PF 05089771

An Nav1.7 channel blocker

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库存: 现货

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数量
5mg

￥2012.00

1610.00

- +
25mg

￥4250.00

3400.00

- +
100mg

￥10412.00

8330.00

- +

已选 0 种 0 瓶

金额: ￥0.00

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Background

PF-05089771 is a voltage-gated sodium channel 1.7 (Na_v1.7) blocker (IC₅₀s = 11, 16, 33, and 20 nM for 5N11S, 5A11L, 5A11S, and 5A11L Na_v1.7 splice variants, respectively).¹ It is selective for Na_v1.7 over Na_v1.1-1.6 and 1.8 channels (IC₅₀s = 0.11-25 μM), L-type calcium, and K_vLQT and hERG potassium channels (IC₅₀s = ≥10 μM), as well as human and cynomolgus monkey TRPV1 receptors (IC₅₀s = 10 and 20 μM, respectively). PF-05089771 is also 1,000-fold selective for half-inactivated over resting Na_v1.7 channels, and mutation of the domain IV voltage-sensor domain (VSD4) reduces PF-05089771 potency by approximately 100-fold.

1.Alexandrou, A.J., Brown, A.R., Chapman, M.L., et al.Subtype-selective small molecule inhibitors reveal a fundamental role for Nav1.7 in nociceptor electrogenesis, axonal conduction and presynaptic releasePLoS One11(4)e0152405(2016)