerenone
(Rac)-BAY 94-8862
|
Mineralocorticoid Receptor
|
Cardiovascular Disease
|
|
(Rac)-Finerenone ((Rac)-BAY 94-8862) is the racemate of Finerenone. Finerenone is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist (IC50=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold).
|
-
- HY-N4081
-
-
- HY-133149
-
-
- HY-114424A
-
-
- HY-B0341S
-
|
Nicorandil-d4
|
Potassium Channel
|
Cardiovascular Disease
|
|
Nicorandil-d4 (SG-75-d4) is the deuterium labeled Nicorandil. Nicorandil (SG-75) is a potent potassium channel activator and targets vascular nucleoside diphosphate-dependent K + channels and cardiac ATP-sensitive K + channels (KATP). Nicorandil is a nicotinamide ester with vasodilatory and cardioprotective effects and has the potential for angina and forischemic heart diseases.
|
-
- HY-13422A
-
|
Zatebradine
UL-FS-49 free base; UL-FS-49CL free base
|
HCN Channel
|
Cardiovascular Disease
|
|
Zatebradine (UL-FS-49 (free base); UL-FS-49CL (free base)) is a potent inhibitor of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels with an IC50 value of 1.96 µM. Zatebradine blocks the slow inward current through human HCN1, HCN2, HCN3 and HCN4 channels, with IC50 values of 1.83 µM, 2.21 µM, 1.90 µM and 1.88 µM, respectively.
|
-
- HY-113301
-
-
- HY-N1798
-
-
- HY-124527
-
|
HET0016
|
Cytochrome P450
|
Cardiovascular Disease
|
|
HET0016 is a potent and selective 20-hydroxyeicosatetraenoic acid (20-HETE) synthase inhibitor, with IC50 values of 17.7 nM, 12.1 nM and 20.6 nM for recombinant CYP4A1-, CYP4A2- and CYP4A3-catalyzed 20-HETE synthesis, respectively. HET0016 also is a selective CYP450 inhibitor, which has been shown to inhibit angiogenesis and tumor growth.
|
-
- HY-B0477AS1
-
-
- HY-18990
-
|
GSK180736A
|
ROCK
|
Cardiovascular Disease
|
|
GSK180736A is potent Rho-associated coiled-coil kinase 1 (ROCK1) inhibitor with an IC50 of 100 nM. GSK180736A is also a selective and ATP-competitive G protein-coupled receptor kinase 2 (GRK2) inhibitor with an IC50 of 0.77 μM.
|
-
- HY-N8144
-
|
Niga-ichigoside F1
|
Others
|
Cardiovascular Disease
|
|
Niga-ichigoside F1, an orally active ursane triterpenoid, has antihyperlipidemic and antioxidant activities. Niga-ichigoside F1 can prevent high-fat diet (HFD)-induced hepatic steatosis.
|
-
- HY-18071A
-
|
BI-9627 hydrochloride
|
Sodium Channel
|
Cardiovascular Disease
|
|
BI-9627 hydrochloride is potent sodium-hydrogen exchanger isoform 1 (NHE1) inhibitor, with IC50s of 6 and 31 nM in intracellular pH recovery (pHi) and human platelet swelling assays, respectively. BI-9627 hydrochloride displays >30-fold selectivity against NHE2 and with no measurable inhibitory activity against the NHE3 isoform. BI-9627 hydrochloride shows low DDI (drug-drug interaction) potential, excellent pharmacokinetics in rat and dog, and remarkably potent activity in the isolated heart model of ischemia-reperfusion injury.
|
-
- HY-118824A
-
|
N-Feruloylserotonin
(E/Z)-Moschamine
|
Others
|
Cardiovascular Disease
|
|
N-Feruloylserotonin, an antioxidative component and bioactive serotonin derivative, from the Seed of Carthamus tinctorius L., ameliorates atherosclerosis and distensibility of the aortic wall in Kurosawa and Kusanagi-hypercholesterolemic (KHC) rabbits.
|
-
- HY-135151
-
|
Difluoro atorvastatin
Fluoroatorvastatin
|
Others
|
Cardiovascular Disease
|
|
Difluoro atorvastatin (Fluoroatorvastatin) is an impurity of Atorvastatin. Atorvastatin is an orally active HMG-CoA reductase inhibitor, has the ability to effectively decrease blood lipids. Atorvastatin inhibits human SV-SMC proliferation and invasion with IC50s of 0.39 μM and 2.39 μM, respectively.
|
-
- HY-12760S
-
-
- HY-N4115
-
-
- HY-N3051
-
-
- HY-100254
-
-
- HY-15392
-
|
Chroman 1
|
ROCK
|
Cardiovascular Disease
|
|
Chroman 1 is a highly potent and selective ROCK inhibitor. Chroman 1 is more potent against ROCK2 (IC50=1 pM) than ROCK1 (IC50=52 pM). Chroman 1 also has inhibitory activity against MRCK, with an IC50 of 150 nM.
|
-
- HY-112075
-
-
- HY-128678
-
-
- HY-B1181A
-
-
- HY-U00172
-
|
Ipramidil
C80-1324
|
Others
|
Cardiovascular Disease
|
|
Ipramidil (C80-1324) is a furoxan compound. Ipramidil (C80-1324) reveals marked dilator activity in the coronary circulation of isolated working hearts.
|
-
- HY-107428
-
|
PD-166793
|
MMP
|
Cardiovascular Disease
|
|
PD-166793 is a potent, selective, orally active and wide‐broad spectrum inhibitor of MMP, exhibiting nanomolar potency against MMP-2, MMP-3 and MMP-13 (IC50=4, 7, and 8 nM, respectively) and micromolar potency vs MMP-1, -7 and -9 (IC50=6.0, 7.2, and 7.9 μM, respectively). PD-166793 can attenuate left ventricular remodeling and dysfunction in a rat model of progressive heart failure.
|
-
- HY-A0230A
-
|
Spirapril hydrochloride
SCH 33844 hydrochloride
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
Spirapril (SCH 33844) hydrochloride is a potent angiotensin converting enzyme (ACE) inhibitor with antihypertensive activity. Spirapril competitively binds to ACE and prevents the conversion of angiotensin I to angiotensin II. Spirapril is an orally active prodrug of Spiraprilat and can be used for the research of hypertension, congestive heart failure.
|
-
- HY-P2496
-
-
- HY-P3142
-
-
- HY-10521
-
-
- HY-14187S
-
-
- HY-W011552
-
-
- HY-15876
-
-
- HY-124873
-
|
SERCA2a activator 1
|
Calcium Channel
|
Cardiovascular Disease
|
|
SERCA2a activator 1 (Compound A) is a sarco/endoplasmic reticulum Ca 2+-dependent ATPase 2a (SERCA2a) activator. SERCA2a activator 1 attenuates phospholamban inhibition and enhances the systolic and diastolic functions of the heart. SERCA2a activator 1 can be used for heart failure.
|
-
- HY-111098
-
-
- HY-136588
-
|
trans-R-138727MP
Prasugrel metabolite R-138727MP
|
P2Y Receptor
|
Cardiovascular Disease
|
|
trans-R-138727MP (Prasugrel metabolite R-138727MP) is the active metabolite derivative of Prasugrel (HY-15284). Prasugrel, a thienopyridine and prodrug, inhibits platelet function. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation.
|
-
- HY-B2087S
-
-
- HY-100937
-
|
DPCPX
PD 116948
|
Adenosine Receptor
|
Cardiovascular Disease
|
|
DPCPX (PD 116948), a xanthine derivative, is a highly potent and selective Adenosine A1 receptor antagonist, with a Ki of 0.46 nM in 3H-CHA binding to A1 receptors in rat whole brain membranes.
|
-
- HY-B0592S
-
-
- HY-108555
-
-
- HY-100720
-
-
- HY-101918
-
|
DS-1040 Tosylate
|
Others
|
Cardiovascular Disease
|
|
DS-1040 Tosylate is an orally active, selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (TAFIa) with IC50s of 5.92 nM and 8.01 nM for human and rat TAFIa. DS-1040 Tosylate is a fibrinolysis enhancer for thromboembolic diseases.
|
-
- HY-101355B
-
-
- HY-106080A
-
|
Furegrelate sodium
U-63557A
|
Others
|
Cardiovascular Disease
|
|
Furegrelate Sodium (U-63557A) is a potent, orally available, and selective thromboxane synthase inhibitor. Furegrelate Sodium inhibits human platelet microsomal thromboxane A2 (TxA2) synthase with an IC50 of 15 nM. Furegrelate Sodium is being developed as an antiplatelet agent.
|
-
- HY-N0454
-
-
- HY-W017540
-
|
Cyclocreatine
|
Others
|
Cardiovascular Disease
|
|
Cyclocreatine is a Creatine analogue and acts as a potent bioenergetic protective agent by providing high levels of ATP. Cyclocreatine crosses membranes, enters the brain, and can be phosphorylated and dephosphorylated by creatine kinases.
|
-
- HY-12593
-
|
GS967
|
Sodium Channel
|
Cardiovascular Disease
|
|
GS967 (GS-458967) is a potent, and selective inhibitor of cardiac late sodium current (late INa ) with IC50 values of 0.13 and 0.21 μM for ventricular myocytes and isolated hearts, respectively.
|
-
- HY-12533S
-
|
Disopyramide-d14 tosylate salt
|
Sodium Channel
Potassium Channel
|
Cardiovascular Disease
|
|
Disopyramide-d14 (Dicorantil-d14) tosylate salt is the deuterium labeled Disopyramide. Disopyramide (Dicorantil) is a class IA antiarrhythmic drug with efficacy in ventricular and atrial arrhythmias. Disopyramide blocks the fast inward sodium current of cardiac muscle and prolongs the duration of cardiac action potentials. Disopyramide inhibits HERG encoded potassium channels. Disopyramide also exhibits complex protein binding, and has a potent negative inotropic action.
|
-
- HY-16915
-
|
RPR-260243
|
Potassium Channel
|
Cardiovascular Disease
|
|
RPR-260243, a potent activator of human ether-a-go-go-related gene (hERG), slows deactivation and attenuates inactivation of hERG1 channels. RPR260243-modified HERG currents are inhibited by Dofetilide (IC50=58 nM). RPR260243 displays no activator-like effects on other voltage-dependent ion channels, including the closely related ERG3 K+ channel.
|
-
- HY-B1061
-
-
- HY-B0312S
-
-
- HY-B0384
-
-
- HY-125643
-
-
- HY-U00201
-
-
- HY-12805
-
|
ML171
2-Acetylphenothiazine; 2-APT
|
NADPH Oxidase
|
Cardiovascular Disease
|
|
ML171 (2-Acetylphenothiazine;2-APT) is a potent and selective NADPH oxidase 1 (Nox1) inhibitor that blocks Nox1-dependent ROS generation, with an IC50 of 0.25 μM in HEK293-Nox1 confirmatory assay.
|
-
- HY-B1438
-
-
- HY-B1167
-
|
Ajmaline
Cardiorythmine; (+)-Ajmaline
|
Sodium Channel
|
Cardiovascular Disease
|
|
Ajmaline (Cardiorythmine) is a sodium channel blocking, class 1A anti-arrhythmic agent. Ajmaline blocks HERG currents with an IC50 of 1 μM in HEK cells and 42.3 μM in Xenopus oocytes. Ajmaline can be used for the research of the ventricular tachyarrhythmia.
|
-
- HY-101957
-
|
AG 1295
|
PDGFR
|
Cardiovascular Disease
|
|
AG 1295 is a selective platelet-derived growth factor receptor (PDGFR) tyrosine-kinase inhibitor. AG1295 abolishes autophosphorylation of the PDGFR whereas not affects the autophosphorylation of the EGF receptor.
|
-
- HY-113986
-
|
(R)-Fadrozole
(R)-CGS 16949A free base; FAD286
|
Others
|
Cardiovascular Disease
|
|
(R)-Fadrozole ((R)-CGS 16949A; FAD286) is a potent nonsteroidal inhibitor. (R)-Fadrozole also inhibits human placental aromatase (pIC50 = 6.17) and aldosterone biosynthesis. (R)-Fadrozole reverses cardiac fibrosis in spontaneously hypertensive heart failure rats..
|
-
- HY-132597
-
-
- HY-18775
-
-
- HY-122908
-
|
Atuliflapon
AZD5718
|
FLAP
|
Cardiovascular Disease
|
|
Atuliflapon (AZD5718) is an orally active inhibitor of FLAP (5‑Lipoxygenase activating protein), with an IC50 of 2 nM. Atuliflapon is used in the study for coronary artery disease.
|
-
- HY-111655
-
|
SKA-31
|
Potassium Channel
|
Cardiovascular Disease
|
|
SKA-31 is a potent potassium channel activator with EC50s of 260 nM, 1.9 μM, 2.9 μM, and 2.9 μM for KCa3.1, KCa2.2, KCa2.1 and KCa2.3, respectively. SKA-31 potentiates endothelium-derived hyperpolarizing factor response and lowers blood pressure.
|
-
- HY-100171
-
-
- HY-114953
-
-
- HY-111755
-
-
- HY-105064B
-
|
Zoniporide hydrochloride
CP-597396 hydrochloride
|
Sodium Channel
|
Cardiovascular Disease
|
|
Zoniporide (CP-597396) hydrochloride is a potent and selective inhibitor of sodium-hydrogen exchanger type 1 (NHE-1). Zoniporide hydrochloride inhibits human NHE-1 (IC50=14 nM), and has >150-fold selectivity versus other NHE isoforms. Zoniporide hydrochloride potently inhibits ex vivo NHE-1-dependent swelling of human platelets (IC50=59 nM).
|
-
- HY-B0382S
-
-
- HY-B0968A
-
|
Trimetazidine
|
Autophagy
|
Cardiovascular Disease
|
|
Trimetazidine is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine is an effective antianginal agent and a cytoprotective drug, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine triggers autophagy. Trimetazidine is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor.
|
-
- HY-11021
-
|
Elinogrel
PRT060128
|
P2Y Receptor
|
Cardiovascular Disease
|
|
Elinogrel (PRT060128) is a potent, direct acting, competitive, and reversible platelet P2Y12 antagonist (IC50=20 nM). It is orally and intravenously available and has potent antiplatelet effects.
|
-
- HY-50667S
-
|
Apixaban 13CD3
BMS-562247-01 13CD3
|
Factor Xa
|
Cardiovascular Disease
|
|
Apixaban 13CD3 (BMS-562247-01 13CD3) is a deuterium labeled Apixaban. Apixaban is a highly selective, reversible inhibitor of Factor Xa with Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively.
|
-
- HY-15798
-
-
- HY-P2090A
-
|
Angiopeptin TFA
|
Somatostatin Receptor
Adenylate Cyclase
|
Cardiovascular Disease
|
|
Angiopeptin TFA, a cyclic octapeptide analogue of somatostatin, a weak sst2/sst5 receptor partial agonist with IC50 values of 0.26 nM and 6.92 nM, respectively. Angiopeptin TFA is a potent inhibitor of growth hormone release and insulin-like growth factor-1 (IGF-1) production. Angiopeptin TFA inhibit adenylate cyclase or stimulate extracellular acidification. Angiopeptin TFA has the potential for coronary atherosclerosis research.
|
-
- HY-109877
-
-
- HY-17567C
-
|
Heparin sodium salt (MW 15kDa)
Sodium heparin (MW 15kDa); Sodium heparinate (MW 15kDa)
|
Thrombin
Factor Xa
Autophagy
|
Cardiovascular Disease
|
|
Heparin sodium salt (MW 15kDa) (Sodium heparin (MW 15kDa)) is a polymer of Heparin with the molecular weight of 15kDa. Heparin sodium salt is an anticoagulant which binds reversibly to antithrombin III (ATIII) and greatly accelerates the rate at which ATIII inactivates coagulation enzymes thrombin factor IIa and factor Xa.
|
-
- HY-12533
-
|
Disopyramide
Dicorantil; SC-7031
|
Sodium Channel
Potassium Channel
|
Cardiovascular Disease
|
|
Disopyramide (Dicorantil) is a class IA antiarrhythmic drug with efficacy in ventricular and atrial arrhythmias. Disopyramide blocks the fast inward sodium current of cardiac muscle and prolongs the duration of cardiac action potentials. Disopyramide inhibits HERG encoded potassium channels. Disopyramide also exhibits complex protein binding, and has a potent negative inotropic action.
|
-
- HY-14255
-
-
- HY-14276A
-
|
Gallopamil hydrochloride
Methoxyverapamil hydrochloride
|
Calcium Channel
|
Cardiovascular Disease
|
|
Gallopamil hydrochloride (Methoxyverapamil hydrochloride), a methoxy derivative of Verapamil, is a phenylalkylamine calcium antagonist. Gallopamil hydrochloride inhibits acid secretion in a concentration-dependent manner with an IC50 of 10.9 μM. Gallopamil hydrochloride is a potent antiarrhythmic and vasodilator agent.
|
-
- HY-118969
-
-
- HY-19886
-
|
F 16915
|
Others
|
Cardiovascular Disease
|
|
F 16915, a Docosahexaenoic Acid (DHA, HY-B2167) derivative, is a potent pro-drug of DHA. F 16915 can prevent heart failure-induced atrial fibrillation.
|
-
- HY-17459
-
|
Clopidogrel hydrogen sulfate
(S)-(+)-Clopidogrel bisulfate; (S)-(+)-Clopidogrel hydrogen sulfate
|
Cytochrome P450
P2Y Receptor
|
Cardiovascular Disease
|
|
Clopidogrel hydrogen sulfate is an antiplatelet agent to prevent blood clots. Clopidogrel hydrogen sulfate inhibits CYP2B6 and CYP2C19 with IC50s of 18.2 nM and 524 nM, respectively. Clopidogrel hydrogen sulfate is a potent antithrombotic agent that inhibits ADP-induced platelet aggregation．Clopidogrel hydrogen sulfate also is an orally active P2Y(12) inhibitor.
|
-
- HY-B2106
-
|
Polidocanol
Polyoxyethylene lauryl ether; Polyoxyethyleneglycol Dodecyl Ether
|
Others
|
Cardiovascular Disease
|
|
Polidocanol is a sclerosing agent used successfully to treat extremity and esophageal varices and telangiectasias.
|
-
- HY-U00218
-
-
- HY-W001940
-
-
- HY-U00211
-
-
- HY-109562A
-
|
CCG258208 hydrochloride
GRK2-IN-1 hydrochloride
|
Others
|
Cardiovascular Disease
|
|
GRKs-IN-1 hydrochloride, Compound 14as, has remarkable potency against and selectivity for G protein-coupled receptor kinase 2 GRK2 (IC50=130 nM) and GRK5 (IC50=7.1 μM).
GRKs-IN-1 hydrochloride is a derivative 14as of paroxetine, shows a 100-fold improvement in cardiomyocyte contractility assays over paroxetine.
|
-
- HY-15392A
-
|
Chroman 1 dihydrochloride
|
ROCK
|
Cardiovascular Disease
|
|
Chroman 1 dihydrochloride is a highly potent and selective ROCK inhibitor. Chroman 1 dihydrochloride is more potent against ROCK2 (IC50=1 pM) than ROCK1 (IC50=52 pM).
Chroman 1 dihydrochloride also has inhibitory activity against MRCK, with an IC50 of 150 nM.
|
-
- HY-B0309
-
|
Felodipine
|
Calcium Channel
Autophagy
|
Cardiovascular Disease
|
|
Felodipine, a dihydropyridine, is a potent, vasoselective calcium channel antagonist. Felodipine lowers blood pressure (BP) by selective action on vascular smooth muscle, especially in the resistance vessels. Felodipine, an anti-hypertensive agent, induces autophagy. Felodipine can cross the blood-brain barrier.
|
-
- HY-B0006C
-
-
- HY-12345
-
|
ML365
|
Potassium Channel
|
Cardiovascular Disease
|
|
ML365 is a selective two-pore domain potassium channel KCNK3/TASK1 inhibitor, with an IC50 of 4 nM. ML365 acts as a pharmacological tool that can be used to examine the specific roles of TASK1 channels.
|
-
- HY-108260
-
|
Deferitrin
GT-56-252
|
Others
|
Cardiovascular Disease
|
|
Deferitrin (GT-56-252), a desferrithiocin (DFT) analogue, is an orally active trident iron chelator. Deferitrin is used for chronic iron overload due to transfusional therapy. Deferitrin has the potential for beta-thalassemia major.
|
-
- HY-N1933
-
|
Allocryptopine
|
Potassium Channel
|
Cardiovascular Disease
|
|
Allocryptopine, a derivative of tetrahydropalmatine, is extracted from Corydalis decumbens (Thunb.) Pers. Papaveraceae. Allocryptopine has antiarrhythmic effects and potently blocks human ether-a-go-go related gene (hERG) current.
|
-
- HY-135121
-
|
Ethacizine hydrochloride
Ethacizin; NIK-244
|
Sodium Channel
|
Cardiovascular Disease
|
|
Ethacizine hydrochloride (Ethacizin; NIK-244) is a longer-lasting Class Ic antiarrhythmic agent than Flecainide. Ethacizine hydrochloride (Ethacizin; NIK-244) inhibits the depolarizing current responsible for the intraatrial and His-Purkinje-ventricular conduction.
|
-
- HY-P1164
-
-
- HY-10277
-
|
Odiparcil
SB-424323
|
Thrombin
|
Cardiovascular Disease
|
|
Odiparcil (SB-424323) is an orally active beta-d-thioxyloside analog with antithrombotic activity associated with a reduced risk of adverse bleeding events. Odiparcil (SB-424323) is indirect thrombin inhibitor that exerts its anticoagulant effect through activation of antithrombin II (heparin cofactor II) .
|
-
- HY-135746
-
-
- HY-135388
-
|
ent-Ezetimibe
ent-SCH 58235
|
Drug Metabolite
|
Cardiovascular Disease
|
|
ent-Ezetimibe (ent-SCH 58235) is the RRS-enantiomer of Ezetimibe. Ezetimibe is a potent cholesterol absorption inhibitor. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator.
|
-
- HY-N2548
-
-
- HY-W011641
-
-
- HY-P1106A
-
|
K41498 TFA
|
CFTR
|
Cardiovascular Disease
|
|
K41498 TFA is a potent and highly selective CRF2 receptor antagonist with Ki values of 0.66 nM, 0.62 nM and 425 nM for human CRF2α, CRF2β and CRF1 receptors respectively. K41498 TFA is an analogues of antisauvagine-30 (aSvg-30), inhibits sauvagine-stimulated cAMP accumulation in hCRF2α- and hCRF2β-expressing cells. K41498 TFA can be used for hypotension study.
|
-
- HY-101415
-
|
Coenzyme Q9
Ubiquinone Q9; CoQ9; Ubiquinone 9
|
Endogenous Metabolite
|
Cardiovascular Disease
|
|
Coenzyme Q9 (Ubiquinone Q9), the major form of ubiquinone in rodents, is an amphipathic molecular component of the electron transport chain that functions as an endogenous antioxidant. Coenzyme Q9 attenuates the diabetes-induced decreases in antioxidant defense mechanisms. Coenzyme Q9 improves left ventricular performance and reduces myocardial infarct size and cardiomyocyte apoptosis.
|
-
- HY-12378
-
|
BQ-123
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
BQ-123 is a potent and selective endothelin A (ETA) receptor antagonist with an IC50 of 7.3 nM and a Ki of 25 nM. BQ-123 inhibits endothelin-1-mediated proliferation of human pulmonary artery smooth muscle cells and lowers blood pressure in different rat models of hypertension.
|
-
- HY-B0341
-
|
Nicorandil
SG-75
|
Potassium Channel
|
Cardiovascular Disease
|
|
Nicorandil (SG-75) is a potent potassium channel activator and targets vascular nucleoside diphosphate-dependent K + channels and cardiac ATP-sensitive K + channels (KATP). Nicorandil is a nicotinamide ester with vasodilatory and cardioprotective effects and has the potential for angina and forischemic heart diseases.
|
-
- HY-123846
-
|
MLS-0437605
|
Phosphatase
|
Cardiovascular Disease
|
|
MLS-0437605 is a selective dual-specificity phosphatase 3 (DUSP3) inhibitor with an IC50 of 3.7 μM. MLS-0437605 is more selective for DUSP3 than DUSP22 and other protein tyrosine phosphatases (PTPs).
|
-
- HY-121018
-
|
Daltroban
BM-13505; SKF 96148
|
Prostaglandin Receptor
|
Cardiovascular Disease
|
|
Daltroban (BM-13505) is a selective and specific thromboxane A2 (TXA2) receptor antagonist. Daltroban increase intracellular calcium in vascular smooth muscle cells. Daltroban shows protective effect in reperfusion injury.
|
-
- HY-116078
-
|
CKD-519
|
CETP
|
Cardiovascular Disease
|
|
CKD-519 is a selective and potent cholesteryl ester transfer protein (CETP) inhibitor, which inhibits CETP-mediated transfer of cholesteryl ester in human serum with an IC50 of 2.3 nM.
|
-
- HY-19354
-
|
Aglafoline
Aglafolin; Rocaglamide U; (-)-Methyl rocaglate
|
Others
|
Cardiovascular Disease
|
|
Aglafoline inhibits in a selective and concentration-dependent manner the aggregation and ATP release reaction induced in washed rabbit platelets by PAF (platelet-activating factor).
|
-
- HY-100986
-
|
L-NIO dihydrochloride
|
NO Synthase
|
Cardiovascular Disease
|
|
L-NIO dihydrochloride is a potent, non-selective and NADPH-dependent nitric oxide synthase (NOS) inhibitor, with Kis of 1.7, 3.9, 3.9 μM for neuronal (nNOS), endothelial (eNOS), and inducible (iNOS), respectively. L-NIO dihydrochloride induces a consistentfocal ischemic infarctin rats.
|
-
- HY-111587
-
|
Ifenprodil glucuronide
|
Others
|
Cardiovascular Disease
|
|
Ifenprodil glucuronide is a derivative of Ifenprodil. Ifenprodil is a vasodilator and an inhibitor of platelet aggregation, and Ifenprodil glucuronide has no effect on platelet aggregation and arterial contraction.
|
-
- HY-112143
-
-
- HY-108573
-
|
P-1075
|
Potassium Channel
|
Cardiovascular Disease
|
|
P-1075 is a potent activator of sulfonylurea receptor 2-associated ATP-sensitive potassium channels (SUR2-KIR6), with an EC50 value of 45 nM for SUR2B-KIR6 channel activation. P-1075 also P1075 opens mitochondrial K(ATP) channels and generates reactive oxygen species resulting in cardioprotection of rabbit hearts.
|
-
- HY-112202
-
-
- HY-N7614
-
|
Anemarrhenasaponin A2
Schidigerasaponin F2; Timosaponin AII
|
Others
|
Cardiovascular Disease
|
|
Anemarrhenasaponin A2 (Schidigerasaponin F2) is a steroidal saponin isolated from the rhizomes of Anemarrhena asphodeloides. Anemarrhenasaponin A2 inhibits ADP-induced platelet aggregation.
|
-
- HY-134686
-
|
Edoxaban impurity 4
|
Factor Xa
Thrombin
|
Cardiovascular Disease
|
|
Edoxaban impurity 4 is an impurity of Edoxaban. Edoxaban (DU-176) is a selective, potent and orally active factor Xa (FXa) inhibitor with Kis of 0.561 nM and 2.98 nM for free FXa and prothrombinase, respectively. Edoxaban is an anticoagulant agent and can be used for stroke prevention.
|
-
- HY-135363
-
-
- HY-108658
-
|
MRS2500 tetraammonium
|
P2Y Receptor
|
Cardiovascular Disease
|
|
MRS2500 tetraammonium is a potent, selective and stable antagonist of the P2Y1 receptor (Ki=0.78 nM for recombinant human P2Y1 receptor). MRS2500 tetraammonium inhibits the ADP-induced aggregation of human platelets with an IC50 value of 0.95 nM. Antithrombotic activity.
|
-
- HY-B1170
-
-
- HY-W000450
-
-
- HY-16056
-
|
Arbutamine
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Arbutamine is a short-acting, potent and nonselective β-adrenoceptor agonist that increases heart rate, cardiac contractility, and systolic blood pressure. Arbutamine is a catecholamine for a pharmacological cardiac stress agen.
|
-
- HY-B2087
-
-
- HY-129851
-
|
NTP42
|
Prostaglandin Receptor
|
Cardiovascular Disease
|
|
NTP42 is a thromboxane A2 (TXA2) receptor antagonist with an IC50 of 3.278 nM for antagonizing T prostanoid receptor (TP)- mediated [Ca 2+] mobilization following stimulation of cells with the alternative TP agonist U46609. NTP42 can be used for the treatment of pulmonary arterial hypertension (PAH).
|
-
- HY-B0772A
-
-
- HY-B0432A
-
-
- HY-100655
-
-
- HY-100400A
-
-
- HY-N2509
-
|
Iristectorigenin B
Iristectrigenin B
|
LXR
|
Cardiovascular Disease
|
|
Iristectorigenin B (Iristectrigenin B) is a liver X receptor (LXR) modulator. Iristectrigenin B stimulates the transcriptional activity of both LXR-α and LXR-β.
|
-
- HY-120355A
-
|
AP14145 hydrochloride
|
Potassium Channel
|
Cardiovascular Disease
|
|
AP14145 hydrochloride is a potent KCa2 (SK) channel negative allosteric modulator with an IC50 of 1.1 μM for KCa2.2 (SK2) and KCa2.3 (SK3) channels. AP14145 hydrochloride inhibition strongly depends on two amino acids, S508 and A533 in the channel. AP14145 hydrochloride prolonged atrial effective refractory period (AERP) in rats and demonstrates antiarrhythmic effects in a Vernakalant-resistant porcine model of atrial fibrillation (AF).
|
-
- HY-132583
-
-
- HY-B0918
-
-
- HY-N0666B
-
|
Aspartic acid calcium
Calcium L-aspartate
|
Others
|
Cardiovascular Disease
|
|
Aspartic acid calcium (Calcium L-aspartate) is a chelate where calcium is attached to an amino acid naming L-Aspartic acid. L-Aspartic acid is an amino acid and serves as a building block for proteins in the body.
|
-
- HY-P1164A
-
-
- HY-108494
-
|
CYM50260
|
LPL Receptor
|
Cardiovascular Disease
|
|
CYM50260 is a potent and exquisitely selective sphingosine-1-phosphate 4 receptor (S1P4-R) agonist with an EC50 of 45 nM. CYM50260 displays no activity against S1P1-R, S1P2-R, S1P3-R and S1P5-R.
|
-
- HY-119695A
-
|
Simvastatin acid ammonium
Tenivastatin ammonium
|
Endogenous Metabolite
|
Cardiovascular Disease
|
|
Simvastatin ammonium is an active metabolite of simvastatin lactone mediated by CYP3A4/5 in the intestinal wall and liver (pKa=5.5). Simvastatin ammonium reduces indoxyl sulfate-mediated reactive oxygen species and modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene.
|
-
- HY-18208
-
-
- HY-N5049
-
-
- HY-B0023
-
-
- HY-111372
-
|
Finerenone
BAY 94-8862
|
Mineralocorticoid Receptor
|
Cardiovascular Disease
|
|
Finerenone (BAY 94-8862) is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist (IC50=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold). Finerenone has the potential for cardiorenal diseases research, such as type 2 diabetes mellitus and chronic kidney disease.
|
-
- HY-B0924
-
-
- HY-N6868
-
-
- HY-P1536
-
-
- HY-10655A
-
|
Palosuran hydrochloride
ACT-058362 hydrochloride
|
Urotensin Receptor
|
Cardiovascular Disease
|
|
Palosuran hydrochloride (ACT-058362 hydrochloride) is a potent, selective, and orally active antagonist of urotensin II receptor, with an IC50 of 3.6 nM for CHO cell membranes expressing human recombinant receptors. Palosuran hydrochloride can improves pancreatic and renal function in diabetic rats.
|
-
- HY-108467
-
|
GGsTop
Nahlsgen
|
Others
|
Cardiovascular Disease
|
|
GGsTop (Nahlsgen) is a potent, non-toxic, highly selective and irreversible γ−glutamyl transpeptidase (GGT) inhibitor, with a Ki of 170 μM for Human GGT. GGsTop shows a pKa of 9.71, also exhibits Kons of 150±10 and 51±3 M -1 s -1 against E.coli GGT and human GGT, respectively. GGsTop protects hepatic ischemia-reperfusion injury in rat model.
|
-
- HY-B0735
-
-
- HY-P1471
-
-
- HY-B1742
-
-
- HY-15293B
-
|
JTV-519 hemifumarate
K201 hemifumarate
|
Calcium Channel
|
Cardiovascular Disease
|
|
JTV-519 hemifumarate (K201 hemifumarate) is a Ca 2+-dependent blocker of sarcoplasmic reticulum Ca 2+-stimulated ATPase (SERCA) and a partial agonist of ryanodine receptors in striated muscle. Antiarrhythmic and cardioprotective properties.
|
-
- HY-130353
-
|
Desethylamiodarone hydrochloride
N-desethylamiodarone hydrochloride; LB 33020 hydrochloride
|
Potassium Channel
Autophagy
|
Cardiovascular Disease
|
|
Desethylamiodarone hydrochloride (N-desethylamiodarone hydrochloride) is a major active metabolite of Amiodarone. Desethylamiodarone hydrochloride is formed by CYP3A isoenzymes. Amiodarone is an antiarrhythmic agent for inhibition of ATP-sensitive potassium channel with an IC50 of 19.1 μM.
|
-
- HY-B0665
-
|
Fibrin
|
Others
|
Cardiovascular Disease
|
|
Fibrin, isolated from bovine blood, is an insoluble protein produced in response to bleeding. Fibrin is the major component of the blood clot and is used for coagulation.
|
-
- HY-135328S
-
-
- HY-107414
-
-
- HY-14739
-
|
Choline Fenofibrate
ABT-335
|
PPAR
COX
|
Cardiovascular Disease
|
|
Choline Fenofibrate (ABT-335), a choline salt of Fenofibric acid (HY-B0760), releases free Fenofibric acid in the gastrointestinal tract. Fenofibric acid is a PPAR activator with antihyperlipidemic effect.
|
-
- HY-P1214
-
-
- HY-66010A
-
|
Cinepazide
|
|
Cardiovascular Disease
|
|
Cinepazide is a piperazine derivative and acts as a weak calcium channel blocker. Cinepazide is a potent vasodilator and can be used for the research of cerebrovascular diseases, including ischemic stroke, brain infarct et. al.
|
-
- HY-N7671
-
-
- HY-17369B
-
|
Tirofiban
L700462; MK383
|
Integrin
|
Cardiovascular Disease
|
|
Tirofiban(L700462;MK383) is a potent non-peptide, glycoprotein IIb/IIIa (integrins alphaIIbbetaIII) antagonist
Target: integrin IIb/IIIa
Tirofiban hydrochloride monohydrate blocks platelet aggregation and thrombus formation.
|
-
- HY-B0331
-
-
- HY-U00135
-
-
- HY-B0382
-
-
- HY-10274A
-
|
Dabigatran etexilate mesylate
BIBR 1048MS; Dabigatran etexilate methanesulfonate
|
Others
|
Cardiovascular Disease
|
|
Dabigatran etexilate mesylate (BIBR 1048MS) is an orally active prodrug of Dabigatran. Dabigatran etexilate mesylate has anticoagulant effects and is used for the prophylaxis of venousthromboembolism and stroke due to atrial fibrillation.
|
-
- HY-109066
-
-
- HY-100145
-
-
- HY-101423
-
-
- HY-18600A
-
-
- HY-B1562
-
|
Bopindolol
(±)-Bopindolol
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Bopindolol is an orally active antagonist of β-adrenoceptors (ARs) with partial agonist activity. Bopindolol is non-selective for β1- and β2-ARs and has low affinity for β3-AR subtype. Bopindolol is a prodrug of pindolol and can be used for essential and renovascular hypertension research.
|
-
- HY-70035
-
|
Otamixaban
FXV673
|
Factor Xa
|
Cardiovascular Disease
|
|
Otamixaban(FXV673) is a potent (Ki = 0.5 nM), selective, rapid acting, competitive and reversible fXa inhibitor that effectively inhibits both free and prothrombinase-bound fXa.
|
-
- HY-14286S
-
-
- HY-117549
-
|
Ibrolipim
NO-1886
|
Others
|
Cardiovascular Disease
|
|
Ibrolipim (NO-1886) is an orally active lipoprotein lipase (LPL)-promoting agent. Ibrolipim decreases plasma triglycerides, increases high-density lipoprotein cholesterol levels. Ibrolipim has renoprotective and hypolipidemic effects.
|
-
- HY-131278
-
-
- HY-113313
-
|
Aldosterone
|
Endogenous Metabolite
|
Cardiovascular Disease
|
|
Aldosterone is the primary mineralocorticoid. Aldosterone is a steroid hormone, and it is synthesized and secreted in response to renin-angiotensin system activation (RAS) or high dietary potassium by the zona glomerulosa (ZG) of the adrenal cortex. Aldosterone activity is dependent by the binding and activation of the cytoplasmic/nuclear mineralocorticoid receptor (MR) at cellular level.
|
-
- HY-137446
-
-
- HY-109121
-
|
Reldesemtiv
CK-2127107
|
Others
|
Cardiovascular Disease
|
|
Reldesemtiv (CK-2127107) is a selective, orally active and next-generation fast skeletal muscle troponin activator (FSTA). Reldesemtiv selectively activates fast skeletal myofibrils with an EC50 of 3.4 μM. Reldesemtiv increases exercise performance in a heart failure model.
|
-
- HY-15284
-
|
Prasugrel
PCR 4099
|
P2Y Receptor
|
Cardiovascular Disease
|
|
Prasugrel (PCR 4099), a thienopyridine and prodrug, inhibits platelet function. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation.
|
-
- HY-101759
-
-
- HY-A0154
-
|
Deslanoside
Deacetyllanatoside C; Desacetyllanatoside C
|
Na+/K+ ATPase
Drug Metabolite
|
Cardiovascular Disease
|
|
Deslanoside (Desacetyllanatoside C) is a rapidly acting cardiac glycoside used to treat congestive heart failure and supraventricular arrhythmias due to reentry mechanisms, and to control ventricular rate in the treatment of chronic atrial fibrillation. Deslanoside inhibits the Na-K-ATPase membrane pump, resulting in an increase in intracellular sodium and calcium concentrations .
|
-
- HY-N4213
-
-
- HY-P1471A
-
|
Adrenomedullin (AM) (22-52), human TFA
22-52-Adrenomedullin (human) (TFA)
|
CGRP Receptor
|
Cardiovascular Disease
|
|
Adrenomedullin (AM) (22-52), human (22-52-Adrenomedullin human) TFA, an NH2 terminal truncated adrenomedullin analogue, is an adrenomedullin receptor antagonist. Adrenomedullin (AM) (22-52), human also antagonizes the calcitonin generelated peptide (CGRP) receptor in the hindlimb vascular bed of the cat.
|
-
- HY-128889
-
-
- HY-100873
-
-
- HY-N6084
-
|
Humulone
α-Lupulic acid
|
COX
GABA Receptor
Apoptosis
|
Cardiovascular Disease
|
|
Humulone (α-Lupulic acid), a prenylated phloroglucinol derivative, is a potent cyclooxygenase-2 (COX-2) inhibitor. Humulone acts as a positive modulator of GABAA receptor at low micromolar concentrations. Humulone is an inhibitor of bone resorption. Humulone possesses antioxidant, anti-angiogenic and apoptosis-inducing properties.
|
-
- HY-Z0081
-
|
2S,4R-Sacubitril
|
Others
|
Cardiovascular Disease
|
|
2S,4R-Sacubitril is the impurity of Sacubitril. Sacubitril is approved by the Food and Drug Administration for use in combination with valsartan for the treatment of patients with heart failure.
|
-
- HY-B0655
-
-
- HY-120006A
-
|
(rel)-AR234960
|
ERK
|
Cardiovascular Disease
|
|
(rel)-AR234960 is an active relative configuration of AR234960. AR234960, a non-peptide MAS (a G protein-coupled receptor) agonist, increases both mRNA and protein levels of CTGF via ERK1/2 signaling in HEK293-MAS cells and adult human cardiac fibroblasts.
|
-
- HY-15718A
-
-
- HY-111346
-
-
- HY-100662
-
-
- HY-Y0882
-
-
- HY-100718
-
|
SCH00013
|
Others
|
Cardiovascular Disease
|
|
SCH00013 is a cardiotonic agent that primarily acts via an increase in myofibrillar Ca++ sensitivity, have a significant Ca(2+)sensitizing effect at pH 7.2 to 7.4.
|
-
- HY-101232
-
|
Tiotidine
ICI 125211
|
Histamine Receptor
|
Cardiovascular Disease
|
|
Tiotidine (ICI 125211) is a potent and selective antagonist of histamine H2-receptor (pA2=7.3-7.8 for guinea-pig right atrium). Tiotidine has low affinity for both the H1 and the H3 receptors.
|
-
- HY-P0139
-
|
Gap 27
|
Gap Junction Protein
|
Cardiovascular Disease
|
|
Gap 27, a synthetic connexin43 mimetic peptide, is a gap junction inhibitor. Gap 27 possesses conserved sequence homology to a portion of the second extracellular loop leading into the fourth transmembrane connexin segment.
|
-
- HY-12654
-
-
- HY-129029
-
|
Bisoprolol
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Bisoprolol is a potent, selective and orally active β1-adrenergic receptor blocker. Bisoprolol has little activity on β2-receptor and has the potential for hypertension, coronary artery disease and stable ventricular dysfunction research.
|
-
- HY-15553A
-
-
- HY-101529
-
|
Imanixil
HOE-402(free base)
|
Others
|
Cardiovascular Disease
|
|
Imanixil (HOE-402 free base) is an inducer of the LDL receptor (LDLR). Imanixil (HOE-402 free base) is also a potent cholesterol-lowering compound, which inhibits very low density-lipoprotein (VLDL) production, and consequently attenuates atherosclerosis development.
|
-
- HY-137431
-
|
Asundexian
BAY-2433334
|
Factor Xa
|
Cardiovascular Disease
|
|
Asundexian (BAY 2433334) is an orally active coagulation factor Xia (FXIa) inhibitor. Asundexian binds directly, potently, and reversibly to the active site of FXIa and thereby inhibits its activity. Asundexian inhibits human FXIa in buffer with an IC50 of 1 nM.
|
-
- HY-P1275
-
-
- HY-19414
-
-
- HY-W001583
-
|
Manganese(salen) chloride
EUK-8
|
Others
|
Cardiovascular Disease
|
|
Manganese(salen) chloride (EUK-8), a superoxide dismutase and catalase mimetic, is an antioxidant with oxyradical scavenging properties. Manganese(salen) chloride ameliorates acute lung injury in endotoxemic swine.
|
-
- HY-13236
-
-
- HY-131276
-
-
- HY-19254
-
|
ZD-0892
|
Elastase
|
Cardiovascular Disease
|
|
ZD-0892 is a selective and potent inhibitor of a neutrophil elastase with Kis of 6.7 and 200 nM for human neutrophil elastase and porcine pancreatic elastase, respectively.
|
-
- HY-B0968S
-
|
Trimetazidine-d8 dihydrochloride
|
Autophagy
|
Cardiovascular Disease
|
|
Trimetazidine-d8 dihydrochloride is the deuterium labeled Trimetazidine dihydrochloride. Trimetazidine dihydrochloride is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine dihydrochloride is an effective antianginal agent and a cytoprotective drug, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine dihydrochloride triggers autophagy. Trimetazidine dihydrochloride is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor.
|
-
- HY-N0899
-
-
- HY-N0684S
-
-
- HY-113926
-
|
BAY 60-2770
|
Guanylate Cyclase
|
Cardiovascular Disease
|
|
BAY 60-2770 is a potent, selective, and orally active soluble guanylyl cyclase (sGC) activator. BAY 60-2770 increases the activity of sGC in a nitric oxide-independent manner. BAY 60-2770 shows antifibrotic effect.
|
-
- HY-P2539
-
-
- HY-U00344
-
-
- HY-16774
-
-
- HY-105686
-
-
- HY-U00209
-
-
- HY-128561
-
-
- HY-117281S
-
-
- HY-A0093
-
-
- HY-14917
-
-
- HY-13289
-
|
Nepicastat
SYN117; RS-25560-197
|
Dopamine β-hydroxylase
|
Cardiovascular Disease
|
|
Nepicastat (SYN117) is a selective, potent, and orally active inhibitor of dopamine-beta-hydroxylase. Nepicastat (SYN117) produces concentration-dependent inhibition of bovine (IC50=8.5 nM) and human (IC50=9 nM) dopamine-beta-hydroxylase. Nepicastat (SYN117) can cross the blood-brain barrier (BBB).
|
-
- HY-19396
-
|
Ingliforib
CP 368296; GPi 296
|
Others
|
Cardiovascular Disease
|
|
Ingliforib (CP 368296) is a glycogen phosphorylase inhibitor, with IC50s of 52, 352 and 150 nM for liver, muscle and brain glycogen phosphorylase, and has cardioprotective activity.
|
-
- HY-125989
-
|
2-Methylthio-AMP
2-MeSAMP; 2-Methylthioadenosine 5′-monophosphate; 2-Methylthioadenosine 5′-phosphate
|
P2Y Receptor
|
Cardiovascular Disease
|
|
2-Methylthio-AMP (2-MeSAMP) is a selective and direct P2Y12 antagonist. 2-Methylthio-AMP is an inhibitor of ADP-dependent platelet aggregation.
|
-
- HY-114672
-
|
MBCQ
|
Phosphodiesterase (PDE)
|
Cardiovascular Disease
|
|
MBCQ is a potent and selective cGMP-specific phosphodiesterase (PDE V; PDE5) inhibitor with an IC50 of 19 nM. MBCQ lacks inhibitory activity toward other PDE isozymes (all IC50s>100 μM). MBCQ dilates coronary arteries via specific inhibition of cGMP-PDE.
|
-
- HY-N2484
-
|
Methylnissolin
Astrapterocarpan
|
PDGFR
ERK
|
Cardiovascular Disease
|
|
Methylnissolin (Astrapterocarpan), isolated from Astragalus membranaceus, inhibits platelet-derived growth factor (PDGF)-BB-induced cell proliferation with an IC50 of 10 μM. Methylnissolin inhibits PDGF-BB-induced phosphorylation of extracellular signal-regulated kinase 1/2 (ERIC1/2) mitogen-activated protein (MAP) kinase. Methylnissolin inhibits PDGF-BB-induced vascular smooth muscle cell proliferation by inhibition of the ERK1/2 MAP kinase cascade.
|
-
- HY-P3138
-
|
(Sar1)-Angiotensin II
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
(Sar1)-Angiotensin II, an analogue of Angiotensin II, is a specific agonist of angiotensin AT1 receptor. (Sar1)-Angiotensin II binds to brain membrane-rich particles, with a Kd of 2.7 nM. (Sar1)-Angiotensin II can stimulate protein synthesis and cell growth in embryonic chick myocytes.
|
-
- HY-113673
-
|
A-935142
|
Potassium Channel
|
Cardiovascular Disease
|
|
A-935142 is a human ether-a-go-go-related gene (hERG, Kv 11.1) channel activator. A-935142 enhances hERG current in a complex manner by facilitation of activation, reduction of inactivation, and slowing of deactivation, and abbreviates atrial and ventricular repolarization.
|
-
- HY-112624
-
|
Dextran
Dextran 40
|
Others
|
Cardiovascular Disease
|
|
Dextran (Dextran 40) has an inhibitory effect on thrombocyte aggregation and coagulation factors and is used as a plasma volume expander.
|
-
- HY-U00309
-
-
- HY-B1140
-
-
- HY-108322
-
-
- HY-13817
-
-
- HY-17404
-
-
- HY-100750
-
-
- HY-14181
-
-
- HY-102054
-
-
- HY-50768
-
-
- HY-18681
-
|
Voxelotor
GBT 440
|
Others
|
Cardiovascular Disease
|
|
Voxelotor (GBT 440) is a potent inhibitor of haemoglobin S (HbS) polymerization. Voxelotor has the potential for sickle cell disease (SCD) treatment.
|
-
- HY-10309
-
|
Sibrafiban
RO 48-3657
|
Integrin
|
Cardiovascular Disease
|
|
Sibrafiban (RO 48-3657) is the orally active, nonpeptide, double-prodrug of Ro 44-3888 and a selective glycoprotein IIb/IIIa receptor antagonist. Sibrafiban inhibits platelet aggregation.
|
-
- HY-N2237
-
-
- HY-N3216
-
-
- HY-14233
-
-
- HY-110390
-
-
- HY-15472
-
-
- HY-N2282
-
-
- HY-N4309
-
|
Lotusine
|
Others
|
Cardiovascular Disease
|
|
Lotusine is a pure alkaloid extracted from the green seed embryo of Nelumbo nucifera Gaertn. Lotusine shows effects on the action potentials in myocardium and slow inward current in cardiac Purkinje fibers.
|
-
- HY-76652
-
-
- HY-B0997
-
|
Hydroquinidine
Dihydroquinidine; (+)-Hydroquinidine; Hydroconquinine
|
Others
|
Cardiovascular Disease
|
|
Hydroquinidine (Dihydroquinidine) is a derivative of Quinidine (an antiarrhythmic agent). Hydroquinidine prolongs the QT interval and has antiarrhythmic efficacy.
|
-
- HY-B0224
-
-
- HY-N3513
-
|
Mulberrin
Kuwanon C
|
Others
|
Cardiovascular Disease
|
|
Mulberrin is a strong inhibitor of organic anion-transporting polypeptide 2B1 (OATP2B1)-mediated estrone-3-sulfate (E3S) uptake with an IC50 value being 1.8 ±1.5 μM.
|
-
- HY-108351
-
|
IM-54
|
Others
|
Cardiovascular Disease
|
|
IM-54 is a selective inhibitor of oxidative stress-induced necrosis. IM-54 shows potent inhibitory activity against H2O2-induced necrosis. IM-54 acts as a potential cardioprotective agent and biological tool for investigating the molecular mechanisms of cell death.
|
-
- HY-N4266
-
|
Vinaginsenoside R8
|
Others
|
Cardiovascular Disease
|
|
Vinaginsenoside R8, a triterpenoid glycoside isolated from the rhizomes of Panacis majoris. Vinaginsenoside R8 displays activities against adenosine diphosphate (ADP)-induced platelet aggregation (IC50=25.18 μM).
|
-
- HY-109039
-
|
Praliciguat
IW-1973
|
Guanylate Cyclase
|
Cardiovascular Disease
|
|
Praliciguat (IW-1973) is a potent and orally active soluble guanylate cyclase stimulator, enhances NO signaling, acts as a vasodilator. Praliciguat (IW-1973) stimulates sGC in HEK-293 cells with an EC50 of 197 nM.
|
-
- HY-N2638
-
|
Ilexsaponin A
|
Others
|
Cardiovascular Disease
|
|
Ilexsaponin A, isolated from the root of Ilex pubescens, attenuates ischemia-reperfusion-induced myocardial injury through anti-apoptotic pathway. Ilexsaponin A can reduce myocardial infarct size, lower the serum levels of LDH, AST and CK-MB, increase cellular viability and inhibit apoptosis in hypoxia/reoxygenation cardiomyocytes.
|
-
- HY-U00208
-
-
- HY-12502B
-
-
- HY-139400
-
|
FTX-6058
|
Histone Methyltransferase
|
Cardiovascular Disease
|
|
FTX-6058 is a potent and orally active inhibitor of Embryonic Ectoderm Development (EED). FTX-6058 can induce HbF protein expression in cell and murine models. FTX-6058 can be used for the research of select hemoglobinopathies, including sickle cell disease and β-thalassemia.
|
-
- HY-120083
-
-
- HY-15574
-
-
- HY-100298
-
-
- HY-100160
-
-
- HY-10163
-
|
Dabigatran
BIBR 953; BIBR 953ZW
|
Thrombin
|
Cardiovascular Disease
|
|
Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM).
|
-
- HY-77521
-
-
- HY-W015007
-
|
Metyrosine
|
COX
|
Cardiovascular Disease
|
|
Metyrosine is a selective tyrosine hydroxylase enzyme inhibitor. Metyrosine exerts anti-inflammatory and anti-ulcerative effects. Metyrosine significantly inhibits high COX-2 activity. Metyrosine is a very effective agent for blood pressure control.
|
-
- HY-108495
-
|
CYM50308
ML248
|
LPL Receptor
|
Cardiovascular Disease
|
|
CYM50308 (ML248) is a potent, selective and high affinity sphingosine-1-phosphate receptor 4 (S1P4-R) agonist with an EC50 of 56 nM. CYM50308 displays 37-fold more selective for S1P4-R than S1P5-R. CYM50308 has no activity at S1P1-R, S1P2-R and S1P3-R subtypes at concentrations up to 25 μM.
|
-
- HY-101054
-
-
- HY-B0204A
-
-
- HY-B0375
-
-
- HY-109592
-
-
- HY-111536
-
-
- HY-B0378A
-
-
- HY-B1582A
-
-
- HY-14254
-
|
Olprinone Hydrochloride
Loprinone Hydrochloride
|
Phosphodiesterase (PDE)
|
Cardiovascular Disease
|
|
Olprinone (Loprinone) Hydrochloride is a potent phosphodiesterase (PDE) 3 inhibitor, with IC50s of 150, 100, 0.35 and 14 μM for PDE1, PDE2, PDE3 and PDE4, respectively. Olprinone Hydrochloride is used for the research of heart failure due to its positive inotropic and vasodilative effects. Anti-inflammatory activity.
|
-
- HY-13422
-
|
Zatebradine hydrochloride
UL-FS-49; UL-FS-49CL
|
HCN Channel
|
Cardiovascular Disease
|
|
Zatebradine (UL-FS-49 (free base)) is a potent inhibitor of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels with an IC50 values 1.96 µM. Zatebradine blocks the slow inward current through human HCN1, HCN2, HCN3 and HCN4 channels, with IC50 values of 1.83 µM, 2.21 µM, 1.90 µM and 1.88 µM, respectively.
|
-
- HY-B0592
-
|
Trandolapril
RU44570
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
Trandolapril (RU44570) is a nonsulfhydryl prodrug that is hydrolysed to the active diacid Trandolaprilat. Trandolapril is an orally administered angiotensin converting enzyme (ACE) inhibitor that has been used in the treatment of hypertension and congestive heart failure (CHF), and after myocardial infarction (MI).
|
-
- HY-101109
-
-
- HY-W050000
-
-
- HY-112264
-
-
- HY-N1982
-
|
Denudatine
|
Others
|
Cardiovascular Disease
|
|
Denudatine, is primarily isolated from plants of the genera Aconitum and Delphinium. Denudatine has effects on action potential of ventricular fibers and inhibits arrhythmogenic action of aconitine.
|
-
- HY-101124
-
-
- HY-117970
-
|
MMPI-1154
|
MMP
|
Cardiovascular Disease
|
|
MMPI-1154 is a promising novel cardio-cytoprotective imidazole-carboxylic acid (ICA) MMP-2 inhibitor(IC50=6.6 μM) and can be used for the study of acute myocardial infarction. MMPI-1154 also inhibits the activity of MMP-13, MMP-1 and MMP-9 with IC50s of 1.8 μM,10 μM, and 13 μM, respectively.
|
-
- HY-135774
-
|
6-Hydroxybenzbromarone
|
Drug Metabolite
Phosphatase
|
Cardiovascular Disease
|
|
6-Hydroxybenzbromarone is the major metabolite of Benzbromarone with a longer half-life and greater pharmacological potency than the parent compound. 6-Hydroxybenzbromarone is a protein Eyes Absent 3 (EYA3) inhibitor with an IC50 value of 21.5 μM. 6-Hydroxybenzbromarone is an angiogenic agent, has strong inhibitory effects on cell migration, tubulogenesis, and angiogenic sprouting.
|
-
- HY-103316
-
|
trans-Ned 19
|
Calcium Channel
|
Cardiovascular Disease
|
|
trans-Ned 19, a NAADP antagonist and TPC blocker, suppresses the calcium signal in human umbilical vein endothelial cells (HUVEC) and the rat aorta relaxation in response to low histamine concentrations.
|
-
- HY-101308
-
|
MRS2179 tetrasodium
|
P2Y Receptor
|
Cardiovascular Disease
|
|
MRS2179 tetrasodium is a competitive P2Y1 receptor antagonist, with a Kb of 102 nM and a pA2 of 6.99 for turkey P2Y1 receptor. MRS2179 tetrasodium is selective for P2Y1 over P2X1 (IC50=1.15 µM), P2X3 (12.9 µM), P2X2, P2X4, P2Y2, P2Y4, and P2Y6 receptors. MRS2179 tetrasodium inhibits platelet aggregation.
|
-
- HY-N9380
-
-
- HY-B0686
-
-
- HY-N2299
-
|
Morusinol
|
Others
|
Cardiovascular Disease
|
|
Morusinol is a flavonoid isolated from Morus alba root bark. Morusinol has an antiplatelet activity and significantly inhibits arterial thrombosis in vivo.
|
-
- HY-101649
-
-
- HY-U00378
-
-
- HY-B0804
-
|
Nadolol
SQ-11725
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Nadolol (SQ-11725) is a non-selective and orally active β-adrenergic receptors blocker and is a substrate of organic anion transporting polypeptide 1A2 (OATP1A2). Nadolol has the the potential for high blood pressure, angina pectoris and vascular headaches research.
|
-
- HY-P1519B
-
-
- HY-103193
-
|
NKH477
Colforsin dapropate hydrochloride
|
Adenylate Cyclase
|
Cardiovascular Disease
|
|
NKH477 (Colforsin dapropate hydrochloride) directly activates the catalytic unit of adenylate cyclase and increases intracellular cAMP. NKH477 is a forskolin derivative that improves cardiac failure mainly through its beneficial effects on diastolic cardiac function. NKH477 exerts an antiproliferative effect in vivo with an altered cytokine profile to inhibit the acute rejection of rat orthotopic lung allografts.
|
-
- HY-P0318
-
-
- HY-B0093
-
-
- HY-Z0075
-
|
(Z)2S,4R-Sacubitril
|
Others
|
Cardiovascular Disease
|
|
(Z)2S,4R-Sacubitril is the impurity of Sacubitril. Sacubitril is approved by the Food and Drug Administration for use in combination with valsartan for the treatment of patients with heart failure.
|
-
- HY-P1839
-
|
Angiotensin I/II (1-5)
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
Angiotensin I/II 1-5 is a peptide that contains the amino acids 1-5, which is converted from Angiotensin I/II. Angiotensin I is formed by the action of renin on angiotensinogen. Angiotensin II is produced from angiotensin I. Angiotensin II has been investigated for the treatment, basic science, and diagnostic of Hypertension, Renin Angiotensin System, and Idiopathic Membranous Nephropathy.
|
-
- HY-A0021S
-
-
- HY-19614
-
|
BMS-795311
|
CETP
|
Cardiovascular Disease
|
|
BMS-795311 is a potent and orally bioavailable inhibitor of cholesteryl ester transfer protein (CETP), with IC50s of 4 nM in an enzyme-based scintillation proximity assay (SPA) and 0.22 μM in a human whole plasma assay (hWPA), respectively.
|
-
- HY-17500
-
|
Ataciguat
HMR-1766
|
Guanylate Cyclase
|
Cardiovascular Disease
|
|
Ataciguat (HMR-1766) is a nitric oxide-independent soluble guanylate cyclase (sGC) activator. Ataciguat is able to activate the ferric heme-iron redox form of sGC that stimulate the production of cyclic GMP (cGMP). Ataciguat exhibits vasodilator effects.
|
-
- HY-N7607
-
-
- HY-112627
-
-
- HY-B0612E
-
-
- HY-101404A
-
-
- HY-B0615
-
|
Moricizine
Moracizine
|
Sodium Channel
|
Cardiovascular Disease
|
|
Moricizine (Moracizine), a phenothiazine derivative, inhibits the rapid inward sodium current (INa) across myocardial cell membranes. Moricizine is an antiarrhythmia agent and has the potential for ventricular tachycardia.
|
-
- HY-B1587
-
-
- HY-12531
-
|
Encainide hydrochloride
MJ9067 hydrochloride
|
Others
|
Cardiovascular Disease
|
|
Encainide (MJ9067) hydrochloride is an antiarrhythmic drug with class IC activity. Encainide has the potential for life-threatening ventricular arrhythmias, symptomatic ventricular arrhythmias and supraventricular arrhythmias research.
|
-
- HY-N2929
-
-
- HY-14667
-
|
Lomitapide
AEGR-733; BMS-201038
|
Others
|
Cardiovascular Disease
|
|
Lomitapide (AEGR-733; BMS-201038) is a potent inhibitor of microsomal triglyceride-transfer protein (MTP) with an IC50 of 8 nM in vitro.
|
-
- HY-N1974
-
-
- HY-U00383
-
-
- HY-118543
-
|
TM6089
|
HIF/HIF Prolyl-Hydroxylase
|
Cardiovascular Disease
|
|
TM6089 is a unique Prolyl Hydroxylase (PHD) inhibitor which stimulates HIF activity without iron chelation and induces angiogenesis and exerts organ protection against ischemia. Local administration of TM6089 enhances angiogenesis, and oral administration stimulates HIF activity in transgenic rats expressing a hypoxia-responsive reporter vector.
|
-
- HY-U00274
-
-
- HY-18206A
-
-
- HY-100471
-
-
- HY-109190
-
|
Seralutinib
GB002; PK10571
|
PDGFR
|
Cardiovascular Disease
|
|
Seralutinib (GB002) is an inhaled PDGFRα and PDGFRβ inhibitor. Seralutinib (GB002) is used in the study for pulmonary arterial hypertension.
|
-
- HY-B1109
-
-
- HY-10627
-
|
GW3965
|
LXR
|
Cardiovascular Disease
|
|
GW3965 is a potent, selective liver X receptor (LXR) agonist with EC50s of 190 nM and 30 nM for hLXRα and hLXRβ, respectively.
|
-
- HY-B0112
-
|
Minoxidil
U10858
|
Potassium Channel
|
Cardiovascular Disease
|
|
Minoxidil (U10858) is an ATP-sensitive potassium (KATP) channel opener, a potent oral antihypertensive agent and a peripheral vasodilator that promotes vasodilation also affects hair growth. Minoxidil is also a potent inhibitor of soybean lipoxygenaseare with an IC50 of 20 μM.
|
-
- HY-N6243
-
-
- HY-101274
-
-
- HY-101312
-
-
- HY-N3460
-
-
- HY-101408
-
-
- HY-19736
-
-
- HY-50903S
-
|
Rivaroxaban D4
BAY 59-7939 D4
|
Factor Xa
|
Cardiovascular Disease
|
|
Rivaroxaban D4 (BAY 59-7939 D4) is a deuterium labeled Rivaroxaban. Rivaroxaban is a highly potent，selective and direct Factor Xa (FXa) inhibitor, achieving a strong gain in anti-FXa potency (IC50 0.7 nM; Ki 0.4 nM).
|
-
- HY-78847
-
|
2R,4S-Sacubitril
|
Others
|
Cardiovascular Disease
|
|
2R,4S-Sacubitril is the impurity of Sacubitril. Sacubitril is approved by the Food and Drug Administration for use in combination with valsartan for the treatment of patients with heart failure.
|
-
- HY-I0400
-
-
- HY-106450
-
|
Binodenoson
MRE-0470; WRC 0470
|
Adenosine Receptor
|
Cardiovascular Disease
|
|
Binodenoson (MRE-0470) is a potent and selective A2A adenosine receptor agonist (KD=270 nM). Binodenoson is being developed as a short-acting coronary vasodilator as an adjunct to radiotracers for use in myocardial stress imaging.
|
-
- HY-N0518
-
|
Toddalolactone
|
PAI-1
|
Cardiovascular Disease
|
|
Toddalolactone, a main component of Toddalia asiatica, inhibits the activity of recombinant human plasminogen activator inhibitor-1 (PAI-1), with an IC50 value of 37.31 μM.
|
-
- HY-14184S
-
|
Macitentan D4
ACT-064992 D4
|
Endothelin Receptor
Apoptosis
|
Cardiovascular Disease
|
|
Macitentan D4 (ACT-064992 D4) is a deuterium labeled Sulfamethoxazole. Macitentan is an orally active, non-peptide dual ETA and ETB (endothelin) receptor antagonist. Macitentan has the potential for idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH).
|
-
- HY-105064D
-
|
Zoniporide hydrochloride hydrate
CP-597396 hydrochloride hydrate
|
Sodium Channel
|
Cardiovascular Disease
|
|
Zoniporide (CP-597396) hydrochloride hydrate is a potent and selective inhibitor of sodium-hydrogen exchanger type 1 (NHE-1). Zoniporide hydrochloride hydrate inhibits human NHE-1 (IC50=14 nM), and has >150-fold selectivity versus other NHE isoforms. Zoniporide hydrochloride hydrate potently inhibits ex vivo NHE-1-dependent swelling of human platelets (IC50=59 nM).
|
-
- HY-114086
-
|
ML359
|
Others
|
Cardiovascular Disease
|
|
ML359 is a potent, selctive and reversible inhibitor of protein disulfide isomerase (PDI), with an IC50 of 250 nM. ML359 can prevent thrombus formation in vivo.
|
-
- HY-W042039
-
-
- HY-N5057
-
|
Przewalskinic acid A
|
Others
|
Cardiovascular Disease
|
|
Przewalskinic acid A is a phenolic acid found in the Salvia przewalskii Maxim herb. Phenolic acids show potent antioxidant activities and potential effects in protecting against brain and heart damage caused by ischemia reperfusion.
|
-
- HY-17369AS
-
-
- HY-101069
-
-
- HY-B0753
-
-
- HY-122560A
-
|
VU0134992 hydrochloride
|
Potassium Channel
|
Cardiovascular Disease
|
|
VU0134992 hydrochloride is the first subtype-preferring, orally active and selective Kir4.1 potassium channel pore blocker, with an IC50 of 0.97 µM. VU0134992 hydrochloride is 9-fold selective for homomeric Kir4.1 over Kir4.1/5.1 concatemeric channels (IC50=9 µM) at -120 mV.
|
-
- HY-15284B
-
|
Prasugrel (Maleic acid)
PCR 4099 (Maleic acid)
|
P2Y Receptor
|
Cardiovascular Disease
|
|
Prasugrel (PCR 4099) Maleic acid is a thienopyridine and prodrug, inhibits platelet function. Prasugrel Maleic acid is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation.
|
-
- HY-12502
-
-
- HY-101628
-
-
- HY-P0143
-
-
- HY-15847
-
|
HS38
|
DAPK
|
Cardiovascular Disease
|
|
HS38 is a potent, selective, and ATP-competitive inhibitor of death-associated protein kinase 1 (DAPK1) and zipper-interacting protein kinase (ZIPK, also called DAPK3), with Kds of 300 nM and 280 nM, respectively. HS38 is also a PIM3 inhibitor with an IC50 of 200 nM. HS38 can be used for the research of smooth muscle related disorders.
|
-
- HY-B1654
-
-
- HY-B1191
-
-
- HY-P0205B
-
-
- HY-14304A
-
|
Zinterol hydrochloride
MJ 9184 hydrochloride
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Zinterol hydrochloride (MJ 9184 hydrochloride) is a potent and selective β2-adrenoceptor agonist. Zinterol hydrochloride increases ICa in a concentration-dependent manner with an EC50 of 2.2 nM. Zinterol hydrochloride induces ventricular arrhythmias in conscious heart failure rabbits.
|
-
- HY-135381
-
-
- HY-19765
-
|
GSK2798745
|
TRP Channel
|
Cardiovascular Disease
|
|
GSK2798745 is a first-in-class, highly potent, selective, orally active transient receptor potential vanilloid 4 (TRPV4) ion channel blocker with IC50s of 1.8 and 1.6 nM for hTRPV4 and rTRPV4, respectively. GSK2798745 is used in research for the treatment of pulmonary edema associated with congestive heart failure.
|
-
- HY-Y1620
-
-
- HY-90009
-
|
Nortadalafil
Demethyl Tadalafil
|
Phosphodiesterase (PDE)
|
Cardiovascular Disease
|
|
Nortadalafil is demethyl Tadalafil, which is a PDE5 inhibitor, currently marketed in pill form for treating erectile dysfunction (ED) under the name Cialis; and under the name Adcirca for the treatment of pulmonary arterial hypertension.
|
-
- HY-N0553
-
-
- HY-B0387
-
-
- HY-17402S1
-
-
- HY-N0660
-
-
- HY-10264B
-
|
Edoxaban tosylate monohydrate
DU-176b monohydrate
|
Factor Xa
Thrombin
|
Cardiovascular Disease
|
|
Edoxaban tosylate monohydrate (DU-176b monohydrate) is a selective, potent and orally active factor Xa (FXa) inhibitor with Kis of 0.561 nM and 2.98 nM for free FXa and prothrombinase, respectively. Edoxaban tosylate monohydrate is an anticoagulant agent and can be used for stroke prevention. Edoxaban tosylate monohydrate is a also weak inhibitor of thrombin and factor IXaβ (FIXa), with Kis of 6.00 μM and 41.7 μM, respectively, exhibits >10 000-fold selectivity for FXa. Edoxaban tosylate monohydrate has antithrombotic properties and has potential for thromboembolic diseases treatment.
|
-
- HY-17567A
-
|
Heparin sodium salt
Sodium heparin; Sodium heparinate
|
Thrombin
Factor Xa
Autophagy
|
Cardiovascular Disease
|
|
Heparin sodium salt (Sodium heparin) is an anticoagulant which binds reversibly to antithrombin III (ATIII) and greatly accelerates the rate at which ATIII inactivates coagulation enzymes thrombin factor IIa and factor Xa. Heparin sodium salt significantly inhibits exosome-cell interactions.
|
-
- HY-B0165CS
-
-
- HY-N5037
-
|
Ilexoside D
|
Others
|
Cardiovascular Disease
|
|
Ilexoside D is isolated from the roots of Ilex pubescens Hook. et Arn. Ilexoside D has the anti-tissue factor activity as well as the antithrombotic activity.
|
-
- HY-15407
-
-
- HY-N3670
-
|
Cycloolivil
Isoolivil
|
Others
|
Cardiovascular Disease
|
|
Cycloolivil (Isoolivil) is a natural polyphenolic compound with a significant radical scavenging activity. Antioxidant and Antiaggregant effects.
|
-
- HY-B0782S
-
-
- HY-100795A
-
-
- HY-U00186
-
-
- HY-P0316A
-
|
TP508 TFA
|
Thrombin
NO Synthase
|
Cardiovascular Disease
|
|
TP508 TFA is a 23-amino acid nonproteolytic thrombin peptide that represents a portion of the receptor-binding domain of thrombin molecule. TP508 TFA activates endothelial NO synthase (eNOS) and stimulates production of NO in human endothelial cells. TP508 TFA activates endothelial cells and stem cells to revascularize and regenerate tissues.
|
-
- HY-B0432AS3
-
|
Propafenone-d5 (hydrochloride)(Ethyl)
|
Sodium Channel
|
Cardiovascular Disease
|
|
Propafenone-d5 hydrochloride(Ethyl) (SA-79-d5 hydrochloride(Ethyl)) is the deuterium labeled Propafenone hydrochloride. Propafenone (SA-79）hydrochloride is a class of anti-arrhythmic medication, which treats illnesses associated with rapid heart beats such as atrial and ventricular arrhythmias.
|
-
- HY-N3164
-
-
- HY-U00149
-
-
- HY-106446
-
-
- HY-B1107
-
|
Naftidrofuryl oxalate
Nafronyl oxalate salt
|
5-HT Receptor
|
Cardiovascular Disease
|
|
Naftidrofuryl oxalate (Nafronyl oxalate salt) is a drug used in the management of peripheral and cerebral vascular disorders as a vasodilator, enhance cellular oxidative capacity, and may also be a 5-HT2 receptor antagonist.
|
-
- HY-50903
-
|
Rivaroxaban
BAY 59-7939
|
Factor Xa
|
Cardiovascular Disease
|
|
Rivaroxaban (BAY 59-7939) is a highly potent, selective and direct Factor Xa (FXa) inhibitor, achieving a strong gain in anti-FXa potency (IC50 0.7 nM; Ki 0.4 nM).
|
-
- HY-N3063
-
|
Pimaric acid
|
Others
|
Cardiovascular Disease
|
|
Pimaric acid is a resin acid that has been found in A. cordata and various pines. Pimaric acid reduces mRNA expression, protein levels, and promoter activity of matrix metalloproteinase-9 (MMP-9) in TNF-α-stimulated human aortic smooth muscle cells (HASMCs).
|
-
- HY-14276
-
|
Gallopamil
Methoxyverapamil
|
Calcium Channel
|
Cardiovascular Disease
|
|
Gallopamil (Methoxyverapamil), a methoxy derivative of Verapamil, is a phenylalkylamine calcium antagonist. Gallopamil inhibits acid secretion in a concentration-dependent manner with an IC50 of 10.9 μM. Gallopamil is a potent antiarrhythmic and vasodilator agent.
|
-
- HY-135328AS
-
|
Norverapamil D7 hydrochloride
(±)-Norverapamil D7 hydrochloride; D591 D7 hydrochloride
|
Calcium Channel
|
Cardiovascular Disease
|
|
Norverapamil D7 ((±)-Norverapamil D7) hydrochloride is a deuterium labeled Norverapamil. Norverapamil ((±)-Norverapamil), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor.
|
-
- HY-10787
-
|
Ximelagatran
H 376/95
|
Thrombin
|
Cardiovascular Disease
|
|
Ximelagatran (H 376/95) is an orally active thrombin inhibitor that selectively and competitively inhibits both free and clot-bound thrombin. Ximelagatran is an anticoagulant agent with a rapid onset of anticoagulant effect, predictable, dose-dependent pharmcokinetics and pharmacodynamics.
|
-
- HY-17429
-
|
Flecainide acetate
R-818
|
Sodium Channel
|
Cardiovascular Disease
|
|
Flecainide acetate (R-818) is a class 1C antiarrhythmic drug especially used for the management of supraventricular arrhythmia; works by blocking the Nav1.5 sodium channel in the heart, causing prolongation of the cardiac action potential.
|
-
- HY-100771
-
-
- HY-U00370
-
-
- HY-13104
-
-
- HY-107396
-
|
YM-750
|
Acyltransferase
|
Cardiovascular Disease
|
|
YM-750 is a potent acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor (IC50=0.18 μM). ACAT catalyzes the formation of cholesteryl esters from cholesterol and long-chain fatty-acyl-coenzyme A.
|
-
- HY-107997
-
-
- HY-103227
-
-
- HY-118628
-
-
- HY-15407S
-
|
Sacubitril-d4
AHU-377-d4
|
Neprilysin
|
Cardiovascular Disease
|
|
Sacubitril-d4 (AHU-377-d4) is the deuterium labeled Sacubitril. Sacubitril (AHU-377) is a potent NEP inhibitor with an IC50 of 5 nM. Sacubitril (AHU-377) is a component of the heart failure medicine LCZ696.
|
-
- HY-U00175
-
-
- HY-N1155
-
-
- HY-108566
-
-
- HY-16104
-
-
- HY-B0279
-
-
- HY-50667
-
|
Apixaban
BMS-562247-01
|
Factor Xa
|
Cardiovascular Disease
|
|
Apixaban (BMS-562247-01) is a highly selective, reversible and orally active inhibitor of Factor Xa with Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively. Apixaban is in development for the prevention and treatment of various thromboembolic diseases.
|
-
- HY-117743
-
|
Eprosartan
SKF-108566J free base
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
Eprosartan (SKF-108566J free base) is a selective, competitive, nonpeptid and orally active angiotensin II receptor antagonist, used as an antihypertensive. Eprosartan binds angiotensin II receptor with IC50s of 9.2 nM and 3.9 nM in rat and human adrenal cortical membranes, respectively .
|
-
- HY-B0930
-
-
- HY-125112
-
-
- HY-B0556
-
|
Tetrahydrozoline
Tetryzoline
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Tetrahydrozoline (Tetryzoline), a derivative of imidazoline, is an α-adrenergic agonist that causes vasoconstriction. Tetrahydrozoline is widely used for the research of nasal congestion and conjunctival congestion.
|
-
- HY-N2073
-
-
- HY-10268
-
-
- HY-N0320
-
-
- HY-B0331AS
-
-
- HY-N0852
-
-
- HY-18200
-
|
Atopaxar
E5555; ER-172594-00
|
Protease-Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
Atopaxar (E5555) is a potent, orally active, selective and reversible thrombin receptor protease-activated receptor-1 (PAR-1) antagonist. Atopaxar interferes with platelet signaling. Atopaxar can be used for the research of atherothrombotic disease.
|
-
- HY-U00212
-
-
- HY-B0735A
-
-
- HY-N0485
-
|
Liensinine Diperchlorate
|
Autophagy
Mitophagy
|
Cardiovascular Disease
|
|
Liensinine Diperchlorate is a major isoquinoline alkaloid, extracted from the seed embryo of Nelumbo nucifera Gaertn. Liensinine Diperchlorate inhibits late-stage autophagy/mitophagy through blocking autophagosome-lysosome fusion. Liensinine Diperchlorate has a wide range of biological activities, including anti-arrhythmias, anti-hypertension, anti-pulmonary fibrosis, relaxation on vascular smooth muscle, etc.
|
-
- HY-100312
-
-
- HY-B0612D
-
-
- HY-B0428B
-
-
- HY-108003
-
-
- HY-W016823S
-
-
- HY-B0209
-
-
- HY-P1271A
-
|
Catestatin TFA
|
nAChR
|
Cardiovascular Disease
|
|
Catestatin TFA is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin TFA is an endogenous peptide that regulates cardiac function and blood pressure. Catestatin TFA is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release.
|
-
- HY-128338
-
|
CETP-IN-3
|
CETP
|
Cardiovascular Disease
|
|
CETP-IN-3 (Compound 13) is an small molecule inhibitor of the plasma glycoprotein cholesterol ester transfer protein (CETP), elevating HDL-C through inhibition of CETP. CETP-IN-3 for the CETP inhibitory activity in the scintillation proximity (SPA) and whole plasma assay (WPA) with IC50s of 0.002 μM and 0.06 μM, respectively.
|
-
- HY-113216
-
-
- HY-A0236A
-
|
Aprindine hydrochloride
|
Potassium Channel
|
Cardiovascular Disease
|
|
Aprindine hydrochloride is a class I-b anti-arrhythmic agent and a hERG channel blocker with an IC50 of 0.23 μM. Aprindine hydrochloride has inhibitory effects on Na +/Ca 2+ exchanger currents, which is partly responsible for their antiarrhythmic and cardioprotective effects. Aprindine hydrochloride is widely used for trial and ventricular tachyarrhythmias treatment research.
|
-
- HY-17421A
-
-
- HY-100469
-
|
LXRβ agonist-2
|
LXR
|
Cardiovascular Disease
|
|
LXRβ agonist-2 is a highly potent and β-selective liver X receptor (LXRβ) agonist with EC50 of 7 nM, displays 28.5-fold selectivity over LXRα (EC50=200 nM) and used in the treatment of atherosclerosis.
|
-
- HY-N0684
-
-
- HY-N4142
-
-
- HY-17378
-
-
- HY-107322A
-
|
Barnidipine
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 (Mepirodipine) is an antihypertensive drug and acts by the reduction of peripheral vascular resistance secondary to its vasodilatory action.
|
-
- HY-B1451
-
-
- HY-B0347
-
-
- HY-A0021
-
-
- HY-N7991
-
-
- HY-10163AS
-
-
- HY-78237
-
-
- HY-107322
-
|
Barnidipine hydrochloride
Mepirodipine hydrochloride; YM-09730-5
|
Calcium Channel
|
Cardiovascular Disease
|
|
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 drug and acts by the reduction of peripheral vascular resistance secondary to its vasodilatory action.
|
-
- HY-76006
-
-
- HY-110015
-
|
(-)-Chromanol 293B
|
Others
|
Cardiovascular Disease
|
|
(-)-Chromanol 293B is a potent and selective inhibitor of the slow component of delayed rectifier K + current (IKs). (-)-Chromanol 293B can be used for the research of antiarrhythmic.
|
-
- HY-15407A
-
-
- HY-101740
-
-
- HY-17004
-
-
- HY-B0416
-
-
- HY-B0632
-
|
Diltiazem
|
Calcium Channel
|
Cardiovascular Disease
|
|
Diltiazem is an orally active L-type Ca 2+ channel blocker, with antihypertensive and antiarrhythmic effects. Diltiazem can be used for the research of cardiac arrhythmia, hypertension, and angina pectoris.
|
-
- HY-B0190
-
-
- HY-B0231AS
-
-
- HY-10264
-
|
Edoxaban
DU-176
|
Factor Xa
Thrombin
|
Cardiovascular Disease
|
|
Edoxaban (DU-176) is a selective, potent and orally active factor Xa (FXa) inhibitor with Kis of 0.561 nM and 2.98 nM for free FXa and prothrombinase, respectively. Edoxaban is an anticoagulant agent and can be used for stroke prevention. Edoxaban is a also weak inhibitor of thrombin and factor IXaβ (FIXa), with Kis of 6.00 μM and 41.7 μM, respectively, exhibits >10 000-fold selectivity for FXa. Edoxaban has antithrombotic properties and has potential for thromboembolic diseases treatment.
|
-
- HY-139448
-
-
- HY-12298
-
-
- HY-W010451
-
-
- HY-100882
-
-
- HY-14182
-
|
Vernakalant
RSD1235
|
Potassium Channel
|
Cardiovascular Disease
|
|
Vernakalant(RSD-1235) is an investigational mixed ion channel blocker that can terminate acute atrial fibrillation (AF) in humans at 2 to 5 mg/kg and may be more atrial-selective than available agents; in treatment of antiarrhythmic.
|
-
- HY-109193
-
-
- HY-B0572
-
-
- HY-14183
-
|
Vernakalant Hydrochloride
RSD1235 hydrochloride
|
Potassium Channel
|
Cardiovascular Disease
|
|
Vernakalant hydrochloride is a mixed voltage- and frequency-dependent Na + and atria-preferred K + channel blocker. IC50 for block by Vernakalant of wild-type and mutant Kv1.5 channels Fractional block is 13.35±0.93 μM, 0.61±0.03 μM, and 1.63±0.09 μM for Kv1.5 channel wt, Kv1.5 channel I508F, Kv1.5 channel T479A, respectively.
|
-
- HY-103045
-
|
CMPD101
|
PKC
ROCK
|
Cardiovascular Disease
|
|
CMPD101 is a potent, highly selective and membrane-permeable small-molecule inhibitor of GRK2/3 with IC50 of 18 nM and 5.4 nM, respectively. CMPD101 exhibits less selectively against GRK1, GRK5, ROCK-2 and PKCα with IC50s of 3.1 μM , 2.3 μM, 1.4 μM and 8.1 μM, respectively. CMPD101 can be used for the study of heart failure.
|
-
- HY-17402
-
-
- HY-B1103
-
-
- HY-B1451S
-
-
- HY-105559A
-
-
- HY-100572
-
-
- HY-B0259S
-
|
(rac)-Indapamide-d3
|
Potassium Channel
|
Cardiovascular Disease
|
|
(Rac)-Indapamide-d3 is a labelled racemic Indapamide. Indapamide is an orally active sulphonamide diuretic agent, that can reduce blood pressure by decreasing vascular reactivity and peripheral vascular resistance. Indapamide is also can reduce left ventricular hypertrophy.
|
-
- HY-122898
-
|
Ru360
|
Calcium Channel
Mitochondrial Metabolism
|
Cardiovascular Disease
|
|
Ru360, an oxygen-bridged dinuclear ruthenium amine complex, is a selective mitochondrial calcium uptake inhibitor. Ru360 potently inhibits Ca 2+ uptake into mitochondria with an IC50 of 0.184 nM. Ru360 binds to mitochondria with high affinity (Kd of 0.34 nM). Ru360 has antiarrhythmic and cardioprotective effects.
|
-
- HY-111754
-
|
DMX-5804
|
MAP4K
|
Cardiovascular Disease
|
|
DMX-5804 is a potent, orally active and selective MAP4K4 inhibitor, with an IC50 of 3 nM, a pIC50 of 8.55 for human MAP4K4, less potent on MINK1/MAP4K6 (pIC50, 8.18), and TNIK/MAP4K7 (pIC50, 7.96). DMX-5804 enhances cardiomyocyte survival, and reduces ischemia-reperfusion injury in mice.
|
-
- HY-B1189
-
-
- HY-15515
-
|
SEA0400
|
Na+/Ca2+ Exchanger
|
Cardiovascular Disease
|
|
SEA0400 is a novel and selective inhibitor of the Na +-Ca 2+ exchanger (NCX), inhibiting Na +-dependent Ca 2+ uptake in cultured neurons, astrocytes, and microglia with IC50s of from 5 to 33 nM.
|
-
- HY-100623
-
-
- HY-101682
-
|
SCH 42495
|
Neprilysin
|
Cardiovascular Disease
|
|
SCH 42495 is an orally active neutral metalloendopeptidase (NEP) inhibitor with antihypertensive effect. SCH 42495 is the orally active ethylester prodrug of SCH 42354.
|
-
- HY-P1000
-
-
- HY-15731
-
-
- HY-N3009
-
-
- HY-131105S
-
-
- HY-15664
-
-
- HY-N7971
-
-
- HY-19485
-
|
XL-784
|
MMP
|
Cardiovascular Disease
|
|
XL-784 is a selective matrix metalloproteinases (MMP) inhibitor, with IC50s of ~1900, 0.81, 120, 10.8, 18, 0.56 nM for MMP-1，MMP-2，MMP-3，MMP-8，MMP-9，MMP-13，respectively.
|
-
- HY-13327
-
|
Evacetrapib
LY2484595
|
CETP
|
Cardiovascular Disease
|
|
Evacetrapib is a potent and selective of CETP inhibitor, which inhibits human recombinant CETP protein (IC50 5.5 nM) and CETP activity in human plasma (IC50 36 nM) in vitro.
|
-
- HY-112704
-
|
PDE5-IN-2
|
Phosphodiesterase (PDE)
|
Cardiovascular Disease
|
|
PDE5-IN-2 is a potent, highly selective, and orally active PDE5 inhibitor, with an IC50 of 0.31 nM, less potently inhibits PDE2A, PDE10A, PDE4D2, and PDE6C, with IC50s of 106, 46, 43, 1.2 nM, respectively. Anti-pulmonary arterial hypertension activity.
|
-
- HY-B0612DS
-
-
- HY-107348
-
-
- HY-N3680
-
-
- HY-P1770A
-
|
Adrenomedullin (16-31), human TFA
|
CGRP Receptor
|
Cardiovascular Disease
|
|
Adrenomedullin (16-31), human TFA is amino acid residues 16-31 fragment of human adrenomedullin (hADM). Adrenomedullin has appreciable affinity for the CGRP1 receptor. Adrenomedullin (16-31), human TFA possesses pressor activity in the systemic vascular bed of the rat, but not the cat.
|
-
- HY-122610
-
|
VUT-MK142
|
Others
|
Cardiovascular Disease
|
|
VUT-MK142 is a potent new cardiomyogenic synthetic agent promoting the differentiation of pre-cardiac mesoderm into cardiomyocytes, which may be useful to differentiate stem cells into cardiomyocytes for cardiac repair.
|
-
- HY-B0442A
-
|
Vardenafil hydrochloride
|
Phosphodiesterase (PDE)
|
Cardiovascular Disease
|
|
Vardenafil hydrochloride is a selective, orally active, potent inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil hydrochloride shows selectivity over PDE1 (180 nM), PDE6 (11 nM), PDE2, PDE3, and PDE4 (>1000 nM). Vardenafil hydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil hydrochloride can be used for the research of erectile dysfunction.
|
-
- HY-P1534
-
-
- HY-50722
-
|
NNC 55-0396
NNC 55-0396 dihydrochloride
|
Calcium Channel
|
Cardiovascular Disease
|
|
NNC 55-0396, Mibefradil derivative, is a highly selective T-type calcium channel blocker; displays IC50 values of 6.8 and > 100 μM for inhibition of Cav3.1 T-type channels and HVA currents respectively in INS-1 cells.
|
-
- HY-10564
-
|
Sarpogrelate hydrochloride
MCI-9042
|
5-HT Receptor
|
Cardiovascular Disease
|
|
Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis.
|
-
- HY-W042301
-
-
- HY-N1505
-
-
- HY-128593
-
-
- HY-78841
-
-
- HY-B0331A
-
-
- HY-120855
-
|
CCG-100602
|
Ras
|
Cardiovascular Disease
|
|
CCG-100602 is a specific inhibitor of myocardin-related transcription factor A/serum response factor (MRTF-A/SRF) signaling. CCG-100602 specifically block MRTF-A nuclear localization and thus inhibit the fibrogenic transcription factor SRF.
|
-
- HY-107418
-
-
- HY-A0018
-
-
- HY-U00137
-
-
- HY-101277
-
|
Vadadustat
PG-1016548; AKB-6548
|
HIF/HIF Prolyl-Hydroxylase
|
Cardiovascular Disease
|
|
Vadadustat (PG-1016548) is a titratable, oral hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor. Vadadustat is an erythropoiesis-stimulating agent and has the potential for anemia treatment in chronic kidney disease in vivo.
|
-
- HY-109897
-
|
CV-6209
|
Others
|
Cardiovascular Disease
|
|
CV-6209 is a potent antagonist of platelet activating factor (PAF). CV-6209 inhibits the PAF-induced aggregation of rabbit and human platelets, with IC50s of 75 nM and 170 nM, respectively. CV-6209 can inhibit PAF-induced hypotension in rats.
|
-
- HY-A0116S
-
-
- HY-66010
-
|
Cinepazide Maleate
MD-67350
|
Calcium Channel
|
Cardiovascular Disease
|
|
Cinepazide Maleate (MD-67350) is a piperazine derivative and acts as a weak calcium channel blocker. Cinepazide Maleate is a potent vasodilator and can be used for the research of cerebrovascular diseases, including ischemic stroke, brain infarct et. al.
|
-
- HY-18965
-
-
- HY-N0062
-
-
- HY-112715
-
-
- HY-15492
-
|
AG-13958
AG-013958
|
VEGFR
|
Cardiovascular Disease
|
|
AG-13958 (AG-013958), a potent VEGFR tyrosine kinase inhibitor, is used for treatment of choroidal neovascularization associated with age-related macular degeneration (AMD).
|
-
- HY-117290
-
|
BMS-962212
|
Factor Xa
|
Cardiovascular Disease
|
|
BMS-962212 is a direct, reversible, selective factor XIa (FXIa) inhibitor . BMS-962212 is well tolerated, with fast onset of pharmacodynamic (PD) responses and rapid elimination. BMS-962212 increases exposure dependently in activated partial thromboplastin time, and decreases exposure dependently in FXI clotting activity.
|
-
- HY-10319
-
|
ROCK-IN-2
Azaindole 1; TC-S 7001
|
ROCK
|
Cardiovascular Disease
|
|
ROCK-IN-2 (Azaindole 1; TC-S 7001) is an orally active and ATP-competitive ROCK inhibitor with IC50s of 0.6 and 1.1 nM for human ROCK-1 and ROCK-2, respectively.
|
-
- HY-13965
-
|
Parmodulin 2
ML161
|
Protease-Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
Parmodulin 2 (ML161) is an allosteric inhibitor of protease-activated receptor 1 (PAR1) with an IC50 of 0.26 μM. Parmodulin 2 is a potent and non-competitive inhibitor of SFLLRN-induced P-selectin expression leading to inhibition of platelet aggregation in vitro and platelet thrombus formation in vivo.
|
-
- HY-B0491A
-
-
- HY-P1440
-
-
- HY-12704
-
-
- HY-N2506
-
-
- HY-N6685
-
-
- HY-N9528
-
-
- HY-33351
-
-
- HY-12343
-
-
- HY-18206
-
-
- HY-15718
-
-
- HY-121526
-
-
- HY-105240
-
|
Delparantag
PMX-60056
|
Factor Xa
|
Cardiovascular Disease
|
|
Delparantag (PMX-60056) is a salicylamide derivative and an effective unfractionated heparin (UFH) and low molecular weight heparin (LMWH) reversing agent. Delparantag shows ability to neutralize the anticoagulation and bleeding effects of UFH and LMWH.
|
-
- HY-N0666
-
-
- HY-P0190
-
|
Iberiotoxin
|
Potassium Channel
|
Cardiovascular Disease
|
|
Iberiotoxin is a toxin isolated from Buthus tamulus scorpion venom. Iberiotoxin is a selective high conductance high conductance Ca 2+-activated K + channel inhibitor with a Kd of ~1 nM. Iberiotoxin does not block other types of voltage-dependent ion channels.
|
-
- HY-100713S
-
|
Temocapril-d5
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
Temocapril-d5 is the deuterium labeled Temocapril. Temocapril is an angiotensin-converting enzyme (ACE) inhibitor. Temocapril hydrochloride can be used for the research of hypertension, congestive heart failure, acute myocardial infarction, insulin resistance, and renal diseases.
|
-
- HY-B2172
-
|
Vitamin K
|
Others
|
Cardiovascular Disease
|
|
Vitamin K, the blood-clotting vitamin, is important for the function of numerous proteins within the body, such as the coagulation factors, osteocalcin and matrix-Gla protein.
|
-
- HY-15293A
-
|
JTV-519 free base
K201 free base
|
Calcium Channel
|
Cardiovascular Disease
|
|
JTV-519 free base (K201 free base) is a Ca 2+-dependent blocker of sarcoplasmic reticulum Ca 2+-stimulated ATPase (SERCA) and a partial agonist of ryanodine receptors in striated muscle. Antiarrhythmic and cardioprotective properties.
|
-
- HY-113938
-
-
- HY-111475
-
-
- HY-14853
-
|
Darexaban
YM150
|
Factor Xa
|
Cardiovascular Disease
|
|
Darexaban (YM150) is a potent, selective and orally active factor Xa (FXa) inhibitor with an IC50 of 54.6 nM. Darexaban shows high selectivity against other related serine proteases, such as trypsin, thrombin, and kallikrein. Darexaban has anticoagulant and antithrombotic effects.
|
-
- HY-10119
-
|
Vorapaxar
SCH 530348
|
Protease-Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
Vorapaxar (SCH 530348), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar (SCH 530348) inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner.
|
-
- HY-W011082
-
|
NLRP3-IN-2
|
NOD-like Receptor (NLR)
|
Cardiovascular Disease
|
|
NLRP3-IN-2, an intermediate substrate in the synthesis of glyburide, inhibits the formation of the NLRP3 inflammasome in cardiomyocytes and limits the infarct size following myocardial ischemia/reperfusion in the mouse, without affecting glucose metabolism.
|
-
- HY-108539
-
|
CE3F4
|
Others
|
Cardiovascular Disease
|
|
CE3F4 is a selective antagonist of exchange protein directly activated by cAMP (Epac1), with IC50s of 10.7 μM and 66 μM for Epac1 and Epac2(B), respectively.
|
-
- HY-P1167A
-
-
- HY-135380
-
-
- HY-B1014
-
-
- HY-103410
-
-
- HY-15283
-
|
Clopidogrel
|
P2Y Receptor
|
Cardiovascular Disease
|
|
Clopidogrel is an orally active platelet inhibitor that targets P2Y12 receptor. Clopidogrel is used to inhibit blood clots in coronary artery disease, peripheral vascular disease, and cerebrovascular disease.
|
-
- HY-109562
-
|
CCG258208
GRKs-IN-1
|
Others
|
Cardiovascular Disease
|
|
GRKs-IN-1, Compound 14as, has remarkable potency against and selectivity for G protein-coupled receptor kinase 2 GRK2 (IC50=30 nM) and GRK5 (IC50=7.1 μM).
GRKs-IN-1 is a derivative 14as of paroxetine, shows a 100-fold improvement in cardiomyocyte contractility assays over paroxetine.
|
-
- HY-B1231
-
-
- HY-B0259
-
|
Indapamide
|
Potassium Channel
|
Cardiovascular Disease
|
|
Indapamide is an orally active sulphonamide diuretic agent, that can reduce blood pressure by decreasing vascular reactivity and peripheral vascular resistance. Indapamide is also can reduce left ventricular hypertrophy.
|
-
- HY-119350B
-
-
- HY-17436
-
-
- HY-N9402
-
|
Prosaikogenin A
|
Others
|
Cardiovascular Disease
|
|
Prosaikogenin A is a triterpene saponin isolated from Clinopodium chinense. Prosaikogenin A has significant promoting effects on platelet aggregation with an EC50 value of 12.2 μM.
|
-
- HY-13861
-
-
- HY-124687
-
-
- HY-114348
-
|
N,N'-Diacetyl-L-cystine
DiNAC; (Ac-Cys-OH)2
|
Others
|
Cardiovascular Disease
|
|
N,N'-diacetyl-L-cystine (DiNAC) is the disulphide dimer of N-acetylcysteine with immunomodulating properties. N,N'-diacetyl-L-cystine is a potent, orally active modulator of contact sensitivity/delayed type hypersensitivity reactions in rodents. N,N'-diacetyl-L-cystine also has antiatherosclerotic effects in Watanabe-heritable hyperlipidemic rabbit (WHHL) rabbits.
|
-
- HY-10913
-
-
- HY-B1654A
-
-
- HY-108582
-
|
Y-27152
|
Potassium Channel
|
Cardiovascular Disease
|
|
Y-27152, a prodrug of the KATP (Kir6) channel opener Y-26763, is a long-acting K+ channel opener with less tachycardia: antihypertensive effects in hypertensive rats and dogs in conscious state.
|
-
- HY-A0016
-
|
Dronedarone
SR 33589
|
mAChR
Sodium Channel
Calcium Channel
Adrenergic Receptor
Cytochrome P450
Autophagy
|
Cardiovascular Disease
|
|
Dronedarone (SR 33589), a derivative of amiodarone (HY-14187), is a class III antiarrhythmic agent for the study of atrial fibrillation (AF) and atrial flutter. Dronedarone is a potent blocker of multiple ion currents, including potassium current, sodium current, and L-type calcium current, and exhibits antiadrenergic effects by noncompetitive binding to β-adrenergic receptors. Dronedarone is a substrate for and a moderate inhibitor of CYP3A4.
|
-
- HY-W011955
-
-
- HY-P0226
-
-
- HY-15125
-
-
- HY-B1486
-
-
- HY-112197
-
-
- HY-103310
-
-
- HY-B1182
-
-
- HY-12283
-
|
Rostafuroxin
PST 2238
|
Na+/K+ ATPase
RSV
|
Cardiovascular Disease
|
|
Rostafuroxin (PST 2238), a digitoxigenin derivative, is an orally active and potent Na +,K +-ATPase (ATP1A1) antognist. Rostafuroxin binds specifically to the ATP1A1 extracellular domain and blocks respiratory syncytial virus (RSV)-triggered EGFR Tyr845 phosphorylation. Rostafuroxin has antihypertensive and anti-RSV activity.
|
-
- HY-U00286
-
-
- HY-135356
-
-
- HY-17611
-
|
Etripamil
MSP-2017; (-)-MSP-2017
|
Calcium Channel
|
Cardiovascular Disease
|
|
Etripamil (MSP-2017) is a short-acting L-type calcium-channel antagonist, can be used for the research of Paroxysmal Supraventricular Tachycardia (PSVT). Etripamil (MSP-2017) slows atrioventricular nodal conduction and prolongs atrioventricular nodal refractory periods by inhibiting calcium ion influx through the calcium slow channels in the atrioventricular node cells.
|
-
- HY-B0984
-
-
- HY-101253
-
|
AM-92016 hydrochloride
|
Others
|
Cardiovascular Disease
|
|
AM-92016 hydrochloride is a specific blocker of rectifier potassium current (IK). AM-92016 hydrochloride delays rectifier potassium channel (IK), repolarizes the membrane thereby restricting the duration of the nerve impulse thereby restricting the duration of the nerve impulse.
|
-
- HY-P1435
-
|
NoxA1ds
|
NADPH Oxidase
|
Cardiovascular Disease
|
|
NoxA1ds is a highly efficacious and selective Nox1 (NADPH oxidase isoform 1) inhibitor. NoxA1ds establishes a critical interaction site for Nox1-NOXA1 binding required for enzyme activation. NoxA1ds can be used for the research of hypertension, atherosclerosis and neoplasia.
|
-
- HY-B0190B
-
-
- HY-12090
-
-
- HY-16461
-
-
- HY-130335
-
|
Encainide
MJ9067
|
Others
|
Cardiovascular Disease
|
|
Encainide (MJ9067) is an antiarrhythmic drug with class IC activity. Encainide has the potential for life-threatening ventricular arrhythmias, symptomatic ventricular arrhythmias and supraventricular arrhythmias research.
|
-
- HY-131041
-
|
Ned-K
|
Calcium Channel
|
Cardiovascular Disease
|
|
Ned-K is a nicotinic acid adenine dinucleotide phosphate (NAADP) antagonist. Ned-K is effective at dampening simulated ischaemia and reperfusion (sIR)-induced Ca 2+ oscillations in cardiomyocytes.
|
-
- HY-U00184
-
-
- HY-130354
-
|
Dibutyryl-cGMP sodium
Bt2cGMP sodium
|
Potassium Channel
|
Cardiovascular Disease
|
|
Dibutyryl-cGMP sodium (Bt2cGMP sodium) is a cell-permeable cGMP analogue. Dibutyryl-cGMP sodium preferentially activates cGMP-dependent protein kinase (PKG). Dibutyryl-cGMP sodium inhibits the release of [ 3H]-arachidonic acid from γ thrombin-stimulated human platelets. Dibutyryl-cGMP sodium induces peripheral antinociception via activation of ATP-sensitive K + channels.
|
-
- HY-B0432B
-
|
(S)-Propafenone
(S)-SA-79
|
Others
|
Cardiovascular Disease
|
|
(S)-Propafenone ((S)-SA-79) is the S-enantiomer of Propafenone. (S)-Propafenone ((S)-SA-79) exerts beta-blocking action and the sodium channel-dependent antiarrhythmic class 1 activity.
|
-
- HY-B0251
-
|
Eplerenone
Epoxymexrenone
|
Mineralocorticoid Receptor
|
Cardiovascular Disease
|
|
Eplerenone (Epoxymexrenone) is a selective, competitive and oreally active aldosterone antagonist with an IC50 of 138 nM. Eplerenone has low affinity for progesterone, androgen, estrogen and glucocorticoid receptors. Eplerenone can be used for hypertension and heart failure after myocardial infarction reserch.
|
-
- HY-14286
-
-
- HY-135358
-
-
- HY-B1294
-
|
Amrinone
Inamrinone
|
Phosphodiesterase (PDE)
|
Cardiovascular Disease
|
|
Amrinone (Inamrinone) is a positive inotropic-vasodilator agent. Amrinone is a selective phosphodiesterase III inhibitor that increases cyclic adenosine monophosphate by preventing its breakdown. Amrinone is also an orally active, non-glycosidic and non-catecholamine cardiotonic agent.
|
-
- HY-B0231
-
-
- HY-B1362
-
-
- HY-N4193
-
|
Glabrol
|
Acyltransferase
|
Cardiovascular Disease
|
|
Glabrol (Compound 1), One isoprenyl flavonoid was isolated from ethanol extract of licorice roots, is a potent and non-competitive Acyl-coenzyme A: cholesterol acyltransferase (ACAT) inhibitor with an IC50 value of 24.6 μM for rat liver microsomal ACAT activity.
|
-
- HY-15529
-
|
S0859
|
Na+/HCO3- Cotransporter
|
Cardiovascular Disease
|
|
S0859 is a selective, high-affinity generic Na +/HCO3 - transporter (NBC) inhibitor. S0859 reversibly inhibits NBC-mediated intracellular pH (pHi) recovery (Ki=1.7 μM, full inhibition at approximately 30 μM).
|
-
- HY-108556
-
|
RWJ-56110
|
Protease-Activated Receptor (PAR)
Apoptosis
|
Cardiovascular Disease
|
|
RWJ-56110 is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 uM) and shows no effect on PAR-2, PAR-3, or PAR-4. RWJ-56110 inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM), quite selective relative to U46619 (HY-108566). RWJ-56110 inhibits angiogenesis and blocks the formation of new vessels in vivo. RWJ-56110 induces cell apoptosis.
|
-
- HY-N0824
-
|
Syringin
Eleutheroside B
|
Autophagy
|
Cardiovascular Disease
|
|
Syringin is a main bioactive phenolic glycoside in Acanthopanax senticosus, with anti-osteoporosis activity. Syringin prevents cardiac hypertrophy induced by pressure overload through the attenuation of autophagy.
|
-
- HY-15833
-
-
- HY-15553
-
|
Mibefradil
Ro 40-5967
|
Calcium Channel
|
Cardiovascular Disease
|
|
Mibefradil (Ro 40-5967) is a calcium channel blocker with moderate selectivity for T-type Ca 2+ channels displaying IC50s of 2.7 μM and 18.6 μM for T-type and L-type currents, respectively.
|
-
- HY-121026
-
-
- HY-135884
-
-
- HY-18732A
-
|
L-NMMA acetate
Tilarginine acetate; Methylarginine acetate
|
NO Synthase
|
Cardiovascular Disease
|
|
L-NMMA acetate is a nitric oxide synthase inhibitor of all NOS isoforms including NOS1, NOS2, and NOS3. The Ki values for nNOS (rat), eNOS (human), and iNOS (mouse) are approximately 0.18, 0.4, and 6 µM, respectively.
|
-
- HY-108588
-
|
NS5806
|
Potassium Channel
|
Cardiovascular Disease
|
|
NS5806, a potent potassium current activator, increases KV4.3/KChIP2 peak current amplitudes with an EC50 of 5.3 μM. NS5806 slows KV4.3 and KV4.2 current dacay in channel complexes containing KChIP2.
|
-
- HY-100401A
-
|
Pactimibe sulfate
CS-505
|
Acyltransferase
|
Cardiovascular Disease
|
|
Pactimibe sulfate (CS-505) is a dual ACAT1/2 inhibitor with IC50s of 4.9 μM and 3.0 μM, respectively. Pactimibe sulfate (CS-505) inhibits ACAT with IC50s of 2.0 μM, 2.7 μM, 4.7 μM in the liver, macrophages and THP-1 cells, respectively. Pactimibe sulfate (CS-505) noncompetitively inhibits oleoyl-CoA with a Ki value of 5.6 μM. Moreover, Pactimibe sulfate (CS-505) obviously inhibits cholesteryl ester formation with an IC50 of 6.7 μM. Pactimibe sulfate (CS-505) possesses anti-atherosclerotic potential with lowering plasma cholesterol activity.
|
-
- HY-B0424
-
-
- HY-122098
-
-
- HY-P1136A
-
|
Gap19 TFA
|
Gap Junction Protein
|
Cardiovascular Disease
|
|
Gap19 TFA, a peptide derived from nine amino acids of the Cx43 cytoplasmic loop (CL), is a potent and selective connexin 43 (Cx43) hemichannel blocker. Gap19 TFA inhibits hemichannels caused by preventing intramolecular interactions of the C-terminus (CT) with the CL. Gap19 TFA is not blocking GJ channels or Cx40/pannexin-1 hemichannels. Gap19 TFA has protective effects against myocardial.
|
-
- HY-108579
-
|
UCL 1684 dibromide
|
Potassium Channel
|
Cardiovascular Disease
|
|
UCL 1684 (dibromide) is a first nanomolar, non-peptidic small conductance calcium-activated potassium (SK) channel blocker. UCL 1684 (dibromide) is effective in preventing the development of atrial fibrillation due to potent atrial-selective inhibition of INa. UCL 1684 (dibromide) causes atrial-selective prolongation of ERP secondary to induction of postrepolarization refractoriness.
|
-
- HY-135384
-
-
- HY-14252
-
-
- HY-P1519
-
-
- HY-111925
-
|
BI-749327
|
TRP Channel
|
Cardiovascular Disease
|
|
BI-749327 is a potent, high selectivity and orally bioavailable TRPC6 antagonist, with IC50s of 13 nM, 19 nM and 15 nM for mouse, human and guinea pig TRPC6, respectively. BI-749327 is 85-fold more selective for mouse TRPC6 than TRPC3 and 42-fold versus TRPC7.
|
-
- HY-14806S
-
-
- HY-U00301
-
-
- HY-110084
-
|
BTZO-1
|
Apoptosis
|
Cardiovascular Disease
|
|
BTZO-1 binds to Macrophage migration inhibitory factor (MIF) with a Kd value of 68.6 nM, and its binding requires the N-terminal Pro1. BTZO-1 can activate antioxidant response element (ARE)-mediated gene expression and suppress oxidative stress-induced cardiomyocyte apoptosis in vitro.
|
-
- HY-P1136
-
|
Gap19
|
Gap Junction Protein
|
Cardiovascular Disease
|
|
Gap19, a peptide derived from nine amino acids of the Cx43 cytoplasmic loop (CL), is a potent and selective connexin 43 (Cx43) hemichannel blocker. Gap19 inhibits hemichannels caused by preventing intramolecular interactions of the C-terminus (CT) with the CL. Gap19 is not blocking GJ channels or Cx40/pannexin-1 hemichannels. Gap19 has protective effects against myocardial.
|
-
- HY-B0753S
-
-
- HY-105559
-
-
- HY-P1166
-
|
UFP-803
|
Urotensin Receptor
|
Cardiovascular Disease
|
|
UFP-803 is a potent urotensin-II receptor (UT) ligand. UFP-803 has lower residual agonist activity, so it may be an important tool for the investigations on the role played by the UT system in physiology and pathology.
|
-
- HY-100826
-
-
- HY-100957
-
|
Dilazep dihydrochloride
|
Others
|
Cardiovascular Disease
|
|
Dilazep dihydrochloride is an inhibitor of adenosine uptake. Dilazep dihydrochloride has cerebral and coronary vasodilating action through enhancement of effect of adenosine. Dilazep dihydrochloride also inhibits the ischemic damage, platelet aggregation, and membrane transport of nucleosides.
|
-
- HY-18940A
-
-
- HY-100652A
-
-
- HY-N2337
-
-
- HY-50769
-
-
- HY-B1815
-
|
Xanthinol Nicotinate
Xanthinol Niacinate
|
Others
|
Cardiovascular Disease
|
|
Xanthinol Nicotinate (Xanthinol Niacinate), a vasodilator, can act directly on the smooth muscle of small arteries and capillaries. Xanthinol Nicotinate expands blood vessels, improves blood rheology and reduces peripheral vascular resistance.
|
-
- HY-N7065
-
-
- HY-113151
-
-
- HY-B0464
-
-
- HY-B0477
-
-
- HY-P1167
-
-
- HY-10274
-
|
Dabigatran etexilate
BIBR 1048
|
Others
|
Cardiovascular Disease
|
|
Dabigatran etexilate (BIBR 1048) is an orally active prodrug of Dabigatran. Dabigatran etexilate has anticoagulant effects and is used for the prophylaxis of venousthromboembolism and stroke due to atrial fibrillation.
|
-
- HY-N0496
-
|
Ruscogenin
|
NOD-like Receptor (NLR)
|
Cardiovascular Disease
|
|
Ruscogenin, an important steroid sapogenin derived from Ophiopogon japonicus, attenuates cerebral ischemia-induced blood-brain barrier dysfunction by suppressing TXNIP/NLRP3 inflammasome activation and the MAPK pathway and exerts significant anti-inflammatory and anti-thrombotic activities.
|
-
- HY-106225
-
|
Rotigaptide
ZP123
|
Gap Junction Protein
|
Cardiovascular Disease
|
|
Rotigaptide (ZP123) is a novel and specific modulator of connexin 43 (Cx43). Rotigaptide prevents the uncoupling of Cx43-mediated gap junction communication and normalizes cell-to-cell communication during acute metabolic stress. Rotigaptide is a potent antiarrhythmic peptide (AAP) with improved stability and has the potential for the investigation of cardiac arrhythmias-specifically atrial fibrillation.
|
-
- HY-129056
-
|
Melagatran
|
Thrombin
|
Cardiovascular Disease
|
|
Melagatran is a direct and orally active inhibitor of thrombin, without interacting with any other enzymes in the coagulation cascade or fibrinolytic enzymes aside from thrombin. Melagatran does not require endogenous co-factors for its antithrombin effect and may help to alleviate some of the damaging effects of endotoxemia. Melagatran has the potential to provide a rational approach in the prevention of arterial occlusion.
|
-
- HY-101436A
-
|
Sematilide hydrochloride
CK-1752 hydrochloride
|
Potassium Channel
|
Cardiovascular Disease
|
|
Sematilide hydrochloride (CK-1752 hydrochloride) is a selective IKr channel blocker. Sematilide causes a concentration-dependent inhibition of the delayed rectifier K + current (IC50=25 μM). Sematilide is a class III antiarrhythmic agent.
|
-
- HY-B1800
-
-
- HY-B0232S
-
-
- HY-B0917
-
-
- HY-100258
-
-
- HY-100151
-
-
- HY-A0064
-
|
Verapamil hydrochloride
(±)-Verapamil hydrochloride; CP-16533-1 hydrochloride
|
Calcium Channel
P-glycoprotein
Cytochrome P450
|
Cardiovascular Disease
|
|
Verapamil hydrochloride ((±)-Verapamil hydrochloride) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil hydrochloride also inhibits CYP3A4. Verapamil hydrochloride has the potential for high blood pressure, heart arrhythmias and angina research.
|
-
- HY-75839
-
-
- HY-139400A
-
|
FTX-6058 hydrochloride
|
Histone Methyltransferase
|
Cardiovascular Disease
|
|
FTX-6058 hydrochloride is a potent and orally active inhibitor of Embryonic Ectoderm Development (EED). FTX-6058 hydrochloride can induce HbF protein expression in cell and murine models. FTX-6058 hydrochloride can be used for the research of select hemoglobinopathies, including sickle cell disease and β-thalassemia.
|
-
- HY-B2087S1
-
-
- HY-108649A
-
-
- HY-100744
-
-
- HY-10913A
-
-
- HY-13815
-
|
KY02111
|
Wnt
|
Cardiovascular Disease
|
|
KY02111 is a canonical WNT signaling (β-catenin) inhibitor which promotes differentiation of hPSCs to cardiomyocytes. KY02111 can be used for the research of human cardiomyocyte regeneration.
|
-
- HY-B0428A
-
-
- HY-19976
-
|
RN-1747
|
TRP Channel
|
Cardiovascular Disease
|
|
RN-1747 is a selective transient receptor potential cation channel subfamily V member 4 (TRPV4) agonist, with EC50 values are 0.77 μM, 4.0 μM and 4.1 μM for hTRPV4, mTRPV4 and rTRPV4 respectively. RN-1747 also antagonizes TRPM8, with an IC50 of 4 μM.
|
-
- HY-113618A
-
|
RO2959 hydrochloride
|
CRAC Channel
Interleukin Related
|
Cardiovascular Disease
|
|
RO2959 hydrochloride is a potent and selective CRAC channel inhibitor with an IC50 of 402 nM. RO2959 hydrochloride is a potent blocker of store operated calcium entry (SOCE) mediated by Orai1/Stim1 channels with an IC50 of 25 nM. RO2959 hydrochloride is also a potent inhibitor of human IL-2 production, and potently blocks T cell receptor triggered gene expression and T cell functional pathways.
|
-
- HY-19664
-
-
- HY-N8218
-
-
- HY-B1069
-
|
Molsidomine
SIN-10; Morsydomine
|
Others
|
Cardiovascular Disease
|
|
Molsidomine is an orally active, long acting vasodilating drug, metabolized in the liver to the active metabolite linsidomine, which is an unstable compound that releases nitric oxide (NO) upon decay as the actual vasodilating compound.
|
-
- HY-15603
-
-
- HY-17567
-
-
- HY-78846
-
|
2R,4R-Sacubitril
|
Others
|
Cardiovascular Disease
|
|
2R,4R-Sacubitril is the impurity of Sacubitril. Sacubitril is approved by the Food and Drug Administration for use in combination with valsartan for the treatment of patients with heart failure.
|
-
- HY-12378A
-
|
BQ-123 TFA
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
BQ-123 TFA is a potent and selective endothelin A (ETA) receptor antagonist with an IC50 of 7.3 nM and a Ki of 25 nM. BQ-123 TFA inhibits endothelin-1-mediated proliferation of human pulmonary artery smooth muscle cells and lowers blood pressure in different rat models of hypertension.
|
-
- HY-139485
-
|
BMS-986224
|
HIV
|
Cardiovascular Disease
|
|
BMS-986224 is a potent, selective and orally bioavailable APJ receptor agonist (Kd = 0.3 nM). BMS-986224 exhibits similar receptor binding and signaling profile to (Pyr 1) apelin-13. BMS-986224 has the potential for the research of heart failure.
|
-
- HY-100615A
-
-
- HY-109037
-
|
Mavacamten
MYK461; SAR439152
|
Myosin
|
Cardiovascular Disease
|
|
Mavacamten (MYK461) is an orally active modulator of cardiac myosin, with IC50s of 490, 711 nM for bovine cardiac and human cardiac, respectively.
|
-
- HY-U00182
-
-
- HY-18252
-
-
- HY-135281
-
-
- HY-B0419S
-
-
- HY-114424
-
-
- HY-121385
-
-
- HY-19749
-
-
- HY-18723
-
-
- HY-12765
-
|
Losartan Carboxylic Acid
E-3174; EXP-3174
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
Losartan Carboxylic Acid (E-3174), an active carboxylic acid metabolite of Losartan, is an angiotensin II receptor type 1 (AT1) antagonist. The Ki values are 0.97, 0.57, 0.67 nM for rat AT1B/AT1A and human AT1, respectively. Losartan Carboxylic Acid blocks the angiotensin II-induced responses in vascular smoothmuscle cells (VSMC). Losartan Carboxylic Acid elevates plasma renin activities and reduces mean arterial pressure.
|
-
- HY-103265B
-
|
ARL67156 trisodium salt hydrate
|
Phosphatase
|
Cardiovascular Disease
|
|
ARL67156 trisodium salt hydrate is an inhibitor of ecto-ATPase. ARL67156 trisodium salt hydrate is a weak competitive inhibitor of NTPDase1 (CD39), NTPDase3 and NPP1, with Kis of 11, 18 and 12 μM, respectively. ARL67156 trisodium salt hydrate prevents in vivo the development of calcific aortic valve disease.
|
-
- HY-P1082A
-
-
- HY-B0735AS
-
-
- HY-125856
-
|
Milvexian
BMS-986177; JNJ-70033093
|
Factor Xa
|
Cardiovascular Disease
|
|
Milvexian (BMS-986177), an effective antithrombotic agent, is an orally-bioavailable, reversible and direct inhibitor of human and rabbit factor XIa (FXIa) with Ki of 0.11, and 0.38 nM, respectively.
|
-
- HY-B0325
-
-
- HY-B0686A
-
-
- HY-P2222
-
-
- HY-108556A
-
|
RWJ-56110 dihydrochloride
|
Protease-Activated Receptor (PAR)
Apoptosis
|
Cardiovascular Disease
|
|
RWJ-56110 dihydrochloride is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 uM) and shows no effect on PAR-2, PAR-3, or PAR-4. RWJ-56110 dihydrochloride inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM), quite selective relative to U46619 (HY-108566). RWJ-56110 dihydrochloride blocks angiogenesis and blocks the formation of new vessels in vivo. RWJ-56110 dihydrochloride induces cell apoptosis.
|
-
- HY-14462
-
-
- HY-P9951
-
|
Ranibizumab
RG-6321
|
VEGFR
|
Cardiovascular Disease
|
|
Ranibizumab (RG-6321) is a humanized anti-VEGF monoclonal antibody fragment and can recognize all VEGF-A isoforms (VEGF110, VEGF121, and VEGF165). Ranibizumab slows vision loss in vivo and is used for wet age-related macular degeneration (AMD) research.
|
-
- HY-U00236
-
-
- HY-14254A
-
|
Olprinone
Loprinone
|
Phosphodiesterase (PDE)
|
Cardiovascular Disease
|
|
Olprinone (Loprinone) is a potent phosphodiesterase (PDE) 3 inhibitor, with IC50s of 150, 100, 0.35 and 14 μM for PDE1, PDE2, PDE3 and PDE4, respectively. Olprinone is used for the research of heart failure due to its positive inotropic and vasodilative effects. Anti-inflammatory activity.
|
-
- HY-P2090
-
|
Angiopeptin
|
Somatostatin Receptor
Adenylate Cyclase
|
Cardiovascular Disease
|
|
Angiopeptin, a cyclic octapeptide analogue of somatostatin, is a weak sst2/sst5 receptor partial agonist with IC50 values of 0.26 nM and 6.92 nM, respectively. Angiopeptin is a potent inhibitor of growth hormone release and insulin-like growth factor-1 (IGF-1) production. Angiopeptin inhibits adenylate cyclase or stimulate extracellular acidification. Angiopeptin has the potential for coronary atherosclerosis research.
|
-
- HY-P1166A
-
|
UFP-803 TFA
|
Urotensin Receptor
|
Cardiovascular Disease
|
|
UFP-803 TFA is a potent urotensin-II receptor (UT) ligand. UFP-803 TFA has lower residual agonist activity, so it may be an important tool for the investigations on the role played by the UT system in physiology and pathology.
|
-
- HY-112911
-
-
- HY-10655
-
|
Palosuran
ACT-058362
|
Urotensin Receptor
|
Cardiovascular Disease
|
|
Palosuran (ACT-058362) is a potent, selective, and orally active antagonist of urotensin II receptor, with an IC50 of 3.6 nM for CHO cell membranes expressing human recombinant receptors. Palosuran can improves pancreatic and renal function in diabetic rats.
|
-
- HY-139397
-
|
TJ-M2010-5
|
MyD88
|
Cardiovascular Disease
|
|
TJ-M2010-5 is a MyD88 inhibitor that binds to the TIR domain of MyD88 to interfere with its homodimerization, and the TLR/MyD88 signal pathway. TJ-M2010-5 can be used for the research of myocardial ischemia/reperfusion injury (MIRI).
|
-
- HY-12631
-
-
- HY-14187
-
-
- HY-18600
-
-
- HY-101436
-
|
Sematilide
CK-1752
|
Potassium Channel
|
Cardiovascular Disease
|
|
Sematilide (CK-1752) is a selective IKr channel blocker. Sematilide causes a concentration-dependent inhibition of the delayed rectifier K + current (IC50=25 μM). Sematilide is a class III antiarrhythmic agent.
|
-
- HY-P1929
-
|
Bivalirudin
|
Thrombin
|
Cardiovascular Disease
|
|
Bivalirudin, a peptide anticoagulant, is a direct thrombin inhibitor for anticoagulation in the setting of invasive cardiology, particularly percutaneous coronary intervention.
|
-
- HY-B1180
-
-
- HY-B1264
-
|
Celiprolol hydrochloride
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Celiprolol hydrochloride is a potent, selective and orally active antagonist of β1-andrenoceptor with partial β2 agonist activity, therefore it is a selective adrenoreceptor modulator (SAM). Celiprolol hydrochloride demonstrates antihypertensive and antianginal activity.
|
-
- HY-U00151
-
-
- HY-N0455
-
|
L-Arginine
(S)-(+)-Arginine
|
NO Synthase
Endogenous Metabolite
|
Cardiovascular Disease
|
|
L-Arginine ((S)-(+)-Arginine) is the substrate for the endothelial nitric oxide synthase (eNOS) to generate NO. L-Arginine is transported into vascular smooth muscle cells by the cationic amino acid transporter family of proteins where it is metabolized to nitric oxide (NO), polyamines, or L-proline.
|
-
- HY-N2168
-
|
Pinoresinol 4-O-β-D-glucopyranoside
(+)-Pinoresinol 4-O-β-D-glucopyranoside
|
Others
|
Cardiovascular Disease
|
|
Pinoresinol 4-O-β-D-glucopyranoside ((+)-Pinoresinol 4-O-β-D-glucopyranoside) is the major active furofuran type lignans in Fructus Forsythiae. Pinoresinol 4-O-β-D-glucopyranoside shows antioxidant, blood pressure reducing, and cyclic adenosine monophosphate (cAMP) phosphodiesterase inhibitory effects.
|
-
- HY-101729
-
-
- HY-14550
-
-
- HY-100401
-
|
Pactimibe
CS-505 free base
|
Acyltransferase
|
Cardiovascular Disease
|
|
Pactimibe (CS-505 free base) is a dual ACAT1/2 inhibitor with IC50s of 4.9 μM and 3.0 μM, respectively. Pactimibe (CS-505 free base) inhibits ACAT with IC50s of 2.0 μM, 2.7 μM, 4.7 μM in the liver, macrophages and THP-1 cells, respectively. Pactimibe (CS-505 free base) noncompetitively inhibits oleoyl-CoA with a Ki value of 5.6 μM. Moreover, Pactimibe (CS-505 free base) obviously inhibits cholesteryl ester formation with an IC50 of 6.7 μM. Pactimibe (CS-505 free base) possesses anti-atherosclerotic potential with lowering plasma cholesterol activity.
|
-
- HY-B0312
-
-
- HY-W005255
-
-
- HY-107635
-
|
TMN355
|
Others
|
Cardiovascular Disease
|
|
TMN355 is a potent chemical cyclophilin A inhibitor and reduces foam cell formation and cytokine secretion. TMN355 is used for atherosclerosis.
|
-
- HY-U00173
-
-
- HY-100253
-
-
- HY-101419
-
-
- HY-133036
-
|
APJ receptor agonist 1
|
Others
|
Cardiovascular Disease
|
|
APJ receptor agonist 1, a biphenyl acid derivative, is a potent APJ receptor (APJ-R) agonist (EC50s 0.093 and 0.12 nM for human and rat APJ-R, respectively). APJ receptor agonist 1 displays in vitro potency to apelin-13, the endogenous peptidic ligand for the APJ receptor. APJ receptor agonist 1 has the potential for the research of heart failure.
|
-
- HY-13063
-
-
- HY-17468S
-
|
Bumetanide D5
|
NKCC
|
Cardiovascular Disease
|
|
Bumetanide D5 is a deuterium labeled Bumetanide. Bumetanide is a selective Na +-K +-Cl - (NKCC1) inhibitor, weakly inhibits NKCC2, with IC50s of 0.68 and 4.0 μM for hNKCC1A and hNKCC2A, respectively.
|
-
- HY-113121
-
|
Vanillylmandelic acid
|
Others
|
Cardiovascular Disease
|
|
Vanillylmandelic acid is the endproduct of epinephrine and norepinephrine metabolism. Vanillylmandelic acid can be used as an indication of the disorder in neurotransmitter metabolism as well. Vanillylmandelic acid has antioxidant activity towards DPPH radical with an IC50 value of 33 μM.
|
-
- HY-108136A
-
|
Bisindolylmaleimide X hydrochloride
BIM-X hydrochloride; Ro31-8425 hydrochloride
|
PKC
CDK
|
Cardiovascular Disease
|
|
Bisindolylmaleimide X hydrochloride (BIM-X hydrochloride) is a potent and selective protein kinase C (PKC) inhibitor. Bisindolylmaleimide X hydrochloride is a potent cyclin-dependent kinase 2 (CDK2) antagonist with an IC50 of 200 nM.
|
-
- HY-101554
-
-
- HY-90009A
-
-
- HY-U00147
-
-
- HY-N8223
-
-
- HY-106369
-
-
- HY-A0182
-
-
- HY-B0149
-
-
- HY-N2507
-
-
- HY-N5098
-
-
- HY-N5016
-
-
- HY-136933
-
|
Gitoxin
|
Na+/K+ ATPase
|
Cardiovascular Disease
|
|
Gitoxin, a Na +/K +-ATPase inhibitor, usually appears as a result of metabolic degradation of Digitoxin, is just the hydroxyl (ZOH) group close to the C-17β position, which changes the pharmacokinetics and pharmacodynamics of these substances considerably.
|
-
- HY-136909
-
|
SR33805
|
Calcium Channel
|
Cardiovascular Disease
|
|
SR33805 is a potent Ca 2+ channel antagonist, with EC50s of 4.1 nM and 33 nM in depolarized and polarized conditions, respectively. SR33805 blocks L-type but not T-type Ca 2+ channels. SR33805 can be used for the research of acute or chronic failing hearts.
|
-
- HY-17402S2
-
-
- HY-18277
-
-
- HY-N7354
-
-
- HY-B0023S
-
-
- HY-15574A
-
-
- HY-106855
-
-
- HY-W016823
-
-
- HY-107929
-
|
Calcium polystyrene sulfonate
Poly(styrenesulfonic acid) calcium salt
|
Others
|
Cardiovascular Disease
|
|
Calcium polystyrene sulfonate is an ion-exchange resin used for reducing blood levels of potassium. Calcium polystyrene sulfonate is used to treat hyperkalemia in patients with chronic kidney disease (CKD).
|
-
- HY-N0265
-
|
Asperosaponin VI
|
Caspase
Apoptosis
|
Cardiovascular Disease
|
|
Asperosaponin VI, A saponin component from Dipsacus asper wall, induces osteoblast differentiation through BMP‐2/p38 and ERK1/2 pathway. Asperosaponin Ⅵ inhibits apoptosis in hypoxia-induced cardiomyocyte by increasing the Bcl-2/Bax ratio and decreasing active caspase-3 expression, as well as enhancing of p-Akt and p-CREB.
|
-
- HY-14854
-
|
Tecarfarin
ATI-5923
|
Others
|
Cardiovascular Disease
|
|
Tecarfarin (ATI-5923) is an orally active and non-competitive vitamin K epoxide reductase (VKOR) antagonist, and impairs the activation of the vitamin K-dependent clotting factors II, VII, IX and X. Tecarfarin has the antithrombotic activity .
|
-
- HY-A0093S
-
|
Mexiletine D6 hydrochloride
KOE-1173 D6 hydrochloride
|
Sodium Channel
|
Cardiovascular Disease
|
|
Mexiletine D6 hydrochloride (KOE-1173 D6 hydrochloride) is a deuterium labeled Mexiletine hydrochloride (KOE-1173 hydrochloride). Mexiletine hydrochloride, a Class IB antianhythmic, is a non-selective voltage-gated sodium channel blocker.
|
-
- HY-P1082
-
-
- HY-P2141
-
|
TRV-120027
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
TRV120027, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ß-arrestins while blocking G-protein signaling. TRV120027 induces acute catecholamine secretion through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R–β-arrestin-1–TRPC3–PLCγ at the plasma membrane. TRV120027 inhibits angiotensin II–mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 has the potential for the acute decompensated heart failure (ADHF) treatment.
|
-
- HY-U00119
-
-
- HY-112486
-
|
TA-316
Megakaryocytes/platelets inducing agent
|
Others
|
Cardiovascular Disease
|
|
TA-3166 (Megakaryocytes/platelets inducing agent) is a novel chemically synthesized c-MPL agonist (CMA) and thrombopoietin (TPO) receptor agonist. TA-316 enhances ex vivo platelet generation from human-induced pluripotent stem (iPS) cells.
|
-
- HY-13463B
-
|
Avatrombopag hydrochloride
AKR-501 hydrochloride; E5501 hydrochloride; YM477 hydrochloride
|
Thrombopoietin Receptor
|
Cardiovascular Disease
|
|
Avatrombopag (AKR-501) hydrochloride is an orally active, nonpeptide thrombopoietin (TPO) receptor agonist (EC50=3.3 nM). Avatrombopag hydrochloride mimics the biological activities of TPO. Avatrombopag hydrochloride increases platelet production by activating the intracellular signaling system, and promotes production of platelets and megakaryocytes from hemopoietic precursor cells. Avatrombopag hydrochloride is a substrate of cytochrome P450 (CYP) 2C9 and CYP3A.
|
-
- HY-B0597
-
-
- HY-N1483
-
|
Guanfu base A
|
Potassium Channel
|
Cardiovascular Disease
|
|
Guanfu base A is an antiarrhythmic alkaloid isolated from Aconitum coreanum and is a potent noncompetitive CYP2D6 inhibitor, with a Ki of 1.20 μM in human liver microsomes (HLMs) and a Ki of 0.37 μM for the human recombinant form (rCYP2D6). Guanfu base A is also a potent competitive inhibitor of CYP2D in monkey (Ki of 0.38 μM) and dog (Ki of 2.4 μM) microsomes. Guanfu base A also inhibits HERG channel current.
|
-
- HY-118941
-
|
BAY 73-1449
|
Prostaglandin Receptor
|
Cardiovascular Disease
|
|
BAY 73-1449 is a selective antagonist of prostacyclin receptor (IP), with high potency (IC50 of less than 0.1 nM) in cAMP assays in Human HEL cells and rat DRG. BAY 73-1449 can be used in the research of lowering blood pressure.
|
-
- HY-10678
-
|
BMS-687453
|
PPAR
|
Cardiovascular Disease
|
|
BMS-687453 is a potent and selective PPARα agonist, with an EC50 and IC50 of 10 nM and 260 nM for human PPARα and 4100 nM and >15000 nM for PPARγ in PPAR-GAL4 transactivation assays.
|
-
- HY-108518
-
-
- HY-100322
-
|
H100
|
Chloride Channel
|
Cardiovascular Disease
|
|
H100 is a Cl - transport inhibitor, with partial effects against both the NaK2Cl cotransporter and the Band 3 anion exchanger, but no effect against KCl cotransporter, in human erythrocytes.
|
-
- HY-B1209
-
|
Etofylline
7-(β-Hydroxyethyl)theophylline
|
Others
|
Cardiovascular Disease
|
|
Etofylline (7-(β-Hydroxyethyl)theophylline) is a N-7-substituted derivative of Theophylline. Etofylline is a bronchodilator which can be used for the research of asthma. Etofylline is also an anticholesteremic and reduces total cholesterol level in the blood.
|
-
- HY-13221
-
-
- HY-19026
-
|
Siguazodan
SKF 94836
|
Phosphodiesterase (PDE)
|
Cardiovascular Disease
|
|
Siguazodan (SKF 94836) is a potent, selective and orally active phosphodiesterase III (PDE-III) inhibitor with an IC50 of 117 nM. Siguazodan increases cAMP accumulation in intact platelets with an EC50 of 18.88 μM. Siguazodan also inhibits phenylephrine-induced 5-HT release with an IC50 value of 4.2 μM.
|
-
- HY-U00336
-
-
- HY-P2141A
-
|
TRV-120027 TFA
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
TRV120027 TFA, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ß-arrestins while blocking G-protein signaling. TRV120027 TFA induces acute catecholamine secretion through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R–β-arrestin-1–TRPC3–PLCγ at the plasma membrane. TRV120027 TFA inhibits angiotensin II–mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 TFA has the potential for the acute decompensated heart failure (ADHF) treatment.
|
-
- HY-19414A
-
-
- HY-U00026
-
-
- HY-101644A
-
-
- HY-101605
-
-
- HY-101674
-
-
- HY-101809
-
-
- HY-U00074
-
-
- HY-15759A
-
-
- HY-101727
-
-
- HY-101682A
-
|
SCH 42495 racemate
|
Neprilysin
|
Cardiovascular Disease
|
|
SCH 42495 racemate is the racemate of SCH 42495. SCH 42495 is an orally active neutral metalloendopeptidase (NEP) inhibitor with antihypertensive effect. SCH 42495 is the orally active ethylester prodrug of SCH 42354.
|
-
- HY-U00013
-
|
Nitroflurbiprofen
HCT 1206; NO-flurbiprofen; Nitroxybutyl flurbiprofen
|
COX
|
Cardiovascular Disease
|
|
Nitroflurbiprofen is a cyclooxygenase (COX) inhibitor with nitric oxide (NO)-donating properties, modulates the increased intrahepatic vascular tone in portal hypertensive cirrhotic rats.
|
-
- HY-101804
-
-
- HY-101617
-
-
- HY-U00075
-
-
- HY-101701
-
-
- HY-19663
-
-
- HY-101723
-
-
- HY-101685
-
-
- HY-101594
-
-
- HY-U00041
-
-
- HY-101807
-
-
- HY-101675
-
-
- HY-101720
-
|
Fradafiban
BIBU-52
|
Integrin
|
Cardiovascular Disease
|
|
Fradafiban is a nonpeptide platelet glycoprotein IIb/IIIa antagonist, which binds to the human platelet GP IIb/IIIa complex with a Kd value of 148 nM.
|
-
- HY-19097
-
-
- HY-19373
-
-
- HY-101668
-
-
- HY-101661
-
-
- HY-101693
-
-
- HY-101811
-
-
- HY-101681
-
-
- HY-19660
-
|
Inogatran
H-314-27
|
Thrombin
|
Cardiovascular Disease
|
|
Inogatran (H-314-27) is a synthetic thrombin inhibitor, developed for the possible treatment and prophylaxis of arterial and venous thrombotic diseases.
|
-
- HY-U00025
-
-
- HY-101700
-
-
- HY-19163
-
-
- HY-101707
-
-
- HY-19102
-
-
- HY-19062
-
-
- HY-101618
-
-
- HY-101577
-
-
- HY-B0432AS2
-
|
Propafenone D5 hydrochloride
|
Sodium Channel
|
Cardiovascular Disease
|
|
Propafenone D5 (SA-79 D5) hydrochloride is the deuterium labeled Propafenone hydrochloride. Propafenone (SA-79) hydrochloride is a class of anti-arrhythmic medication, which treats illnesses associated with rapid heart beats such as atrial and ventricular arrhythmias.
|
-
- HY-135379
-
|
Atorvastatin acetonide
|
Others
|
Cardiovascular Disease
|
|
Atorvastatin acetonide is an impurity of Atorvastatin, and extracted from patent WO2011131605A1, Compound 4. Atorvastatin is an orally active HMG-CoA reductase inhibitor and has the ability to effectively decrease blood lipids.
|
-
- HY-P0316
-
|
TP508
|
Thrombin
NO Synthase
|
Cardiovascular Disease
|
|
TP508 is a 23-amino acid nonproteolytic thrombin peptide that represents a portion of the receptor-binding domain of thrombin molecule. TP508 activates endothelial NO synthase (eNOS) and stimulates production of NO in human endothelial cells. TP508 activates endothelial cells and stem cells to revascularize and regenerate tissues.
|
-
- HY-103061
-
|
Dehydro-ZINC39395747
|
Others
|
Cardiovascular Disease
|
|
Dehydro-ZINC39395747 is a derivative of ZINC39395747. ZINC39395747 is a potent cytochrome b5 reductase 3 (CYB5R3) inhibitor with an IC50 of 9.14 μM and a Kd of 1.11 μM. ZINC39395747 can increase NO bioavailability in vascular cells.
|
-
- HY-13289A
-
|
Nepicastat hydrochloride
SYN-117 hydrochloride; RS-25560-197 hydrochloride
|
Dopamine β-hydroxylase
|
Cardiovascular Disease
|
|
Nepicastat hydrochloride (SYN-117 hydrochloride) is a selective, potent, and orally active inhibitor of dopamine-beta-hydroxylase. Nepicastat hydrochloride produces concentration-dependent inhibition of bovine (IC50=8.5 nM) and human (IC50=9 nM) dopamine-beta-hydroxylase. Nepicastat hydrochloride can cross the blood-brain barrier (BBB).
|
-
- HY-15551
-
-
- HY-N0856
-
|
Alisol C 23-acetate
23-O-Acetylalisol C; Alisol C monoacetate
|
Others
|
Cardiovascular Disease
|
|
Alisol C 23-acetate, a natural product extracted from Alisma orientale, can significantly and strongly inhibit DTH response after oral administration.
|
-
- HY-100295
-
-
- HY-A0016S
-
|
Dronedarone D6 hydrochloride
|
mAChR
Sodium Channel
Calcium Channel
Adrenergic Receptor
Cytochrome P450
Autophagy
|
Cardiovascular Disease
|
|
Dronedarone D6 hydrochloride is the deuterium labeled Dronedarone. Dronedarone hydrochloride, a derivative of Amiodarone (HY-14187), is a class III antiarrhythmic agent for the study of atrial fibrillation (AF) and atrial flutter. Dronedarone hydrochloride is a potent blocker of multiple ion currents, including potassium current, sodium current, and L-type calcium current, and exhibits antiadrenergic effects by noncompetitive binding to β-adrenergic receptors. Dronedarone hydrochloride is a substrate for and a moderate inhibitor of CYP3A4.
|
-
- HY-103311
-
|
Ruthenium red
Ammoniated ruthenium oxychloride
|
Calcium Channel
|
Cardiovascular Disease
|
|
Ruthenium red (Ammoniated ruthenium oxychloride) is a polycationic dye widely used for electron microscopy (EM) of cells, tissues and vegetative bacteria. Ruthenium red strongly reacts with phospholipids and fatty acids and binds to acidic mucopolysaccharides. Ruthenium red is a L-type calcium current (ICa) blocker.
|
-
- HY-P1829
-
|
Angiotensin I/II (1-6)
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
Angiotensin I/II 1-6 contains the amino acids 1-6 and is converted from Angiotensin I/II peptide. The precursor angiotensinogen is cleaved by renin to form angiotensin I. Angiotensin I ishydrolyzed by angiotensin-converting enzyme (ACE) to form the biologically active angiotensin II. Angiotensin II has been investigated for the treatment, basic science, and diagnostic of Hypertension, Renin Angiotensin System, and Idiopathic Membranous Nephropathy.
|
-
- HY-106150B
-
-
- HY-Z0478
-
|
(-)-Limonene
(S)-(-)-Limonene
|
Others
|
Cardiovascular Disease
|
|
(-)-Limonene ((S)-(-)-Limonene) is a monoterpene found in many pine-needle oils and in turpentine. (-)-Limonene can induce a mild bronchoconstrictive effect.
|
-
- HY-A0043A
-
-
- HY-N3049
-
-
- HY-U00116
-
|
GP531
|
Adenosine Receptor
|
Cardiovascular Disease
|
|
GP531 is a potent, second-generation adenosine regulating agent, is pharmacologically silent under basal conditions but increases localized endogenous adenosine during ischemia.
|
-
- HY-112461A
-
|
NF449 octasodium
|
P2X Receptor
|
Cardiovascular Disease
|
|
NF449 octasodium is a highly potent P2X1 receptor antagonist, with IC50s of 0.28, 0.69, and 120 nM for rP2X1, rP2X1+5, P2X2+3, respectively. NF449 octasodium is a Gsα-selective G Protein antagonist. NF449 octasodium suppresses the rate of GTP[γS] binding to Gsα-s, inhibits the stimulation of adenylyl cyclase activity, and blocks the coupling of β-adrenergic receptors to Gs.
|
-
- HY-12804
-
-
- HY-P3137
-
|
TRV056
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
TRV056 is a Gq-biased ligand of the angiotensin II receptor type 1 (AT1R). TRV056 is efficacious in stimulating cellular Gq-mediated signaling. TRV056 can be used to develop the Gq-biased AT1R agonists.
|
-
- HY-N1923
-
-
- HY-16953
-
|
JNJ 303
|
Potassium Channel
|
Cardiovascular Disease
|
|
JNJ 303 is a potent IKs blocker with an IC50 value of 64 nM. JNJ 303 does not have any effects on other cardiac channels at concentrations of 3.3 μM for INa, Ica, Ito, and IKr. JNJ 303 induces QT-prolongations and causes unprovoked torsades de pointes (TdP).
|
-
- HY-B2141
-
-
- HY-U00369
-
|
FCE 28654
|
Acyltransferase
|
Cardiovascular Disease
|
|
FCE 28654 is an inhibitor of acylCoA: cholesterol acyltransferase (ACAT), weakly inhibiting ACAT in microsomes from rabbit aorta and intestine, and monkey liver, with IC50s of 2.55, 1.08 and 5.69 μM, respcetively.
|
-
- HY-126010
-
|
Dooku1
|
Others
|
Cardiovascular Disease
|
|
Dooku1, an analog of Yoda1, is a selective antagonist of the endogenous Piezo1 channel. Dooku1 inhibited 2 μM Yoda1-induced Ca 2+-entry with IC50 values of 1.3 μM (in HEK 293 cells) and 1.5 μM (in HUVECs). Dooku1 inhibits Yoda1-induced relaxation of aorta.
|
-
- HY-123349
-
|
5α-Hydroxy-6-keto cholesterol
|
Drug Metabolite
|
Cardiovascular Disease
|
|
5α-Hydroxy-6-keto cholesterol is major metabolite of β-epoxide (5α,6β-epoxycholesterol) during direct exposure of intact cultured human bronchial epithelial cells (16-HBE) to ozone. 5α-Hydroxy-6-keto cholesterol inhibits cholesterol synthesis with an IC50 of 350 nM.
|
-
- HY-U00232
-
-
- HY-B1696A
-
|
Methyldopate hydrochloride
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Methyldopate hydrochloride is an ethyl ester hydrochloride prodrug of α-Methyldopa (α-MD; HY-B0225). Methyldopa (L-(-)-α-Methyldopa) is an α-adrenergic agonist (selective for α2-adrenergic receptors). Methyldopate hydrochloride has the potential for severe hypertension research.
|
-
- HY-108660
-
|
PSB-0739
|
P2Y Receptor
|
Cardiovascular Disease
|
|
PSB-0739 is a high-affinity potent, competitive, nonselective platelet P2Y12 receptor antagonist with a Ki values of 24.9 nM. The P2Y12 receptor plays a crucial role in platelet aggregation. Antithrombotic effect.
|
-
- HY-136347
-
-
- HY-112298
-
-
- HY-119850
-
|
Aladorian
ARM036
|
Others
|
Cardiovascular Disease
|
|
Aladorian (ARM036) is a benzothiazepine derivative, with anti-arrhythmia effect. Aladorian is used for the research of heart failure and catecholaminergic polymorphic ventricular tachycardia.
|
-
- HY-B1357
-
-
- HY-119964
-
|
Cetaben
|
Others
|
Cardiovascular Disease
|
|
Cetaben is a PPARα-independent peroxisome proliferator. Cetaben is a non-fibrate hypolipidemic drug and potently reduces the concentration of cholesterol and triglycerides.
|
-
- HY-B0165
-
-
- HY-14668
-
-
- HY-N8178
-
-
- HY-113618B
-
|
RO2959 monohydrochloride
|
CRAC Channel
Interleukin Related
|
Cardiovascular Disease
|
|
RO2959 monohydrochloride is a potent and selective CRAC channel inhibitor with an IC50 of 402 nM. RO2959 monohydrochloride is a potent blocker of store operated calcium entry (SOCE) mediated by Orai1/Stim1 channels with an IC50 of 25 nM. RO2959 monohydrochloride is also a potent inhibitor of human IL-2 production, and potently blocks T cell receptor triggered gene expression and T cell functional pathways.
|
-
- HY-131277
-
-
- HY-131948
-
|
3-Chlorodiphenylamine
|
Potassium Channel
|
Cardiovascular Disease
|
|
3-Chlorodiphenylamine is a high affinity Ca 2+ sensitizer of cardiac muscle. 3-Chlorodiphenylamine is based on diphenylamine and binds to the isolated N-domain of cardiac troponin C (cTnC) (Kd=6 µM). 3-Chlorodiphenylamine is an excellent starting scaffold for the development of more potent Ca 2+-sensitizing compounds due to its small size, and can be used for systolic heart failure research.
|
-
- HY-15284A
-
|
Prasugrel hydrochloride
PCR 4099 hydrochloride
|
P2Y Receptor
|
Cardiovascular Disease
|
|
Prasugrel hydrochloride (PCR 4099 hydrochloride), a thienopyridine and prodrug, inhibits platelet function. Prasugrel hydrochloride is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation.
|
-
- HY-A0124A
-
-
- HY-B0093A
-
-
- HY-P1766
-
-
- HY-100276
-
-
- HY-B0006B
-
-
- HY-122560
-
|
VU0134992
|
Potassium Channel
|
Cardiovascular Disease
|
|
VU0134992 is the first subtype-preferring, orally active and selective Kir4.1 potassium channel pore blocker, with an IC50 of 0.97 µM. VU0134992 is 9-fold selective for homomeric Kir4.1 over Kir4.1/5.1 concatemeric channels (IC50=9 µM) at -120 mV.
|
-
- HY-101308A
-
|
MRS2179 tetrasodium hydrate
|
P2Y Receptor
|
Cardiovascular Disease
|
|
MRS2179 tetrasodium hydrate is a competitive P2Y1 receptor antagonist, with a Kb of 102 nM and a pA2 of 6.99 for turkey P2Y1 receptor. MRS2179 tetrasodium hydrate is selective for P2Y1 over P2X1 (IC50=1.15 µM), P2X3 (12.9 µM), P2X2, P2X4, P2Y2, P2Y4, and P2Y6 receptors. MRS2179 tetrasodium hydrate inhibits platelet aggregation.
|
-
- HY-10268S
-
-
- HY-P3136
-
|
TRV055
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
TRV055 is a Gq-biased ligand of the angiotensin II receptor type 1 (AT1R). TRV055 is efficacious in stimulating cellular Gq-mediated signaling. TRV055 can be used to develop the Gq-biased AT1R agonists.
|
-
- HY-12319A
-
|
Cardiogenol C hydrochloride
|
β-catenin
Wnt
|
Cardiovascular Disease
|
|
Cardiogenol C hydrochloride is a potent cell-permeable pyrimidine inducer which prompts the differentiation of ESCs into cardiomyocytes (EC50=100 nM). Cardiogenol C hydrochloride also acts cardiomyogenic on already lineage-committed progenitor cell types with a limited degree of plasticity. Cardiogenol C hydrochloride is a useful cardiomyogenic agent and can be used as a tool to improve cardiac repair by cell transplantation therapy in animal models.
|
-
- HY-N7004
-
-
- HY-B1304
-
-
- HY-18071
-
|
BI-9627
|
Sodium Channel
|
Cardiovascular Disease
|
|
BI-9627 is potent sodium-hydrogen exchanger isoform 1 (NHE1) inhibitor, with IC50s of 6 and 31 nM in intracellular pH recovery (pHi) and human platelet swelling assays, respectively. BI-9627 displays >30-fold selectivity against NHE2 and with no measurable inhibitory activity against the NHE3 isoform. BI-9627 shows low DDI (drug-drug interaction) potential, excellent pharmacokinetics in rat and dog, and remarkably potent activity in the isolated heart model of ischemia-reperfusion injury.
|
-
- HY-14779S1
-
-
- HY-12246
-
|
XEN445
|
Others
|
Cardiovascular Disease
|
|
XEN445 is a potent and selective EL inhibitor(IC50=0.237 uM), that showed good ADME and PK properties, and demonstrated in vivo efficacy in raising plasma HDLc concentrations in mice.
|
-
- HY-A0126A
-
|
Epoprostenol sodium
Prostaglandin I2 sodium salt; Prostacyclin sodium salt; Flolan
|
Others
|
Cardiovascular Disease
|
|
Epoprostenol sodium (Prostaglandin I2 (sodium salt)), the synthetic form of the natural prostaglandin derivative prostacyclin (prostaglandin I2), is registered worldwide for the treatment of Pulmonary arterial hypertension (PAH). Epoprostenol sodium is used in pulmonary hypertension and transplantation as a potent inhibitor of platelet aggregation.
|
-
- HY-128345
-
|
UDM-001651
|
Protease-Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
UDM-001651 is a potent, selective, and orally bioavailable protease-activated receptor 4 (PAR4) antagonist (IC50=4 nM; Kd=1.4 nM). UDM-001651 shows antiplatelet potency (IC50=25 nM) in a γ-thrombin-induced platelet-rich plasma aggregation assay (γ-Thr PRP).
|
-
- HY-103315
-
-
- HY-100545
-
|
BAPTA-AM
|
Potassium Channel
|
Cardiovascular Disease
|
|
BAPTA-AM is a well-known membrane permeable Ca 2+ chelator. BAPTA-AM inhibits hERG channels, hKv1.3 and hKv1.5 channels in HEK 293 cells with IC50s of 1.3 μM, 1.45 μM and 1.23 μM, respectively.
|
-
- HY-B0908
-
-
- HY-B0419
-
-
- HY-N2115
-
|
Araloside A
Chikusetsusaponin IV
|
Renin
|
Cardiovascular Disease
|
|
Araloside A (Chikusetsusaponin IV) is a component of Panax japonicus, with low-renin-inhibitory activity, with an IC50 of 77.4 μM.
|
-
- HY-A0043
-
-
- HY-N8095
-
|
Kushenol N
|
Others
|
Cardiovascular Disease
|
|
Kushenol N is a prenylated flavonoid that can be isolated from the root of Sophora flavescens. Kushenol N has anti-allergic and vasorelaxation activities.
|
-
- HY-P2538
-
-
- HY-128694
-
|
Foropafant
SR27417
|
Others
|
Cardiovascular Disease
|
|
Foropafant (SR27417) highly potent, competitive, selective and orally active antagonist of platelet-activating factor (PAF) receptor, with a Ki value of 57 pM for [ 3H]PAF binding, at least 5-fold lower than that of unlabeled PAF itself. Foropafant potently inhibits PAF-induced aggregation of rabbit and human platelets.
|
-
- HY-112499
-
|
Menaquinone-7
Vitamin K2-7; Vitamin K2(35); Vitamin MK-7
|
Others
|
Cardiovascular Disease
|
|
Menaquinone-7 (Vitamin K2-7), belongs to a class of K2-vitamin homologs, is originally discovered as the anti-hemorrhagic factors. Menaquinone-7 (Vitamin K2-7) is identified as the most bioactive cofactor for the carboxylation reaction of Gla-proteins . Supplementation with Menaquinone-7 (Vitamin K2-7) is a pharmacological option for activating matrix Gla protein and intervening in the progression of calcific aortic valve stenosis (CAVS).
|
-
- HY-N3961
-
|
Neoglycyrol
|
Others
|
Cardiovascular Disease
|
|
Neoglycyrol is isolated from the root of Glycyrrhiza uralensis Fisch. Neoglycyrol is a potential myocardial protection active compound screened from traditional patent medicine Tongmai Yangxin pill (TMYXP).
|
-
- HY-15706
-
-
- HY-N8102
-
-
- HY-18763
-
|
Indobufen
Ibustrin
|
COX
|
Cardiovascular Disease
|
|
Indobufen is a platelet aggregation inhibitor. Indobufen is a reversible platelet cyclooxygenase (Cox) activity inhibitor. Indobufen suppresses thromboxane A2 (TxA2) synthesis. Indobufen down-regulates tissue factor (TF) in monocytes.
|
-
- HY-109058
-
|
Firibastat
QGC001; RB150
|
Aminopeptidase
|
Cardiovascular Disease
|
|
Firibastat (QGC001), an orally active brain penetrating prodrug of EC33, is a first-in-class brain aminopeptidase A (APA) inhibitor (Ki=200 nM). Firibastat selectively and specifically inhibits conversion of brain angiotensin-II into angiotensin-III and decreases blood pressure in hypertensive rats.
|
-
- HY-107754
-
|
Cesium chloride
|
Potassium Channel
|
Cardiovascular Disease
|
|
Cesium chloride is a blocker of potassium channel. Cesium chloride prevents the decrease of Na + transport produced by Alloxan. Cesium chloride has induced cardiac arrhythmias, including torsade de pointes in animal models.
|
-
- HY-14304
-
-
- HY-119802
-
-
- HY-112605
-
-
- HY-100615
-
-
- HY-N2165
-
-
- HY-N0079
-
-
- HY-17567B
-
-
- HY-19424
-
-
- HY-U00136
-
-
- HY-18336
-
-
- HY-109059
-
-
- HY-W007606
-
-
- HY-B0612DS1
-
-
- HY-17608
-
-
- HY-14779
-
-
- HY-P1829A
-
|
Angiotensin I/II (1-6) (TFA)
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
Angiotensin I/II (1-6) TFA contains the amino acids 1-6 and is converted from Angiotensin I/II peptide. The precursor angiotensinogen is cleaved by renin to form angiotensin I. Angiotensin I ishydrolyzed by angiotensin-converting enzyme (ACE) to form the biologically active angiotensin II. Angiotensin II has been investigated for the treatment, basic science, and diagnostic of Hypertension, Renin Angiotensin System, and Idiopathic Membranous Nephropathy.
|
-
- HY-B1409
-
-
- HY-P1214A
-
-
- HY-U00113
-
-
- HY-N7326
-
-
- HY-15991
-
-
- HY-10915
-
|
LUF6096
|
Adenosine Receptor
|
Cardiovascular Disease
|
|
LUF6096, a potent allosteric enhancer of the adenosine A3 receptor, is able to allosterically enhance agonist binding. LUF6096 shows low orthosteric affinity for any of the adenosine receptors. LUF6096 shows protective effects in myocardial ischemia/reperfusion injury.
|
-
- HY-U00039
-
-
- HY-119350
-
|
Zalunfiban
RUC-4
|
Others
|
Cardiovascular Disease
|
|
Zalunfiban (RUC-4) is a potent, selective platelet αIIbβ3 antagonist (IC50=45 nM). Zalunfiban can be used for the research of myocardial infarction (MI).
|
-
- HY-19052
-
-
- HY-101750
-
-
- HY-B0153A
-
-
- HY-B0347S
-
-
- HY-U00393
-
-
- HY-N4090
-
-
- HY-B0204
-
-
- HY-11091
-
|
Razaxaban hydrochloride
BMS 561389 hydrochloride; DPC 906 hydrochloride
|
Factor Xa
Thrombin
|
Cardiovascular Disease
|
|
Razaxaban hydrochloride (BMS 561389 hydrochloride) is a highly potent, selective and orally active factor Xa inhibitor with a Ki of 0.19 nM. Razaxaban hydrochloride exhibits excellent selectivity (>5000-fold) for factor Xa over other related serine proteases. Razaxaban hydrochloride is also a potent thrombin inhibitor with a Ki of 540 nM. Razaxaban hydrochloride has strongly antithrombotic activity.
|
-
- HY-10119A
-
|
Vorapaxar sulfate
SCH 530348 sulfate
|
Protease-Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
Vorapaxar sulfate (SCH 530348 sulfate), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar sulfate inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner.
|
-
- HY-112160
-
|
XL-784 free base
|
MMP
|
Cardiovascular Disease
|
|
XL-784 free base is a selective matrix metalloproteinases (MMP) inhibitor, with IC50s of ~1900, 0.81, 120, 10.8, 18, 0.56 nM for MMP-1, MMP-2, MMP-3, MMP-8, MMP-9 and MMP-13, respectively.
|
-
- HY-10217
-
-
- HY-103157
-
|
PD146176
NSC168807
|
Autophagy
Ferroptosis
|
Cardiovascular Disease
|
|
PD146176 (NSC168807), a 15-Lipoxygenase (15-LO) inhibitor, inhibits rabbit reticulocyte 15-LO (Ki=197 nM, IC50=0.54 μM). PD146176 reverses cognitive impairment, brain amyloidosis, and tau pathology by stimulating autophagy in aged triple transgenic mice.
|
-
- HY-N6925
-
-
- HY-N1620
-
|
1-Cinnamoylpyrrolidine
|
Others
|
Cardiovascular Disease
|
|
1-Cinnamoylpyrrolidine (Compound 3), a crude extract prepared from Piper caninum, is a DNA strand scission agent, induces the relaxation of supercoiled pBR322 plasmid DNA.
1-Cinnamoylpyrrolidine (Compound 4) inhibits platelet aggregation induced by PAF with an IC50 of 37.3 μM.
|
-
- HY-103265
-
|
ARL67156 trisodium salt
|
Phosphatase
|
Cardiovascular Disease
|
|
ARL67156 trisodium salt is an inhibitor of ecto-ATPase. ARL 67156 trisodium salt is a weak competitive inhibitor of NTPDase1 (CD39), NTPDase3 and NPP1, with Kis of 11, 18 and 12 μM, respectively. ARL67156 trisodium salt prevents in vivo the development of calcific aortic valve disease.
|
-
- HY-B1399
-
-
- HY-N6066
-
-
- HY-14744A
-
|
Levamlodipine besylate
(S)-Amlodipine besylate; Levoamlodipine besylate
|
Calcium Channel
|
Cardiovascular Disease
|
|
Levamlodipine besylate ((S)-Amlodipine besylate) is a powerful dihydropyridine calcium channel blocker, possessing vasodilation properties and used in the treatment of hypertension and angina.
|
-
- HY-100315
-
-
- HY-120088A
-
-
- HY-14362
-
|
GSK-25
|
ROCK
Ribosomal S6 Kinase (RSK)
|
Cardiovascular Disease
|
|
GSK-25 is a potent, selective and orally bioavailable ROCK1 inhibitor (IC50=7 nM). GSK-25 maintains good selectivity against a panel of 31 kinases (>100 fold), as well as RSK1 and p70S6K (RSK1: IC50=398 nM, p70S6K: IC50=1 μM). GSK-25 inhibits P450 profile (IC50s of 2.5, 5.2, 2.5 µM for CYP2C9, CYP2D6, CYP3A4, respectively).
|
-
- HY-104081
-
|
Cholestyramine
Cholestyramine resin; Colestyramine
|
Others
|
Cardiovascular Disease
|
|
Cholestyramine (Colestyramine) is a bile acid binding resin and can inhibit intestinal bile acid absorption which results in the increasing bile acid synthesis from cholesterol.
|
-
- HY-131180
-
|
BMS-986235
LAR-1219
|
Others
|
Cardiovascular Disease
|
|
BMS-986235 (LAR-1219) is a selective, orally active formyl peptide receptor 2 (FPR2) agonist, with EC50s of 0.41 nM and 3.4 nM for hFPR2 and mFPR2, respectively. BMS-986235 has potential for the prevention of heart failure.
|
-
- HY-16787
-
|
ICA-121431
|
Sodium Channel
|
Cardiovascular Disease
|
|
ICA-121431 is a nanomolar potent and broad-spectrum voltage-gated sodium channel (Nav) blocker, shows equipotent selectivity for human Nav1.1 and Nav1.3 subtypes with IC50 values of 13 nM and 23 nM, respectively. ICA-121431 shows less potent inhibition of Nav1.2 (IC50=240 nM) and 1,000 fold selectivity against Nav1.4, Nav1.6, and the TTX-resistant human Nav1.5 and Nav1.8 channels (IC50s >10 µM).
|
-
- HY-B0231BS
-
-
- HY-103153
-
-
- HY-108997
-
-
- HY-B0612A
-
-
- HY-13008
-
-
- HY-135390
-
|
Hydroxy desmethyl Bosentan
Ro 64-1056
|
Drug Metabolite
|
Cardiovascular Disease
|
|
Hydroxy desmethyl Bosentan (Ro 64-105) is a Bosentan metabolism produced by the cytochrome P450 enzymes CYP2C9 and CYP3A4 in the liver. Bosentan is a competitive and dual antagonist of endothelin-1 (ET) for the ETA and ETB receptors with Ki of 4.7 nM and 95 nM in human SMC, respectively. Bosentan can be used in treatment of pulmonary arterial hypertension.
|
-
- HY-B0368
-
|
Captopril
SQ 14225
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Angiotensin-converting Enzyme (ACE)
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Cardiovascular Disease
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Captopril (SQ 14225), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM) and has been widely used for research of hypertension and congestive heart failure. Captopril is also a New Delhi metallo-β-lactamase-1 (NDM-1) inhibitor with an IC50 of 7.9 μM.
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- HY-U00284
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- HY-76948
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5-R-Rivaroxaban
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Factor Xa
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Cardiovascular Disease
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5-R-Rivaroxaban is (R)-enantiomer of Rivaroxaban. Rivaroxaban (BAY 59-7939) is a highly potent and selective, direct Factor Xa (FXa) inhibitor, achieving a strong gain in anti-FXa potency (IC50 0.7 nM; Ki 0.4 nM).
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- HY-U00143
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- HY-115486
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- HY-N0333
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- HY-117853
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Atreleuton
ABT-761; VIA-2291
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Lipoxygenase
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Cardiovascular Disease
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Atreleuton (ABT-761) is a selective, reversible, and orally bioavailable 5-Lipoxygenase (5-LO) inhibitor. Atreleuton (ABT-761) exhibits potent and selective inhibition of leukotriene formation.
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- HY-100114
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- HY-125989B
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2-Methylthio-AMP diTEA
2-MeSAMP diTEA; 2-Methylthioadenosine 5′-monophosphate diTEA; 2-Methylthioadenosine 5′-phosphate diTEA
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P2Y Receptor
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Cardiovascular Disease
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2-Methylthio-AMP (2-MeSAMP) diTEA is a selective and direct P2Y12 antagonist. 2-Methylthio-AMP diTEA is an inhibitor of ADP-dependent platelet aggregation.
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- HY-14994
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SCH79797 dihydrochloride
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Protease-Activated Receptor (PAR)
Apoptosis
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Cardiovascular Disease
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SCH79797 dihydrochloride is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. SCH79797 dihydrochloride inhibits binding of a high-affinity thrombin receptor-activating peptide to PAR1 with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 dihydrochloride inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. SCH79797 dihydrochloride has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 dihydrochloride also potently prevents PAR1 activation in vascular smooth muscle cells, endothelial cells, and astrocytes.
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- HY-B0968
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Trimetazidine dihydrochloride
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Autophagy
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Cardiovascular Disease
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Trimetazidine dihydrochloride is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine dihydrochloride is an effective antianginal agent and a cytoprotective drug, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine dihydrochloride triggers autophagy. Trimetazidine dihydrochloride is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor.
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- HY-P1271
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Catestatin
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nAChR
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Cardiovascular Disease
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Catestatin is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin is an endogenous peptide that regulates cardiac function and blood pressure. Catestatin is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release.
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- HY-103002
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SU5408
VEGFR2 Kinase Inhibitor I
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VEGFR
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Cardiovascular Disease
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SU5408 (VEGFR2 Kinase Inhibitor I) is a potent and cell-permeable inhibitor of VEGFR2 kinase with an IC50 of 70 nM.
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- HY-100239
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- HY-19644
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GSK2256294A
GSK 2256294
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Epoxide Hydrolase
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Cardiovascular Disease
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GSK2256294A is a potent, reversible, tight binding inhibitor of isolated recombinant human sEH (soluble epoxide hydrolase) (IC50 = 27 pM; t1/2 = 121 min) and displays potent inhibition against the rat (IC50 = 61 pM) and murine (IC50 = 189 pM) orthologs of sEH.
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- HY-P1770
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Adrenomedullin (16-31), human
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CGRP Receptor
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Cardiovascular Disease
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Adrenomedullin (16-31), human is amino acid residues 16-31 fragment of human adrenomedullin (hADM). Adrenomedullin has appreciable affinity for the CGRP1 receptor. Adrenomedullin (16-31), human possesses pressor activity in the systemic vascular bed of the rat, but not the cat.
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- HY-P1486A
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- HY-17403
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- HY-100245
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- HY-W010184
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- HY-W071746
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Linolelaidic acid
Linoelaidic acid
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Endogenous Metabolite
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Cardiovascular Disease
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Linolelaidic acid (Linoelaidic acid), an omega-6 trans fatty acid, acts as a source of energy. Linolelaidic acid is an essential nutrient, adding in enteral, parenteral, and infant formulas. Linolelaidic acid can be used for heart diseases research.
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- HY-101973
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- HY-105309
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GSK-626616
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DYRK
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Cardiovascular Disease
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GSK-626616 is a potent, orally bioavailable inhibitor of DYRK3 (IC50=0.7 nM). GSK-626616 inhibits other members of the DYRK family (e.g., DYRK1A and DYRK2) with similar potency, which is a potential therapy for the treatment of anemia.
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- HY-114252
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Strophanthidin
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Na+/K+ ATPase
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Cardiovascular Disease
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Strophanthidin is a naturally available cardiac glycoside. Strophanthidin 0.1 and 1 nmol/L increases and 1~100 µmol/L inhibits the Na+/K+-ATPase activities, but Strophanthidin 10 and 100 nmol/L does not affect Na+/K+-ATPase activities in cardiac sarcolemmal. Strophanthidin increases both diastolic and systolic intracellular Ca 2+ concentration.
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- HY-121567
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- HY-131346
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- HY-B1181
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- HY-103460
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IRL 2500
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Endothelin Receptor
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Cardiovascular Disease
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IRL 2500 is a potent Endothelin receptor antagonist. IRL 2500 shows IC50 values of 1.3 and 94 nM for ETB and ETA receptors, respectively. IRL 2500 inhibits ETB receptor-mediated blood pressure increase and renal vascular resistance in rats in vivo.
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- HY-N1462
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Atractyloside potassium salt
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Others
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Cardiovascular Disease
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Atractyloside potassium salt is a toxic diterpenoid glycoside that can be isolated from the fruits of Xanthium sibiricum. Atractyloside potassium salt is a powerful and specific inhibitor of mitochondrial ADP/ATP transport. Atractyloside potassium salt inhibits chloride channels from mitochondrial membranes of rat heart.
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- HY-U00354
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- HY-116042
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FSCPX
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Adenosine Receptor
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Cardiovascular Disease
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FSCPX is a potent and selective irreversible antagonist of A1 adenosine receptor (A1AR), with low nanomolar potency for binding to the A1AR. FSCPX could modify the effect of NBTI, a nucleoside transport inhibitor, by reducing the interstitial adenosine level in the guinea pig atrium.
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- HY-N0590
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Corynoxeine
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ERK
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Cardiovascular Disease
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Corynoxeine, isolated from the hook of Uncaria rhynchophylla, is a potent ERK1/ERK2 inhibitor of key PDGF-BB-induced vascular smooth muscle cells (VSMCs) proliferation.
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- HY-17369
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- HY-B2233
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- HY-P1486
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- HY-136278
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- HY-14858
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Derenofylline
SLV 320
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Adenosine Receptor
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Cardiovascular Disease
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Derenofylline (SLV 320) is a potent, selective and orally active adenosine A1 receptor antagonist, with Ki values of 1 nM, 200 nM and 398 nM for human A1, A3 and A2A receptors respectively. Derenofylline suppresses cardiac fibrosis and attenuates albuminuria without affecting blood pressure in rats.
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- HY-B0612
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- HY-112544
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IK1 inhibitor PA-6
PA-6
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Potassium Channel
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Cardiovascular Disease
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IK1 inhibitor PA-6 (PA-6), a pentamidine analogue, is a selective and potent IK1 (KIR2.x ion-channel-carried inward rectifier current) inhibitor, with IC50 values of 12-15 nM for human and mouse KIR2.x currents. IK1 inhibitor PA-6 (PA-6) elevates KIR2.1 protein expression and induces intracellular KIR2.1 accumulation. IK1 inhibitor PA-6 (PA-6) has the potential to treat atrial fibrillation and arrhythmia.
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- HY-112441
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- HY-U00134
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Benzcyclane
Bencyclane; Benzcyclan
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Others
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Cardiovascular Disease
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Benzcyclane (Bencyclane; Benzcyclan) is a platelet aggregation inhibitor and a vasodilator effective in a variety of peripheral circulation disorders.
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- HY-15378
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- HY-15799
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- HY-W014394
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Vanillyl butyl ether
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Others
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Cardiovascular Disease
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Vanillyl butyl ether is a major contributor to the characteristic flavor and fragrance of vanilla. Vanillyl butyl ether is one of the eco-friendly and nontoxic substances. Vanillyl butyl ether has been proposed as a mild warming agent providing a warming sensation and enhancing the blood circulation.
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- HY-14284
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- HY-10264A
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Edoxaban tosylate
DU-176b
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Factor Xa
Thrombin
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Cardiovascular Disease
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Edoxaban tosylate (DU-176b) is a selective, potent and orally active factor Xa (FXa) inhibitor with Kis of 0.561 nM and 2.98 nM for free FXa and prothrombinase, respectively. Edoxaban tosylate is an anticoagulant agent and can be used for stroke prevention. Edoxaban tosylate is a also weak inhibitor of thrombin and factor IXaβ (FIXa), with Kis of 6.00 μM and 41.7 μM, respectively, exhibits >10 000-fold selectivity for FXa. Edoxaban tosylate has antithrombotic properties and has potential for thromboembolic diseases treatment.
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- HY-10835
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DG-041
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Prostaglandin Receptor
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Cardiovascular Disease
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DG-041 is a potent, high affinity and selective EP3 receptor antagonist with IC50s of 4.6 nM and 8.1 nM in the binding and FLIPR assay, respectively. DG-041 inhibits PGE2 facilitation of platelet aggregation. DG-041 crosses the blood-brain barrier.
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- HY-B1236
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- HY-135328
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- HY-12502A
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- HY-B2233B
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Phosphorylcholine
Phosphocholine
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Endogenous Metabolite
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Cardiovascular Disease
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Phosphatidylcholine is the main phospholipid component in eukaryotic biofilms. Phosphatidylcholine exists in commensal or pathogenic bacteria associated with eukaryotes in prokaryotes. Phosphorylcholine exhibits a surprising range of immunomodulatory properties.
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- HY-N8214
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- HY-12402
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- HY-111557
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YM-254890
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P2Y Receptor
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Cardiovascular Disease
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YM-254890 is a selective Gαq/11 protein inhibitor isolated from Chromobacterium sp. YM-254890 shows no inhibition of other G protein subtypes. YM-254890 inhibits platelet aggregation induced by ADP by blocking the P2Y1 signal transduction pathway, with an IC50 value below 0.6 μM.
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- HY-107658
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- HY-N0107
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Cyclovirobuxine D
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Apoptosis
Autophagy
mTOR
Akt
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Cardiovascular Disease
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Cyclovirobuxine D (CVB-D) is the main active component of the traditional Chinese medicine Buxus microphylla. Cyclovirobuxine D induces autophagy and attenuates the phosphorylation of Akt and mTOR. Cyclovirobuxine D inhibits cell proliferation of gastric cancer cells through suppression of cell cycle progression and inducement of mitochondria-mediated apoptosis. Cyclovirobuxine D is beneficial for heart failure induced by myocardial infarction.
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- HY-105940
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IQB-782
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Others
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Cardiovascular Disease
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IQB-782 is a cysteine derivative. IQB-782 has inhibition for thrombin activatable fibrinolysis inhibitor (TAFI), with an Ki(app) of 0.14 μM. IQB-782 shows a potent mucolytic-expectorant activity.
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- HY-103484
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GATA4-NKX2-5-IN-1
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Others
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Cardiovascular Disease
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GATA4-NKX2-5-IN-1 (Compound 3) dose-dependently inhibits the GATA4–NKX2-5 transcriptional synergy with an IC50 of 3 μM. GATA4-NKX2-5-IN-1 exhibits no activity on the protein kinases involved in the regulation of GATA4 phosphorylation, and it modulates the hypertrophic agonist-induced cardiac gene expression.
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