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编 号:F140593
分子式:C23H21F3N4O4
分子量:474.43
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生物活性:
AZD-3161 is a potent and selective blocker of NaV1.7 channel, with a pIC50 of 7.1. AZD-3161 can be used for the research of neuropathic and inflammatory pain.

体内研究:
AZD-3161 (16-99 μmol/kg; p.o.) displays a dose dependent antinociceptive effect in the phase 1 of the formalin model of pain in rats.AZD-3161 (3 μmol/kg; i.v.) exhibits long half-life (2.2 h) and Vss (4.2 L/kg).AZD-3161 (10 μmol/kg; p.o.) exhibits high oral bioavailability (44%), long half-life (4.8 h) and Cmax (0.30 μmol/L).

体外研究:
AZD-3161 (compound 29) is selective for NaV1.7 over NaV1.5 and hERG, with pIC50s of 7.1, 4.9 and 4.9, respectively.AZD-3161 inhibits Adenosine Transporter (AT) and Cannabinoid B1 (CB1) receptor, with IC50s of 1.8 μM and 5 μM, respectively.
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