ASIC1a inhibitor 5b
Modify Date: 2023-01-16 13:38:48
ASIC1a inhibitor 5b structure
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Common Name | ASIC1a inhibitor 5b | ||
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| 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 5bASIC1a 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. |
| Name | ASIC1a inhibitor 5b |
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| 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. |
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| 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. |
| Molecular Formula | C23H29Cl3N4O2 |
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| Molecular Weight | 499.861 |