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By Targets:	5-HT Receptor (1) Adrenergic Receptor (1) Antibiotic (3) Apoptosis (3) Autophagy (1) Bacterial (3) c-Kit (3) Carbonic Anhydrase (1) Cytochrome P450 (1) Endogenous Metabolite (1) FAK (2) FGFR (3) Histamine Receptor (1) Histone Methyltransferase (2) Influenza Virus (2) PDGFR (3) RSV (3) Src (3)
By Research Areas:	Cancer (5) Cardiovascular Disease (4) Endocrinology (1) Infection (6) Metabolic Disease (2) Neurological Disease (1)

Inhibitors & Agonists

Screening Libraries

Natural
Products

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-B1907

Rifamycin sodium Rifamycin SV sodium	Bacterial Antibiotic	Infection
Rifamycin sodium (Rifamycin SV monosodium) belongs to the family of ansamycin antibiotics and has been isolated from the fermentation of A. mediterranei or its mutants. Rifamycin sodium displays a broad spectrum of antibiotic activity against Gram-positive and, to a lesser extent, Gram-negative bacteria .

HY-100596

AS1842856 Maximum Cited Publications 59 Publications Verification	Autophagy	Metabolic Disease
AS1842856, a specific Foxo1 inhibitor (IC₅₀=30 nM), potently suppresses autophagy . AS1842856 reduces Foxo1 activity and, to a lesser extent, inhibits Foxo1 protein expression by simply binding to Foxo1 .

HY-133031

CSV0C018875	Histone Methyltransferase	Cancer
CSV0C018875 is a quinoline-based EHMT2/G9a inhibitor. CSV0C018875 exhibits lesser cytotoxicity than BIX-01294 .

HY-W780787

(E,Z)-3,13-Octadecadienyl acetate E3,Z13-18:Ac	Others	Endocrinology
(E,Z)-3,13-Octadecadienyl acetate (E3,Z13-18:Ac) is an insect sex pheromone that elicits attraction in male lesser peachtree borers (Lesser Peachtree Borer), which can be isolated from female lesser peachtree borers .

HY-133031A

CSV0C018875 hydrochloride	Histone Methyltransferase	Others
CSV0C018875 hydrochloride is a G9a (EHMT2) inhibitor that inhibits G9a activity. CSV0C018875 can effectively inhibit G9a activity in both enzyme and cell-based assays, and its toxicity is much lower than that of the known G9a inhibitor BIX-01294. CSV0C018875 binds tightly to the active site cavity of G9a, thereby improving the binding firmness and prolonging the residence time of the compound, further enhancing the inhibitory effect of G9a. CSV0C018875 has the potential to improve its ADME (absorption, distribution, metabolism and excretion) and pharmacodynamic properties through further optimization .

HY-B1907A

Rifamycin Rifamycin SV	Bacterial Antibiotic	Infection
Rifamycin (Rifamycin SV) belongs to the family of ansamycin antibiotics and has been isolated from the fermentation of A. mediterranei or its mutants. Rifamycin displays a broad spectrum of antibiotic activity against Gram-positive and, to a lesser extent, Gram-negative bacteria .

HY-130626

RSV/IAV-IN-1	RSV Influenza Virus	Infection
RSV/IAV-IN-1 (compound 14e) is a potent and dual inhibitor of RSV/IAV. RSV/IAV-IN-1 has lesser cytotoxicity than the clinical agent, Ribavirin. RSV/IAV-IN-1 has the potential for the research of RSV and/or IAV infections .

HY-130627

RSV/IAV-IN-2	RSV Influenza Virus	Infection
RSV/IAV-IN-2 (compound 14c) is a potent and dual inhibitor of RSV/IAV. RSV/IAV-IN-2 has lesser cytotoxicity than the clinical agent, Ribavirin. RSV/IAV-IN-2 has the potential for the research of RSV and/or IAV infections .

HY-154966

RSV L-protein-IN-3	RSV	Infection
RSV L-protein-IN-3 is a wild-type RSV polymerase inhibitor with an IC₅₀ value of 10.4 μM and an EC₅₀ value of 2.1 μM (against RSV). RSV L-protein-IN-3 has lesser cytotoxicity than the clinical agent, Ribavirin (HY-B0434) .

HY-B1907R

Rifamycin sodium (Standard)	Bacterial Antibiotic	Infection
Rifamycin (sodium) (Standard) is the analytical standard of Rifamycin (sodium). This product is intended for research and analytical applications. Rifamycin sodium (Rifamycin SV monosodium) belongs to the family of ansamycin antibiotics and has been isolated from the fermentation of A. mediterranei or its mutants. Rifamycin sodium displays a broad spectrum of antibiotic activity against Gram-positive and, to a lesser extent, Gram-negative bacteria .

HY-129706

LY127210 free base	Others	Cardiovascular Disease
LY127210 (free base) is a potent vasodilator with antihypertensive effects that reduces pressure in chloralose-anesthetized spontaneously hypertensive rats primarily by direct arteriolar dilation and to a lesser extent by decreasing cardiac output. LY127210 (free base) reduces blood pressure, heart rate and left ventricular end-diastolic pressure in hypertensive rats by reducing vascular resistance .

HY-P3186

Glucose dehydrogenase, recombinant Microorganisms	Endogenous Metabolite	Metabolic Disease
Glucose dehydrogenase, recombinant Microorganisms is a oxidoreductase. Glucose dehydrogenase (GDH) catalyzes the oxidation of β-D-glucose to β-D-glucono-1,5-lactone with simultaneous reduction of the cofactor NADP ⁺ to NADPH or, to a lesser extent, NAD ⁺ to NADH. Glucose dehydrogenase (GDH) accepts both NAD ⁺ and NADP ⁺ as cofactors and can be used for the regeneration of NADH and NADPH .

HY-19340

TMS 5+ Cited Publications (E)-2,3',4,5'-tetramethoxystilbene	Cytochrome P450	Cancer
TMS ((E)-2,3',4,5'-tetramethoxystilbene) is a selective and competitive CYP1B1 inhibitor with an IC₅₀ of 6 nM and a K_i value of 3 nM. TMS shows a lesser extent inhibitory effect on CYP1A1 (IC₅₀=300 nM) and CYP1A2 (IC₅₀=3.1 μM). TMS is a methylated derivative of resveratrol and has anti-cancer activity .

HY-10209

Masitinib 5 Publications Verification AB1010	c-Kit PDGFR Src FGFR FAK Apoptosis	Cancer
Masitinib (AB1010) is a potent, orally bioavailable, and selective inhibitor of c-Kit (IC₅₀=200 nM for human recombinant c-Kit). It also inhibits PDGFRα/β (IC₅₀s=540/800 nM), Lyn (IC₅₀= 510 nM for LynB), Lck, and, to a lesser extent, FGFR3 and FAK. Masitinib (AB1010) has anti-proliferative, pro-apoptotic activity and low toxicity .

HY-10209A

Masitinib mesylate 5 Publications Verification AB-1010 mesylate	c-Kit PDGFR Src FGFR Apoptosis	Cancer
Masitinib mesylate (AB-1010 mesylate) is a potent, orally bioavailable, and selective inhibitor of c-Kit (IC₅₀=200 nM for human recombinant c-Kit). It also inhibits PDGFRα/β (IC₅₀s=540/800 nM), Lyn (IC₅₀= 510 nM for LynB), Lck, and, to a lesser extent, FGFR3 and FAK. Masitinib mesylate (AB-1010 mesylate) has anti-proliferative, pro-apoptotic activity and low toxicity .

HY-101390B

Niguldipine free base	Others	Cardiovascular Disease
Niguldipine free base is a calcium channel blocker with activity in regulating cardiovascular function. Niguldipine free base can reduce systolic and diastolic blood pressure, thereby increasing heart rate and cardiac output. Niguldipine free base exhibits dose-dependent and sustained increases in coronary blood flow. Niguldipine free base also increases perfusion in the kidneys and femoral arteries, but the effect is temporary and to a lesser extent. The effect of Niguldipine free base on myocardial metabolism is not significant .

HY-10209R

Masitinib (Standard)	c-Kit PDGFR Src FGFR FAK Apoptosis	Cancer
Masitinib (Standard) is the analytical standard of Masitinib. This product is intended for research and analytical applications. Masitinib (AB1010) is a potent, orally bioavailable, and selective inhibitor of c-Kit (IC₅₀=200 nM for human recombinant c-Kit). It also inhibits PDGFRα/β (IC₅₀s=540/800 nM), Lyn (IC₅₀= 510 nM for LynB), Lck, and, to a lesser extent, FGFR3 and FAK. Masitinib (AB1010) has anti-proliferative, pro-apoptotic activity and low toxicity .

HY-134043

Chlorthalidone Impurity G Chlorthalidone EP Impurity G	Carbonic Anhydrase	Cardiovascular Disease
Chlorthalidone Impurity G (Chlorthalidone EP Impurity G) is a potential impurity found in commercial preparations of chlorthalidone with moderate antihypertensive effects. Chlorthalidone is a thiazide diuretic that inhibits the Na+/Cl- cotransporter in the distal tubule of the kidney, thereby preventing sodium and chloride reabsorption, resulting in decreased plasma volume and cardiac output. It also inhibits carbonic anhydrase (CA), including isoenzymes CAVB, VII, IX, XII, and XIII (Kis=2.8-23 nM) and to a lesser extent CAI, CAII, IV, VA, and VI (Ki=138-1,347 nM), mediating vasodilatory activity.

HY-121586

Nafazatrom Bay g 6575	Others	Cardiovascular Disease
Nafazatrom (Bay g 6575) is an orally active cardioprotective agent that protects against ischemic damage. Nafazatrom dose-dependently inhibits neutrophil aggregation, superoxide anion generation, arachidonic acid metabolism, and to a lesser extent the release of β-glucosidase, platelet aggregation or arachidonic acid in vitro. Acid metabolism has no significant effect. In a dog ischemia-reperfusion model, Nafazatrom (10 mg/kg; po) reduced infarct size and the occurrence of arrhythmias and rescued ischemic myocardial function without affecting any hemodynamic changes. The basis of Nafazatrom's cardioprotection may be inhibition of neutrophil function and cellular infiltration in vitro .

HY-117046A

AVN-101 hydrochloride	5-HT Receptor Histamine Receptor Adrenergic Receptor	Neurological Disease
AVN-101 hydrochloride is a potent, brain-penetrant and orally active 5-HT7 receptor antagonist (K_i of 153 pM), with slightly lesser potency toward 5-HT6, 5-HT2A, and 5HT-2C receptors (K_i values of 2.04 nM, 1.56 nM, and 1.17 nM, respectively). AVN-101 hydrochloride also exhibits a rather high affinity toward histamine H1 (K_i of 0.58 nM) and adrenergic α2A, α2B, and α2C (Ki= 0.41-3.6 nM) receptors. AVN-101 hydrochloride can be studied in such diseases as general anxiety disorders, depression, schizophrenia, and multiple sclerosis .

HY-102093A

ZD 7155	Others	Others
ZD 7155 is an AT1R selective antagonist with renal function modulating activity. The effects of ZD 7155 on glomeruli and tubules were measured in 1- (N = 9) and 6-week-old (N = 13) lambs. Pretreatment with ZD 7155 after L-NAME infusion did not alter glomerular function in 1- or 6-week-old lambs. During postnatal development, Ang II modulates the effects of NO on electrolyte handling via AT1R and AT2R. In 6-week-old lambs, selective inhibition of AT1R and AT2R increased the excretion of Na+, K+, and Cl-. In 6-week-old lambs, pretreatment with ZD 7155 and PD 123319 followed by the addition of L-NAME increased urine flow rate by 200%, free water clearance by 50%, and decreased urine osmolality by 40%. The same trends of changes in these variables were also observed when L-NAME was added to ZD 7155 or PD 123319, although to a lesser extent.

Cat. No.	Product Name

HY-L145

Antihypertensive Compound Library	639 compounds
The majority of hypertensive patients have primary (or essential) hypertension, that is, hypertension in which secondary causes are not present. Management aims to control arterial pressure, prevent end-organ damage (cerebrovascular, cardiovascular, and renal), and reduce the risk of premature death. Antihypertensive drugs may be divided into two broad groups, the first group being those which directly or indirectly block the renin–angiotensin system (RAS), for example, ACEIs, angiotensin receptor antagonists (ARAs), direct renin inhibitors (DRIs), and to a lesser extent β-blockers. The second group of drugs works by increasing water and sodium excretion, thereby reducing intravascular volume, or by causing vasodilatation through non-RAS pathways, for example, diuretics and calcium channel blockers (CCBs). MCE offers a unique collection of 639 compounds with identified and potential antihypertensive activity. MCE Antihypertensive Compound Library is critical for antihypertensive drug discovery and development.

Antihypertensive Compound Library

639 compounds

The majority of hypertensive patients have primary (or essential) hypertension, that is, hypertension in which secondary causes are not present. Management aims to control arterial pressure, prevent end-organ damage (cerebrovascular, cardiovascular, and renal), and reduce the risk of premature death.

Antihypertensive drugs may be divided into two broad groups, the first group being those which directly or indirectly block the renin–angiotensin system (RAS), for example, ACEIs, angiotensin receptor antagonists (ARAs), direct renin inhibitors (DRIs), and to a lesser extent β-blockers. The second group of drugs works by increasing water and sodium excretion, thereby reducing intravascular volume, or by causing vasodilatation through non-RAS pathways, for example, diuretics and calcium channel blockers (CCBs).

MCE offers a unique collection of 639 compounds with identified and potential antihypertensive activity. MCE Antihypertensive Compound Library is critical for antihypertensive drug discovery and development.

Rifamycin sodium Rifamycin SV sodium	Infection Structural Classification Microorganisms Antibiotics Source classification Antibacterial Disease Research Disease Research Fields Other Antibiotics	Bacterial Antibiotic
Rifamycin sodium (Rifamycin SV monosodium) belongs to the family of ansamycin antibiotics and has been isolated from the fermentation of A. mediterranei or its mutants. Rifamycin sodium displays a broad spectrum of antibiotic activity against Gram-positive and, to a lesser extent, Gram-negative bacteria .

(E,Z)-3,13-Octadecadienyl acetate E3,Z13-18:Ac	Structural Classification Natural Products Animals Source classification	Others
(E,Z)-3,13-Octadecadienyl acetate (E3,Z13-18:Ac) is an insect sex pheromone that elicits attraction in male lesser peachtree borers (Lesser Peachtree Borer), which can be isolated from female lesser peachtree borers .

Rifamycin sodium (Standard)	Structural Classification Microorganisms Antibiotics Source classification Antibacterial Disease Research Other Antibiotics	Bacterial Antibiotic
Rifamycin (sodium) (Standard) is the analytical standard of Rifamycin (sodium). This product is intended for research and analytical applications. Rifamycin sodium (Rifamycin SV monosodium) belongs to the family of ansamycin antibiotics and has been isolated from the fermentation of A. mediterranei or its mutants. Rifamycin sodium displays a broad spectrum of antibiotic activity against Gram-positive and, to a lesser extent, Gram-negative bacteria .

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