| Identification | Back Directory | [Name]
VU0810464 | [CAS]
2126040-21-7 | [Synonyms]
VU0810464
Benzeneacetamide, 3-chloro-N-(1-cyclohexyl-3-methyl-1H-pyrazol-5-yl)-4-fluoro- | [Molecular Formula]
C18H21ClFN3O | [MDL Number]
MFCD32689471 | [MOL File]
2126040-21-7.mol | [Molecular Weight]
349.83 |
| Chemical Properties | Back Directory | [Boiling point ]
549.1±50.0 °C(Predicted) | [density ]
1.31±0.1 g/cm3(Predicted) | [storage temp. ]
Sealed in dry,2-8°C | [solubility ]
DMSO: ≥ 250 mg/mL (714.63 mM) | [form ]
Solid | [pka]
13.35±0.70(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
VU0810464 is a potent and selective non-ureaG protein-gated inwardly-rectifying potassium channels (GIRK, Kir3) activator. VU0810464 displays nanomolar potency for neuronal (EC50=165 nM) and GIRK1/4 (EC50=720 nM) channels with improved brain penetration[1][2]. | [in vivo]
VU0810464 (intraperitoneal?injection; 30 mg/kg, 10 mg/kg; 30mg/kg; pre-treated 30 mins) produces a dose-dependent reduction of SIH response in Male C57BL/6J mice. To test if VU0810464 plays it role through Kir3 channel activation, VU0810464 (10 mg/kg) suppresses the SIH response in wild‐ type mice, but has no impact on Kcnj3?/? mice[2].
VU0810464 (intraperitoneal?injection?; 30 mg/kg; 15, 30, 45, or 60 min post‐injection) displays a favourable distribution to the brain (Kp,uu = 0.83), has a improvement over ML297 (Kp,uu= 0.32). Clearance of VU0810464 is rapid,brain and plasma half-lives is 20 min in a PK study[2]. | Animal Model: | Male C57BL/6J mice, Kcnj3?/? siblings female and male C57BL/6J mice | | Dosage: | 10 mg/kg; 30mg/kg | | Administration: | Intraperitoneal?injection | | Result: | Reduced stress‐induced hyperthermia (SIH), a physiological test of
anxiolytic efficacy in wild mice, but had no impact in and Kcnj3 (Girk1) ?/? mice.
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| [References]
[1] Vo BN, et al. VU0810464, a non-urea G protein-gated inwardly rectifying K+?(Kir?3/GIRK) channel activator, exhibits enhanced selectivity for neuronal Kir?3 channels and reduces stress-induced hyperthermia in mice.Br J Pharmacol.?2019 Jul;176(13):2238-2249. DOI:10.1111/bph.14671
[2] Wieting JM,et al. Discovery and Characterization of 1H-Pyrazol-5-yl-2-phenylacetamides as Novel, Non-Urea-Containing GIRK1/2 Potassium Channel Activators.ACS Chem Neurosci.?2017?Sep 20;8(9):1873-1879. DOI:10.1021/acschemneuro.7b00217 |
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| Company Name: |
cjbscvictory
|
| Tel: |
13348960310 |
| Website: |
https://www.weikeqi-biotech.com/ |
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