Search Result
Results for "
contractile
" in MedChemExpress (MCE) Product Catalog:
5
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-W050000
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- HY-111098
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TRP Channel
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Cardiovascular Disease
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GSK1702934A is a selective TRPC3 agonist. GSK1702934A modulates cardiac contractility and f arrhythmogenesis by activation of TRPC3 .
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- HY-162345
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Others
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Cardiovascular Disease
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CK-963 is an activator for cardiac troponin (cTnC) with Ki of 11.5 μM. CK-963 exhibits activity in enhancing cardiac contractility in Sprague-Dawley rats .
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- HY-123268A
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Adrenergic Receptor
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Cardiovascular Disease
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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-106049
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Others
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Cardiovascular Disease
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Acrihellin is a type of cardiac-active steroid. Acrihellin can increase the contractility of the left atrium in guinea pigs .
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- HY-103296
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- HY-N9141
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5-HT Receptor
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Neurological Disease
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Nantenine is a serotonergic receptor antagonist. Nantenine selectively inhibits the contractile response of tissues to serotonin. Nantenine can be isolated from Nandina domestica .
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- HY-125304
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Neurokinin Receptor
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Endocrinology
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L 363851 is a Neurokinin 2 receptor agonist, and induces the contractile response of tracheal smooth muscle devoid of epithelium (IC50 of 3.2 nM) and phosphoinositide hydrolysis (IC50 of 36 μM).
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- HY-120180
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Calcium Channel
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Cardiovascular Disease
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BMS-188107 is a calcium antagonist that exerts anti-ischemic effects. BMS-188107 improves postischemic contractile function and reduces lactate dehydrogenase release. BMS-188107 can be utilized in cardiovascular research .
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- HY-123268
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Adrenergic Receptor
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Cardiovascular Disease
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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-W016733
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H-D-Cit-OH
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Endogenous Metabolite
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Cardiovascular Disease
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D-Citrulline (H-D-Cit-OH) is a stereoisomer of L-citrulline (HY-N0391). D-Citrulline significantly attenuates polymorphonuclear leukocyte (PMN)-induced cardiac contractile dysfunction in the isolated perfused rat heart subjected to ischemia/reperfusion via a non-NO-mediated mechanism .
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- HY-139801
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CI-907
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Angiotensin-converting Enzyme (ACE)
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Metabolic Disease
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Indolapril hydrochloride (CI-907) is an orally active nonsulfhydryl angiotensin converting enzyme (ACE) inhibitor. Indolapril hydrochloride is highly specific in suppressing the contractile or pressor responses to Angiotensin I. Indolapril hydrochloride is a potent antihypertensive agent .
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- HY-P10655
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Proton Pump
Calcium Channel
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Cardiovascular Disease
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Caloxin 1C2 is a specific PMCA (plasma-membrane Ca 2+-ATPases) inhibitor. Caloxin 1C2 is selective for PMCA4 over PMCA1, 2 and 3. The Ki values of Caloxin 1C2 are 2.3 μM for PMCA4 and 21 μM for PMCA1. Caloxin 1C2 dose not cause any significant effects on total Ca 2+ transfer. Caloxin 1C2 affects coronary contractility .
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- HY-119926
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Hydroxylupanine
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Others
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Cardiovascular Disease
Neurological Disease
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13-Hydroxylupanine (Hydroxylupanine) is the typical alkaloid profile of sweet lupins.13-Hydroxylupanine blocks ganglionic transmission, decreases cardiac contractility and contracts uterine smooth muscle .
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- HY-106844A
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Others
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Cardiovascular Disease
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(+)-EMD 57033 is a cardiac troponin C (cTnC) activator, is a dominant Ca 2+ sensitizer. (+)-EMD 57033 binds the cardiac/slow skeletal troponin C isoform and exerts myocardial contractile promotion function .
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- HY-117717
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Prostaglandin Receptor
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Others
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(Rac)-SC-31391, a prostaglandin analog, is a strong activator of the bladder muscle contractility that enhanced twitch responses elicited by field stimulation in the guinea pig detrusor muscle. (Rac)-SC-31391 contracts human bladder muscle through the activation of PGF2α receptors .
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- HY-120648
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Cytochrome P450
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Cardiovascular Disease
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CAY 10434 is a potent CYP4A hydroxylase inhibitor. CAY 10434 improves contractile response to angiotensin II with the maximal contractile response (Emax) 6764 mg .
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- HY-120648A
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Cytochrome P450
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Cardiovascular Disease
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CAY 10434 dihydrochloride is a potent CYP4A hydroxylase inhibitor. CAY 10434 dihydrochloride improves contractile response to angiotensin II with the maximal contractile response (Emax) 6764 mg .
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- HY-106577
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Cifenline; Ro 22-7796
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Potassium Channel
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Cardiovascular Disease
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Cibenzoline is a potent inhibitor of KATP channel with directly affecting the pore-forming Kir6.2 subunit rather than the SUR1 subunit. Cibenzoline is a class Ia antiarrhythmic agent. Cibenzoline has little anticholinergic activity. Cibenzoline markedly attenuate LVPG which has a close relationship with myocardial contractility decreasing. Cibenzoline has the potential for the research of hypertrophic obstructive cardiomyopathy .
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- HY-106045
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CI 914 free base
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Phosphodiesterase (PDE)
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Cardiovascular Disease
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Imazodan is a selective inhibitor for phosphodiesterase III (PDE III), which increases myocardial contractility by blocking the cAMP degradation, and improves the contractile function of heart. Imazodan serves also as a peripheral vasodilator .
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- HY-106844
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Phosphodiesterase (PDE)
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Cardiovascular Disease
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EMD 53998 is a cardiotonic agent that increases myocardial contractility as an inhibitor for phosphodiesterase III (PDE III) and a calcium sensitizer. EMD 53998 increases myocardial contractility, reduces energy consumption and the risk of inducing arrhythmias .
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- HY-106577R
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Potassium Channel
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Cardiovascular Disease
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Cibenzoline (Standard) is the analytical standard of Cibenzoline. This product is intended for research and analytical applications. Cibenzoline is a potent inhibitor of KATP channel with directly affecting the pore-forming Kir6.2 subunit rather than the SUR1 subunit. Cibenzoline is a class Ia antiarrhythmic agent. Cibenzoline has little anticholinergic activity. Cibenzoline markedly attenuate LVPG which has a close relationship with myocardial contractility decreasing. Cibenzoline has the potential for the research of hypertrophic obstructive cardiomyopathy .
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- HY-106045A
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CI 914
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Phosphodiesterase (PDE)
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Cardiovascular Disease
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Imazodan hydrochloride is the hydrochloride form of Imazodan (HY-106045). Imazodan hydrochloride is a selective inhibitor for phosphodiesterase III (PDE III), which increases myocardial contractility by blocking the cAMP degradation, and improves the contractile function of heart. Imazodan hydrochloride serves also as a peripheral vasodilator .
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- HY-19003
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- HY-121306
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Ricainide
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Others
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Neurological Disease
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Indecainide (Ricainide) is an orally active antiarrhythmic agent. Indecainide can be used in the research of ventricular dysfunction .
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- HY-19003A
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323MHb hydrochloride; Isosulmazole hydrochloride
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Phosphodiesterase (PDE)
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Cardiovascular Disease
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Isomazole (323MHb) hydrochloride is a cardiotonic agent. Isomazole hydrochloridei increases the calcium sensitivity in atrial fibers and has a direct effect on contractile proteins .
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- HY-107645
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mAChR
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Neurological Disease
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DAU 5884 hydrochloride is a potent muscarinic M3 receptor antagonist. DAU 5884 hydrochloride inhibits methacholine-dependent effects on cell proliferation and muscle contractility .
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- HY-13338A
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Others
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Cardiovascular Disease
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(S)-Mabuterol is a selective β2 adrenoreceptor agonist that demonstrates blood pressure reduction and increased heart rate and contractile force in animal models.
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- HY-120926
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Others
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Others
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BBR 2160 is a compound with cardiac electrophysiological effects and is a dihydropyridine calcium antagonist that can reduce myocardial contractility and action potential duration and has calcium antagonist properties.
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- HY-118833
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Others
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Cardiovascular Disease
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RAC 109 is a local anesthetic. RAC 109 reduces ventricular conduction velocity and myocardial contractility in rabbits in a stereospecific manner (EC50=30 μM) .
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- HY-160076
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Apelin Receptor (APJ)
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Cardiovascular Disease
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APJ receptor agonist 8 (compound 99) is an agonist of APJ receptor. APJ receptor agonist 8 increases the load independent cardiac contractility of isolated perfused rat hearts .
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- HY-W008820
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Endogenous Metabolite
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Metabolic Disease
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Glutaric acid, C5 dicarboxylic acid, is an intermediate during the catabolic pathways of lysine and tryptophan. Glutaric acid affects pericyte contractility and migration. Glutaric acid is an indicator of glutaric aciduria type I .
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- HY-119926A
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Hydroxylupanine hydrochloride
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Others
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Cardiovascular Disease
Neurological Disease
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13-Hydroxylupanine Hydroxylupanine is the typical alkaloid profile of sweet lupins. 13-Hydroxylupanine Hydroxylupanine blocks ganglionic transmission, decreases cardiac contractility and contracts uterine smooth muscle .
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- HY-P1721
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Bradykinin Receptor
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Cardiovascular Disease
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NPC 17731 is a new bradykinin (BK) receptor antagonist. NPC 17731 antagonized both the contractile and relaxant responses caused by BK in longitudinal smooth muscle with IC50 of 23 and 29 nM, respectively .
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- HY-122409
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Others
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Others
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Cularine is a compound that relaxes guinea pig tracheal and human bronchial smooth muscle, inhibits contraction induced by a variety of contractile agents, and has nonspecific antispasmodic activity, and its activity is structure-related.
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- HY-123028
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Arginylphenylalaninamide
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Others
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Others
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RFamide (Arginylphenylalaninamide) is a neuropeptide that has contraction-inducing activity in gastropod muscles. Its contractile effect is additive with acetylcholine and is regulated by 5-hydroxytryptamine. It can also mobilize intracellular calcium to maintain tension.
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- HY-105572
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MC-838 calcium
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Others
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Cardiovascular Disease
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Moveltipril calcium (MC-838 calcium) is an orally active angiotensin converting enzyme (ACE) inhibitor with antihypertensive activity. Moveltipril calcium binds via a stable thioester bond and exhibits relative resistance to enzymatic hydrolysis in rat liver homogenate. Moveltipril calcium effectively inhibits ACE extracted from rabbit lung in a concentration-dependent manner. Moveltipril calcium is able to highly specifically inhibit the contractile response to angiotensin-I (AI) in free rat aortic rings and guinea pig ileum preparations, while enhancing the contractile response to calcitonin .
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- HY-112071
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Adrenergic Receptor
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Cardiovascular Disease
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Prenalterol is a selective β1-adrenergic receptor agonist. Prenalterol has no effect on gut smooth muscle contractile activity. Prenalterol can be used for researching cardiovascular disease .
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- HY-108991
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(-)-T-0509
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Adrenergic Receptor
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Cardiovascular Disease
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T-0509 ((-)-T-0509) is a selective full agonist of the β1 receptor. T-0509 activates the cAMP signaling pathway through the β1 receptor and enhances myocardial contractility .
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- HY-111018
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Calcium Channel
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Cardiovascular Disease
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FPL 62129 is an antagonist for calcium channel. FPL 62129 reduces blood pressure and total peripheral resistance, increases the cardiac contractility and cardiac output in anarsthetised beagle model. FPL 62129 also serves as a vasodilator and a direct decelerator .
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- HY-P3853
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Neurokinin Receptor
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Neurological Disease
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GR 87389 is a potent NK2 receptor antagonist. GR 87389 antagonized GA 64349-induced smooth muscle strips contractions in a competitive manner in the human detrusor, prostate and prostatic urethra .
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- HY-W008820S
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Endogenous Metabolite
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Metabolic Disease
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Glutaric acid-d6 is the deuterium labeled Glutaric acid. Glutaric acid is an intermediate during the catabolic pathways of lysine and tryptophan. Glutaric acid affects pericyte contractility and migration. Glutaric acid is an indicator of glutaric aciduria type I[1][2][3].
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- HY-126763
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Others
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Others
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ATI22-107 is a dual-pharmacophore compound designed to simultaneously inhibit cardiac phosphodiesterase (PDE-III) and L-type calcium channels (LTCC), with activity that has specific effects on calcium cycling and contractility in cat ventricular myocytes and trabeculae.
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- HY-113096
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PGD1
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Endogenous Metabolite
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Metabolic Disease
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Prostaglandin D1 is a prostanoid which causes contractile and relaxant on isolated human pial arteries, it is also an inhibitor of ADP-induced platelet aggregation with an IC50 value of 320 ng/ml. Prostaglandin D1 can be used for metabolic research .
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- HY-122364
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Adrenergic Receptor
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Cardiovascular Disease
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Bucumolol hydrochloride is a β-adrenergic receptor antagonist that can slow heart rate (negative chronotropic effect) and reduce cardiac contractility (negative inotropic effect). Bucumolol hydrochloride has antiarrhythmic and local anesthetic activity and can be used in the study of cardiovascular diseases .
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- HY-B1233
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2-Amino-6-methylheptane; 1,5-Dimethylhexylamine; 6-Methyl-2-heptylamine
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Dopamine Receptor
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Others
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Octodrine (2-Amino-6-methylheptane) is a central nervous stimulant that increases the uptake of dopamine and noradrenaline. Octodrine is found to increase the pain threshold, cardiac rate (positive chronotropic effect) and myocardial contractility (positive inotropic effect) .
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- HY-B1233A
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2-Amino-6-methylheptane hydrochloride; 1,5-Dimethylhexylamine hydrochloride; 6-Methyl-2-heptylamine hydrochloride
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Dopamine Receptor
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Neurological Disease
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Octodrine (2-Amino-6-methylheptane) is a central nervous activator that increases the uptake of dopamine and noradrenaline. Octodrine is found to increase the pain threshold, cardiac rate (positive chronotropic effect) and myocardial contractility (positive inotropic effect) .
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- HY-P4678
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Vasopressin Receptor
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Neurological Disease
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(Phe2,Orn8)-Oxytocin is a selective V1 vasopressin agonist. (Phe2,Orn8)-Oxytocin induces a sustained contractility of rabbit epididymis with EC50 value of 280 nM .
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- HY-P4678A
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Vasopressin Receptor
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Neurological Disease
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(Phe2,Orn8)-Oxytocin acetate is a selective V1 vasopressin agonist. (Phe2,Orn8)-Oxytocin acetate induces a sustained contractility of rabbit epididymis with EC50 value of 280 nM .
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- HY-137574
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19(R)-Hydroxy PGE1
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Prostaglandin Receptor
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Others
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19(R)-Hydroxy prostaglandin E1 (19(R)-Hydroxy PGE1), the major prostaglandin in primate semen, is an agonist of EP1 and EP3 receptor subtypes and exhibits contractile activity on smooth muscle preparations .
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- HY-W008820S1
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Endogenous Metabolite
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Metabolic Disease
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Glutaric acid-d4 is the deuterium labeled Glutaric acid. Glutaric acid, C5 dicarboxylic acid, is an intermediate during the catabolic pathways of lysine and tryptophan. Glutaric acid affects pericyte contractility and migration. Glutaric acid is an indicator of glutaric aciduria type I[1][2][3].
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- HY-W008820S2
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Endogenous Metabolite
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Metabolic Disease
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Glutaric acid-d2 is the deuterium labeled Glutaric acid. Glutaric acid, C5 dicarboxylic acid, is an intermediate during the catabolic pathways of lysine and tryptophan. Glutaric acid affects pericyte contractility and migration. Glutaric acid is an indicator of glutaric aciduria type I[1][2][3].
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- HY-153977
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NADPH Oxidase
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Cardiovascular Disease
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GLX481304 is a specific inhibitor of Nox-2 and -4, with IC50s of 1.25 μM. GLX481304 suppresses ROS production in isolated mouse cardiomyocytes and improves cardiomyocyte contractility. GLX481304 can be used for research of ischemic injury to the heart .
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- HY-P3618
-
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Somatostatin Receptor
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Neurological Disease
Inflammation/Immunology
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Cortistatin-29 is a neuropeptide. Cortistatin-29 alleviates neuropathic pain. Cortistatin-29 binds all somatostatin (SS) receptor subtypes with high affinity and shows IC50 values of 2.8 nM, 7.1 nM, 0.2 nM, 3.0 nM, 13.7 nM for SSTR1, SSTR2, SSTR3, SSTR4, SSTR5, respectively. Cortistatin-29 shows anti-fibrotic effects .
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- HY-P2150
-
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Somatostatin Receptor
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Neurological Disease
Inflammation/Immunology
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Cortistatin-29 is a neuropeptide. Cortistatin-29 alleviates neuropathic pain. Cortistatin-29 binds all somatostatin (SS) receptor subtypes with high affinity and shows IC50 values of 2.8 nM, 7.1 nM, 0.2 nM, 3.0 nM, 13.7 nM for SSTR1, SSTR2, SSTR3, SSTR4, SSTR5, respectively. Cortistatin-29 shows anti-fibrotic effects .
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- HY-121467A
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Z-338; YM443
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Cholinesterase (ChE)
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Others
Metabolic Disease
Inflammation/Immunology
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Acotiamide hydrochloride is an orally active, selective and reversible acetylcholinesterase (AChE) inhibitor, with an IC50 of 1.79 μM. Acotiamide hydrochloride can enhance gastric contractility and accelerate delayed gastric emptying. Acotiamide hydrochloride has the potential for the research of functional dyspepsia involving gastric motility dysfunction and intestinal inflammatory .
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- HY-121467
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Z-338 free base; YM443 free base
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Cholinesterase (ChE)
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Metabolic Disease
Inflammation/Immunology
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Acotiamide is an orally active, selective and reversible acetylcholinesterase (AChE) inhibitor, with an IC50 of 1.79 μM. Acotiamide can enhance gastric contractility and accelerate delayed gastric emptying. Acotiamide has the potential for the research of functional dyspepsia involving gastric motility dysfunction and intestinal inflammatory .
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- HY-103283
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GRP(18-27) (porcine)
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Biochemical Assay Reagents
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Neurological Disease
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Neuromedin C porcine (GRP, 18-27, porcine) is a bombesin-like neuropeptide that can be obtained from porcine spinal cord. Neuromedin C porcine exhibits a potent contractile activity on rat uterus in the characteristic manner of bombesin. Neuromedin C porcine has research potential for neurological-related diseases .
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- HY-W722221
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Adrenergic Receptor
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Cardiovascular Disease
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Colterol acetate is a selective inhibitor of β-adrenergic receptors. Colterol acetate can relax tracheal smooth muscle (primarily acting on β2 receptors), reduce subspastic contractions of tricholoma (acting on β2), and increase contractility of left ventricular papillary muscles (acting on β1) .
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- HY-B1793
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Potassium Channel
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Neurological Disease
Cancer
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Tetraethylammonium chloride is a non-selective potassium channel blocker. Tetraethylammonium chloride is a good substrate for organic cation transporter (OCTN1). Tetraethylammonium chloride antitumor properties .
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- HY-107610
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Leukotriene Receptor
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Inflammation/Immunology
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SR2640 (hydrochloride) is a potent and selective competitive leukotriene D4/leukotriene E4 antagonist. SR2640 can be used for researching the role of leukotrienes in human asthma .
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- HY-B2155
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Cholinesterase (ChE)
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Metabolic Disease
Inflammation/Immunology
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Acotiamide monohydrochloride trihydrate is an orally active, selective and reversible acetylcholinesterase (AChE) inhibitor, with IC50 of 1.79 μM. Acotiamide monohydrochloride trihydrate can enhance gastric contractility and accelerate delayed gastric emptying. Acotiamide monohydrochloride trihydrate has the potential for the research of functional dyspepsia involving gastric motility dysfunction and intestinal inflammatory .
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- HY-P1428A
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Neuropeptide Y Receptor
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Cardiovascular Disease
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RFRP-1(human) TFA is a potent endogenous NPFF receptor agonist (EC50 values are 0.0011 and 29 nM for NPFF2 and NPFF1, respectively). Attenuates contractile function of isolated rat and rabbit cardiac myocytes. Reduces heart rate, stroke volume, ejection fraction and cardiac output, and increases plasma prolactin levels in rats.
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- HY-165045
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DG(15:0/15:0/0:0); 1,2-Dipentadecanoin
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Others
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Others
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1,2-Dipentadecanoyl-rac-glycerol (DG(15:0/15:0/0:0)) is a compound mentioned in the study of the effects of insulin on 1,2-diacylglycerol in rat hearts. Insulin can increase the content of 1,2-diacylglycerol with a specific fatty acid composition in the heart, which may be related to cardiac contractility.
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- HY-B0763
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KC-404; AV-411; MN-166
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Phosphodiesterase (PDE)
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Inflammation/Immunology
Cancer
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Ibudilast (KC-404; AV-411; MN-166) is a cyclic AMP phosphodiesterase (PDE) inhibitor. Ibudilast has platelet anti-aggregatory effects. Ibudilast can be used for the research of asthma for its inhibitory effects on tracheal smooth muscle contractility. Ibudilast may be a useful neuroprotective and anti-dementia agent counteracting neurotoxicity in activated microglia .
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- HY-103209
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Adrenergic Receptor
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Cardiovascular Disease
Endocrinology
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Rec 15/2615 hydrochloride is a potent and selective α-1B adrenoceptor antagonist with Ki values of 1.9 nM, 0.3 nM, 2.6 nM for α1A, α1B, α1D, respectively. Rec 15/2615 hydrochloride modulates vaginal smooth muscle contractility and genital engorgement .
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- HY-16056
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Adrenergic Receptor
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Cardiovascular Disease
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Arbutamine is a short-acting, potent and nonselective β-adrenoceptor agonist. Arbutamine stimulates cardiac β1-, tracheal β2-, and adiopocyte β3- adrenergic receptors. Arbutamine provides cardiac stress increases heart rate, cardiac contractility, and systolic blood pressure. Arbutamine can be used for cardiac stress agent .
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- HY-16056A
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Adrenergic Receptor
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Cardiovascular Disease
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Arbutamine hydrochloride is a short-acting, potent and nonselective β-adrenoceptor agonist. Arbutamine hydrochloride stimulates cardiac β1-, tracheal β2-, and adiopocyte β3- adrenergic receptors. Arbutamine hydrochloride provides cardiac stress increases heart rate, cardiac contractility, and systolic blood pressure. Arbutamine hydrochloride can be used for cardiac stress agent .
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- HY-115381
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Endogenous Metabolite
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Cardiovascular Disease
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Lipoxin A5 is an eicosapentaenoic acid derived from pig white blood cells. Lipoxin A5 slowly contracted the guinea pig lung parenchymal strips with a contractile force similar to that of LXA4 and LXB4.2, but LXA5 did not have the vasodilating effect on the aortic smooth muscle shown by LXA4 and LXB4.2 .
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- HY-118960
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ATP Synthase
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Cardiovascular Disease
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BMS-199264 hydrochloride is an inhibitor of F1F0 ATP hydrolase (IC50=0.5 μM) without inhibitory effect on F1F0 ATP synthase. BMS-199264 hydrochloride selectively inhibits ATP decline during ischemia to reduces cardiac necrosis. BMS-199264 hydrochloride also enhances the recovery of contractile function following reperfusion .
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- HY-103291
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Bradykinin Receptor
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Inflammation/Immunology
Endocrinology
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Sar-[D-Phe8]-des-Arg9-Bradykinin is a agonist of B1 receptor. Sar-[D-Phe8]-des-Arg9-Bradykinin selectively amplifies the contractile response when incubation with human recombinant interleukin-1 β (IL-1 β) in rabbit aortic rings .
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![Sar-[D-Phe8]-des-Arg9-Bradykinin](//file.medchemexpress.eu/product_pic/hy-103291.gif)
- HY-123459
-
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ABT-232; NS-49; PNO-49B
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Others
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Endocrinology
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Garomefrine hydrochlorid (ABT-232) is an α1A-adrenergic agonist with the potential to inhibit urinary incontinence. Garomefrine hydrochlorid showed the greatest contractility in pig nasal mucosal vessels. The biological activity of Garomefrine hydrochlorid has been shown to give it a competitive advantage compared to other drugs. The potency of Garomefrine hydrochlorid makes it a valuable research object in related research .
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- HY-B0763S1
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Isotope-Labeled Compounds
Phosphodiesterase (PDE)
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Inflammation/Immunology
Cancer
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Ibudilast-d7 is the deuterium labeled Ibudilast. Ibudilast (KC-404; AV-411; MN-166) is a cyclic AMP phosphodiesterase (PDE) inhibitor. Ibudilast has platelet anti-aggregatory effects. Ibudilast can be used for the research of asthma for its inhibitory effects on tracheal smooth muscle contractility. Ibudilast may be a useful neuroprotective and anti-dementia agent counteracting neurotoxicity in activated microglia[1].
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- HY-150039
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G Protein-coupled Receptor Kinase (GRK)
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Cardiovascular Disease
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CCG-271423 is a potent and selective GRK5 inhibitor with IC50 values of 0.0021 μM and 44 μM for GRK5 and GRK2, respectively. CCG-271423 inhibits cardiomyocyte contractility and decreases in Ca 2+ transience . CCG-271423 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-A0252A
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Others
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Cancer
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Bupranolol hydrochloride is a non-selective β-adrenergic blocker with potent membrane stabilizing activity. Bupranolol hydrochloride is able to significantly modulate the contractile activity of the non-pregnant human uterus. Bupranolol hydrochloride showed significant effects on spontaneous uterine contractions in an in vitro study in patients with ovarian cancer. Bupranolol hydrochloride is similar in potency to propranolol, another β-adrenergic blocker. Bupranolol hydrochloride is rapidly and completely absorbed in vivo, and its major metabolite is carboxybupranolol .
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- HY-B1116A
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(-)-Metaraminol; (-)-erythro-Metaraminol; (-)-m-Hydroxynorephedrine
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Others
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Neurological Disease
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Metaraminol ((-)-Metaraminol) is a sympathomimetic compound with activity that acts primarily at alpha-1 adrenergic receptors. Metaraminol is used to inhibit hypotension due to vasodilation, particularly in critically ill patients who do not respond well to volume resuscitation. Metaraminol may also be used as an adjunct to help improve cardiac contractility. The use of metaraminol may be supported by less evidence, but its effectiveness in specific situations remains of interest .
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- HY-B0763R
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Phosphodiesterase (PDE)
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Inflammation/Immunology
Cancer
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Ibudilast (Standard) is the analytical standard of Ibudilast. This product is intended for research and analytical applications. Ibudilast (KC-404; AV-411; MN-166) is a cyclic AMP phosphodiesterase (PDE) inhibitor. Ibudilast has platelet anti-aggregatory effects. Ibudilast can be used for the research of asthma for its inhibitory effects on tracheal smooth muscle contractility. Ibudilast may be a useful neuroprotective and anti-dementia agent counteracting neurotoxicity in activated microglia .
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- HY-106761
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Calcium Channel
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Cardiovascular Disease
Others
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Oxodipine, a dihydropyridine-type calcium antagonist, inhibits KCl-induced aortic contraction in rabbits and reduces cardiac force in less potent rat ventricular test-paper contractions. In rat cultured neonatal ventricular myocytes, Oxodipine reduces L-type Ca currents (I) with an IC50 of 0.24 μM, and against T-type Ca currents (I) with an IC50 of 0.41 μM. Oxodipine causes constipation in mice and gingival hyperplasia in dogs .
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- HY-B0763S2
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KC-404-d7-1; AV-411-d7-1; MN-166-d7-1
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Phosphodiesterase (PDE)
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Inflammation/Immunology
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Ibudilast-d7-1 is the deuterium labeled Ibudilast[1]. Ibudilast (KC-404;AV-411;MN-166) is a cyclic AMP phosphodiesterase (PDE) inhibitor. Ibudilast has platelet anti-aggregatory effects. Ibudilast can be used for the research of asthma for its inhibitory effects on tracheal smooth muscle contractility. Ibudilast may be a useful neuroprotective and anti-dementia agent counteracting neurotoxicity in activated microglia[2].
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- HY-B2155R
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Cholinesterase (ChE)
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Metabolic Disease
Inflammation/Immunology
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Acotiamide (monohydrochloride trihydrate) (Standard) is the analytical standard of Acotiamide (monohydrochloride trihydrate). This product is intended for research and analytical applications. Acotiamide monohydrochloride trihydrate is an orally active, selective and reversible acetylcholinesterase (AChE) inhibitor, with IC50 of 1.79 μM. Acotiamide monohydrochloride trihydrate can enhance gastric contractility and accelerate delayed gastric emptying. Acotiamide monohydrochloride trihydrate has the potential for the research of functional dyspepsia involving gastric motility dysfunction and intestinal inflammatory .
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- HY-117181
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Phosphodiesterase (PDE)
Adrenergic Receptor
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Cardiovascular Disease
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UK-1745 is a cardiotonic agent with vasodilating and antiarrhythmic properties. It increases intracellular levels of cyclic adenosine monophosphate (cAMP) in cardiomyocytes by inhibiting phosphodiesterase III, thereby enhancing myocardial contractility. Additionally, UK-1745 exhibits β-adrenergic receptor blocking activity, which helps reduce the oxygen consumption of the heart and prevent calcium overload. These characteristics make UK-1745 a promising candidate for research in congestive heart failure .
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- HY-N2071
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- HY-P4160
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THG113.31; ILGHXDYK
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Prostaglandin Receptor
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Endocrinology
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PDC31 (THG113.31; ILGHXDYK) is an allosteric and non-competitive inhibitor of FP Prostaglandin Receptor. PDC31 is the D-amino acid-based oligopeptide, is used for smooth muscle contractile agent. PDC31 decreases the strength and duration of uterine contractions in vivo, which can be used for research of preterm labor and primary dysmenorrhea (PD). PDC31 also enhances Ca 2+-dependent large-conductance K +-channel in human myometrial cells .
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- HY-19279A
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Others
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Endocrinology
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JTH-601 Free base is a novel alpha1-adrenoceptor antagonist that exhibits potent activity in inhibiting phenylephrine-induced contractions in lower urinary tract tissues. JTH-601 Free base competitively antagonizes alpha1-adrenoceptor-mediated contractile responses, demonstrating greater potency than prazosin or tamsulosin. JTH-601 Free base is anticipated to be effective in treating urinary outlet obstruction associated with benign prostatic hyperplasia.
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- HY-N2071R
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Cytochrome P450
Fungal
Apoptosis
Caspase
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Infection
Neurological Disease
Inflammation/Immunology
Cancer
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Cedrol (Standard) is the analytical standard of Cedrol. This product is intended for research and analytical applications. Cedrol is a potent competitive inhibitor of cytochrome P-450(CYP) enzyme. Cedrol plays an anticancer role by inducing cell cycle arrest and Caspase-dependent apoptosis. Cedrol acts as a neutrophil agonist that can desensitize cells to subsequent stimulation of N-formyl peptides. Cedrol prevents neuropathic pain caused by chronic contractile injury by inhibiting oxidative stress and inflammation. In addition, Cedrol has antibacterial, hair loss prevention and anti-anxiety properties.
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- HY-B0204B
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(-)-UD-CG115
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Others
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Cardiovascular Disease
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(-)-Pimobedan is an isomer of pimobedan. It has the property of stereoselective partitioning or distribution into erythrocytes. The clearance of (-)-pimobedan from erythrocytes is significantly lower than that of (+)-pimobedan, which is entirely due to its stereoselective distribution into erythrocytes. This stereoselective property of (-)-pimobedan may explain the phenomenon previously reported that it produces a 1.5-fold greater contractile force than the (+)-isomer in detergent-treated myocardial specimens of guinea pigs and dogs. These properties suggest that (-)-pimobedan may have unique advantages in terms of in vivo distribution and pharmacological action, which may have important implications for its clinical use.
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- HY-121998
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Aurora Kinase
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Others
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Binucleine 2 is an isoform-specific and ATP-competitive inhibitor of Drosophila Aurora B kinase (Ki=0.36 μM), a kinase involved in cell division. It is specific for Drosophila Aurora B kinase, inhibiting it in a dose-dependent manner, with minimal inhibition of human or X. laevis Aurora B kinases at concentrations up to 100 μM. Binucleine 2 induces mitotic and cytokinesis defects in Drosophila Kc167 cells. It prevents Drosophila S2 cells from assembling a contractile ring during cell division when used at a concentration of 40 μM but does not affect ring ingression, suggesting that Aurora B kinase activity is not required for that step.
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- HY-P2141A
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Angiotensin Receptor
Arrestin
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Cardiovascular Disease
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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 .
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- HY-P2141
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Angiotensin Receptor
Arrestin
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Cardiovascular Disease
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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 .
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- HY-W008820R
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Endogenous Metabolite
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Metabolic Disease
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Glutaric acid (Standard) is the analytical standard of Glutaric acid. This product is intended for research and analytical applications. Glutaric acid, C5 dicarboxylic acid, is an intermediate during the catabolic pathways of lysine and tryptophan. Glutaric acid affects pericyte contractility and migration. Glutaric acid is an indicator of glutaric aciduria type I .
In Vitro: Glutaric acid (GA) at concentrations of 1 and 2 mM is able to reduce TRAP measurement by up to 28% in a dose-dependent manner (β=0.77; P<0.001). Furthermore, a significantly inverse correlation is also verified between chemiluminescence and TRAP (β=0.81; P<0.001). Glutaric acid does not alter the activities of Cat and SOD, but strongly inhibits (up to 46%) the activity of GPx even at the lower concentration used (0.5 mM). It is observed that the metabolite inhibits this activity in a dose-dependent manner at concentrations as low as 0.05 mM .
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Product Name |
Target |
Research Area |
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- HY-P3618
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Somatostatin Receptor
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Neurological Disease
Inflammation/Immunology
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Cortistatin-29 is a neuropeptide. Cortistatin-29 alleviates neuropathic pain. Cortistatin-29 binds all somatostatin (SS) receptor subtypes with high affinity and shows IC50 values of 2.8 nM, 7.1 nM, 0.2 nM, 3.0 nM, 13.7 nM for SSTR1, SSTR2, SSTR3, SSTR4, SSTR5, respectively. Cortistatin-29 shows anti-fibrotic effects .
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- HY-W016733
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H-D-Cit-OH
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Endogenous Metabolite
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Cardiovascular Disease
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D-Citrulline (H-D-Cit-OH) is a stereoisomer of L-citrulline (HY-N0391). D-Citrulline significantly attenuates polymorphonuclear leukocyte (PMN)-induced cardiac contractile dysfunction in the isolated perfused rat heart subjected to ischemia/reperfusion via a non-NO-mediated mechanism .
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- HY-P10655
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Proton Pump
Calcium Channel
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Cardiovascular Disease
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Caloxin 1C2 is a specific PMCA (plasma-membrane Ca 2+-ATPases) inhibitor. Caloxin 1C2 is selective for PMCA4 over PMCA1, 2 and 3. The Ki values of Caloxin 1C2 are 2.3 μM for PMCA4 and 21 μM for PMCA1. Caloxin 1C2 dose not cause any significant effects on total Ca 2+ transfer. Caloxin 1C2 affects coronary contractility .
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- HY-P3591
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- HY-P1721
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Bradykinin Receptor
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Cardiovascular Disease
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NPC 17731 is a new bradykinin (BK) receptor antagonist. NPC 17731 antagonized both the contractile and relaxant responses caused by BK in longitudinal smooth muscle with IC50 of 23 and 29 nM, respectively .
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- HY-P10528
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Peptides
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Others
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Echinotocin is a neuropeptide found in sea urchins that has muscle contractile activity. Echinotocin can cause contractions of the tube feet and esophagus of sea urchins. Echinotocin can be used to study the role of neuropeptides in invertebrate physiology and behavior .
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- HY-P3853
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Neurokinin Receptor
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Neurological Disease
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GR 87389 is a potent NK2 receptor antagonist. GR 87389 antagonized GA 64349-induced smooth muscle strips contractions in a competitive manner in the human detrusor, prostate and prostatic urethra .
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- HY-P4678
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Vasopressin Receptor
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Neurological Disease
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(Phe2,Orn8)-Oxytocin is a selective V1 vasopressin agonist. (Phe2,Orn8)-Oxytocin induces a sustained contractility of rabbit epididymis with EC50 value of 280 nM .
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- HY-P4678A
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Vasopressin Receptor
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Neurological Disease
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(Phe2,Orn8)-Oxytocin acetate is a selective V1 vasopressin agonist. (Phe2,Orn8)-Oxytocin acetate induces a sustained contractility of rabbit epididymis with EC50 value of 280 nM .
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- HY-P2150
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Somatostatin Receptor
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Neurological Disease
Inflammation/Immunology
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Cortistatin-29 is a neuropeptide. Cortistatin-29 alleviates neuropathic pain. Cortistatin-29 binds all somatostatin (SS) receptor subtypes with high affinity and shows IC50 values of 2.8 nM, 7.1 nM, 0.2 nM, 3.0 nM, 13.7 nM for SSTR1, SSTR2, SSTR3, SSTR4, SSTR5, respectively. Cortistatin-29 shows anti-fibrotic effects .
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- HY-103283
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GRP(18-27) (porcine)
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Biochemical Assay Reagents
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Neurological Disease
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Neuromedin C porcine (GRP, 18-27, porcine) is a bombesin-like neuropeptide that can be obtained from porcine spinal cord. Neuromedin C porcine exhibits a potent contractile activity on rat uterus in the characteristic manner of bombesin. Neuromedin C porcine has research potential for neurological-related diseases .
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- HY-P1428A
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Neuropeptide Y Receptor
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Cardiovascular Disease
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RFRP-1(human) TFA is a potent endogenous NPFF receptor agonist (EC50 values are 0.0011 and 29 nM for NPFF2 and NPFF1, respectively). Attenuates contractile function of isolated rat and rabbit cardiac myocytes. Reduces heart rate, stroke volume, ejection fraction and cardiac output, and increases plasma prolactin levels in rats.
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- HY-103291
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Bradykinin Receptor
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Inflammation/Immunology
Endocrinology
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Sar-[D-Phe8]-des-Arg9-Bradykinin is a agonist of B1 receptor. Sar-[D-Phe8]-des-Arg9-Bradykinin selectively amplifies the contractile response when incubation with human recombinant interleukin-1 β (IL-1 β) in rabbit aortic rings .
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- HY-P0084
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SRIF-14; Somatostatin-14
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Peptides
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Cardiovascular Disease
Neurological Disease
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Cyclic somatostatin (SRIF-14) is a growth hormone-release inhibiting factor used in the research of severe, acute hemorrhages of gastroduodenal ulcers. Cyclic somatostatin is a neuropeptide co-stored with acetylcholine in the cardiac parasympathetic innervation, exerts influences directly on contraction of ventricular cardiomyocytes. Cyclic somatostatin inhibits the contractile response of isoprenaline with an IC50 value of 13 nM. Cyclic somatostatin can be used for the research of cardiovascular disease .
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- HY-P4160
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THG113.31; ILGHXDYK
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Prostaglandin Receptor
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Endocrinology
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PDC31 (THG113.31; ILGHXDYK) is an allosteric and non-competitive inhibitor of FP Prostaglandin Receptor. PDC31 is the D-amino acid-based oligopeptide, is used for smooth muscle contractile agent. PDC31 decreases the strength and duration of uterine contractions in vivo, which can be used for research of preterm labor and primary dysmenorrhea (PD). PDC31 also enhances Ca 2+-dependent large-conductance K +-channel in human myometrial cells .
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- HY-P2601A
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Peptides
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Others
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Tyr-α-CGRP (human) TFA is an N-terminally extended human α-CGRP analog. Tyr-α-CGRP (human) TFA can bind to membrane preparations from rat brain and spleen with IC50 values of 0.2 nM and 0.5 nM, respectively, and induce positive chronotropic and inotropic effects in isolated guinea pig right and left atria with EC50 values of 282 nM and 74 nM, respectively. Tyr-α-CGRP (human) TFA also inhibits contractile responses in rat vas deferens with an EC50 value of 1.9 nM .
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- HY-P2141A
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Angiotensin Receptor
Arrestin
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Cardiovascular Disease
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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 .
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- HY-P2141
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Angiotensin Receptor
Arrestin
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Cardiovascular Disease
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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 .
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
| Cat. No. |
Product Name |
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Classification |
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- HY-150039
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Alkynes
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CCG-271423 is a potent and selective GRK5 inhibitor with IC50 values of 0.0021 μM and 44 μM for GRK5 and GRK2, respectively. CCG-271423 inhibits cardiomyocyte contractility and decreases in Ca 2+ transience . CCG-271423 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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![Sar-[D-Phe8]-des-Arg9-Bradykinin](http://file.medchemexpress.eu/product_pic/hy-103291.gif)
