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Chemical Structure : VU0810464
CAS No.: 2126040-21-7
Catalog No.: PC-36154Not For Human Use, Lab Use Only.
VU0810464 (VU 0810464, VU464) is a selective neuronal GIRK channels activator, displays nanomolar potency for GIRK1/2 (EC50=163 nM) and improved brain penetration.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $198 | In stock | |
| 10 mg | $298 | In stock | |
| 25 mg | $498 | In stock | |
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| 100 mg | Get quote |
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VU0810464 (VU 0810464, VU464) is a selective neuronal GIRK channels activator, displays nanomolar potency for GIRK1/2 (EC50=163 nM) and improved brain penetration.
VU0810464 exhibits comparable efficacy and potency compared with ML297, but VU0810464 is more selective for neuronal GIRK channels (GIRK1/4 EC50>500 nM).
VU0810464 displays >3-fold more potent on GIRK1/2-expressing HEK293 cells compared to GIRK1/4-expressing cells, as measured using a Tl+ flux assay.
VU0810464 reduced stress-induced hyperthermia in a GIRK-dependent manner in mice, ML297, but not VU0810464, decreased anxiety-related behavior as assessed with the elevated plus maze test.
| M.Wt | 349.834 | |
| Formula | C18H21ClFN3O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
2-(3-chloro-4-fluorophenyl)-N-(1-cyclohexyl-3-methyl-1H-pyrazol-5-yl)acetamide |
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1. Vo BN, et al. Br J Pharmacol. 2019 Mar 29. doi: 10.1111/bph.14671.
2. Wieting JM, et al. ACS Chem Neurosci. 2017 Sep 20;8(9):1873-1879.
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