Cardiovascular Disease

(±)-Equol (Standard) is the analytical standard of (±)-Equol. This product is intended for research and analytical applications. (±)-Equol is the racemate of equol. (±)-equol exhibits EC50s of 200 and 74 nM for human ERα and ERβ, respectively. Equol is a metabolite of the soy isoflavones, daidzin and daidzein.

Sch 13835 is a platelet-derived growth factor (PDGFR) inhibitor.

Tovinontrine (Standard) is the analytical standard of Tovinontrine (HY-109193). This product is intended for research and analytical applications. Tovinontrine (IMR-687) is a highly potent and selective phosphodiesterase-9 (PDE9) inhibitor specifically for the treatment of sickle cell disease. IC₅₀s are 8.19 nM and 9.99 nM for PDE9A1 and PDE9A2, respectively.

GRL-098-22 (Compound 6t) is a potent inhibitor targeting G protein-coupled receptor kinase 5 (GRK5) and GRK6 with IC₅₀ values of 0.6 μM and 0.19 μM, respectively. GRL-098-22 is promising for research of diseases such as heart failure and multiple myeloma.

FCW34 is a cell-permeable, selective Sialyltransferase inhibitor. FCW34 inhibits α2,3-N-linked ST3GALIII (IC₅₀ 1.74 μM) and α2,6-N-linked ST6GALI (IC₅₀ 3.6 μM), reducing N-glycoprotein sialylation. FCW34 decreases cell migration ability by inhibiting the Talin/Integrin/FAK/Paxillin and Integrin/NFκB signaling pathways. FCW34 significantly inhibits tumor growth, reduces angiogenesis, and suppresses spontaneous lung metastasis in a nude mouse model of breast cancer. FCW34 can be used for research on breast cancer.

Perindoprilat-d₃ disodium is deuterated labeled Perindoprilat (HY-B1433). Perindoprilat (S 9780) is an angiotensin-converting enzyme (ACE) inhibitor with the IC₅₀ value ranging from 1.5 to 3.2 nM. Perindoprilat can be used in hypertension research.

Enalapril-d₃ (MK-421-d₃) is the deuterated-labeled Enalapril (HY-B0331). Enalapril is an orally active angiotensin-converting enzyme inhibitor. Enalapril blocks the conversion of angiotensin I to angiotensin II, regulates the renin-angiotensin system, reduces preload and afterload, and decreases plasma angiotensin II levels. Enalapril inhibits apoptosis, reduces nitric oxide metabolite levels, stabilizes endothelial cells, enhances endothelial antioxidant defense, scavenges reactive oxygen species (ROS), and alleviates neuronal damage. Enalapril attenuates glutathione depletion, protein/lipid oxidation, tissue damage, and type III collagen immunolabeling in organs of diabetic rats. Enalapril reduces systolic blood pressure and urinary albumin excretion, and delays the progression of diabetic cardiac/renal injury. Enalapril is used in research related to asymptomatic left ventricular dysfunction, congestive heart failure, Alzheimer's disease, diabetes mellitus, acute myocardial infarction, atrial fibrillation, hypertension, cerebral ischemia, chronic heart failure, and single-ventricle physiology.

VPC12249 (ammonium) is a phosphatidic acid.

Methyl maslinate is a β-adrenergic antagonist. Methyl maslinate is a potent cardiotonic and antidysrhythmic agent. Methyl maslinate has the potential for hypertension research.

VBIT-4 (Standard) is the analytical standard of VBIT-4 (HY-129122). This product is intended for research and analytical applications. VBIT-4 is an inhibitor of voltage-dependent anion channel 1 (VDAC1) oligomerization with a binding affinity (K_d) of 17 μM. VBIT-4, as an apoptosis inhibitor, can be used for therapeutic purposes in apoptosis-associated disorders, such as neurodegenerative and cardiovascular diseases.

1-EBIO (1-Ethyl-2-benzimidazolinone) (Standard) is the analytical standard of 1-EBIO (HY-101360). This product is intended for research and analytical applications. 1-EBIO is an activator of Ca²⁺ sensitive K⁺ channels wirh an EC₅₀ of 136 μM for K_Ca3.1. 1-EBIO induces Cl^- secretion, K⁺ conductance, membrane hyperpolarization, and afterhyperpolarisation currents. 1-EBIO reduces epileptiform activity, seizure incidence, and rescues cells from Ionomycin (HY-13434)-induced death.

Luminacin C1 has a strong inhibitory effect on capillary formation (IC₅₀ is less than 0.1 μg/mL).

H142/08 is a β1-adrenergic receptor-selective agonist. H142/08 induces concentration-dependent relaxation of isolated rat uterus and acts as a chronotropic stimulant to increase atrial rate, and its effects are effectively antagonized by Pafenolol (HY-165495). H142/08 also antagonizes the chronotropic effect of isoproterenol on isolated rat right atrium, but requires a higher proportion of receptor occupancy to produce sufficient stimulatory effects.

(+)-ITD-1 is an inhibitor for TGF-β, that inhibits the TGF-β2 with an IC₅₀ of 0.46 μM. (+)-ITD-1 promotes the degradation of TGF-b type II receptor (TGFBR2) and the differentiation of cardiomyocyte, and inhibits the mesoderm formation in the early differentiation stage of mouse embryonic stem cells (mESCs).

Aprocitentan (Standard) is the analytical standard of Aprocitentan. This product is intended for research and analytical applications. Aprocitentan (ACT-132577) is the major and pharmacologically active metabolite of Macitentan. Aprocitentan is dual ETA/ETB antagonist with IC50s of 3.4 nM and 987 nM, and pA2 valus of 6.7 and 5.5, respectively.

Tolvaptan (Standard) is the analytical standard of Tolvaptan. This product is intended for research and analytical applications. Tolvaptan is a selective, competitive and orally active vasopressin receptor 2 (V2R) antagonist with an IC50 of 1.28 μM for the inhibition of arginine vasopressin (AVP)-induced platelet aggregation. Tolvaptan induces cell apoposis and affects cell cycle. Tolvaptan can be used for the research of hyponatremia.

Isopentaquine is an orally active antimalarial agent. Isopentaquine induces mild morphological changes in the exoerythrocytic stage of Plasmodium fallax, with a ED₅₀ of 6.7 mg/L. Isopentaquine causes degenerative changes in the development of Plasmodium oocysts in infected mosquitoes. Isopentaquine reduces the infectivity of Plasmodium falciparum gametocytes. Isopentaquine impairs sympathetic cardiovascular reflexes. Isopentaquine decreases the recurrence rate and total disease duration of Plasmodium vivax infection. Isopentaquine can be used in malaria-related research.

Cyclocreatine, a creatine analogue, acts as a brain-penetrant and potent bioenergetic protective agent by providing high levels of ATP. Cyclocreatine can be phosphorylated and dephosphorylated by creatine kinases. Cyclocreatine suppresses creatine metabolism ameliorating the cognitive, autistic and epileptic phenotype in a mouse model of creatine transporter defciency. Cyclocreatine protects against ischemic injury and enhances cardiac recovery during early reperfusion in dogs and rats. Cyclocreatine decreases plaque-adjacent neuronal dystrophy in TREM2-deficient mice with amyloid-β pathology. Cyclocreatine is proming for research of ischemic heart disease, cardiovascular diseases, Alzheimer’s disease and other neurodegenerative diseases associated with microglial dysfunction, prostate cancer.

ZINC13466751 (Standard) is the analytical standard of ZINC13466751 (HY-101028). This product is intended for research and analytical applications. ZINC13466751 is a potent inhibitor of HIF-1α/von Hippel-Lindau interaction with an IC50 of 2.0 µM.

(Rac)-BW 245C is a Rac isomer of BW 245C (HY-101987 ). BW 245C is a prostanoid DP-receptor (DP1) agonist, can be used to study stroke.