1787243-08-6
1787243-08-6 structure
- Name: ASIC1a inhibitor 5b
- Chemical Name: ASIC1a inhibitor 5b
- CAS Number: 1787243-08-6
- Molecular Formula: C23H29Cl3N4O2
- Molecular Weight: 499.861
- Create Date: 2022-07-01 15:04:22
- Modify Date: 2023-01-16 13:38:48
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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.
| Name | ASIC1a inhibitor 5b |
|---|
| 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. |
| Molecular Formula | C23H29Cl3N4O2 |
|---|---|
| Molecular Weight | 499.861 |