Chemical Structure : KR-36996
CAS No.:
1816268-07-1
KR-36996
(KR36996)
Catalog No.: PC-28262Not For Human Use, Lab Use Only.
KR-36996 is a potent, selective urotensin II receptor (UTR, U-II receptor, GPR14) antagonist with Ki of 4.44 nM.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
KR-36996 is a potent, selective urotensin II receptor (UTR, U-II receptor, GPR14) antagonist with Ki of 4.44 nM.
KR-36996 significantly inhibits urotensin II-induced stress fiber formation and cellular hypertrophy in H9c2UT cells.
KR-36996 inhibits UII (50 nM) induced proliferation in primary human aortic SMCs (HASMCs) with IC50 of 3.5 nM.
KR-36996 inhibits UII-induced phosphorylation level of ERK1/2, also reduces UII-induced ROS generation
KR-36996 (30 mg/kg, daily oral administration) for 14 days significantly decreased left ventricular weight by 40% (P<0.05) in transverse aortic constriction-induced cardiac hypertrophy model in mice.
KR-36996 decreased interstitial fibrosis and cardiomyocyte hypertrophy in the infarct border zone.
Physicochemical Properties
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M.Wt
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528.51
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Formula
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C26H30BrN3O2S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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N-(1-(3-bromo-4-(piperidin-4-yloxy)benzyl)piperidin-4-yl)benzo[b]thiophene-3-carboxamide
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References
1. Oh KS, et al. Eur J Pharmacol. 2017 Mar 15;799:94-102.
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