ASIC1a inhibitor 5b

Modify Date: 2023-01-16 13:38:48

ASIC1a inhibitor 5b Structure
ASIC1a inhibitor 5b structure
Common Name ASIC1a inhibitor 5b
CAS Number 1787243-08-6 Molecular Weight 499.861
Density N/A Boiling Point N/A
Molecular Formula C23H29Cl3N4O2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of ASIC1a inhibitor 5b


ASIC1a inhibitor 5b is a highly selective and potent ASIC1a inhibitor, inhibits proton-evoked ASIC1a currents with an apparent IC50 of 27 nM at pH 6.7.ASIC1a inhibitor 5b can potently and selectively inhibit acid-induced activation of ASIC1a-containing channels, including both ASIC1a homotrimers and ASIC1a-ASIC2 heterotrimers, in a pH-dependent manner.ASIC1a inhibitor 5b binds to the acidic pocket of ASIC1a, exhibits a dramatic leftward shift under pH 6.7 activation of ASIC1a as compared to pH 6.0.ASIC1a inhibitor 5b protected neurons from ASIC1a-dependent cell death and is blood-brain barrier permeable.ASIC1a inhibitor 5b (5 mg/kg) attenuated neurological impairment and alleviated infarct volume in mouse MCAO model of ischemic stroke.

 Names

Name ASIC1a inhibitor 5b

 ASIC1a inhibitor 5b Biological Activity

Description ASIC1a inhibitor 5b is a highly selective and potent ASIC1a inhibitor, inhibits proton-evoked ASIC1a currents with an apparent IC50 of 27 nM at pH 6.7.ASIC1a inhibitor 5b can potently and selectively inhibit acid-induced activation of ASIC1a-containing channels, including both ASIC1a homotrimers and ASIC1a-ASIC2 heterotrimers, in a pH-dependent manner.ASIC1a inhibitor 5b binds to the acidic pocket of ASIC1a, exhibits a dramatic leftward shift under pH 6.7 activation of ASIC1a as compared to pH 6.0.ASIC1a inhibitor 5b protected neurons from ASIC1a-dependent cell death and is blood-brain barrier permeable.ASIC1a inhibitor 5b (5 mg/kg) attenuated neurological impairment and alleviated infarct volume in mouse MCAO model of ischemic stroke.
References 1. Xin Qi, et al. Front Pharmacol. 2022 Mar 24;13:849498. 2. Andriy Buta, et al. J Med Chem. 2015 Jun 11;58(11):4449-61.

 Chemical & Physical Properties

Molecular Formula C23H29Cl3N4O2
Molecular Weight 499.861