PF 05089771 tosylate

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本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1430806-04-4

PF 05089771 tosylate 是有效的、具有口服活性的、选择性的Na_v1.7丙烯酰胺抑制剂，其对 hNa_v1.7、cynNa_v1.7、dogNa_v1.7、ratNa_v1.7 和 musNa_v1.7 的IC₅₀值分别为11 nM、12 nM、13 nM、171 nM 和 8 nM。PF 05089771 目前正用于疼痛和糖尿病神经性疾病的研究。

生物活性

PF 05089771 tosylate is a potent, orally active and selective arylsulfonamideNa_v1.7inhibitor, withIC₅₀values of 11 nM, 12 nM, 13 nM, 171 nM and 8 nM for hNa_v1.7, cynNa_v1.7, dogNa_v1.7, ratNa_v1.7, and musNa_v1.7, respectively. PF 05089771 is under the study for pain and diabetic neuropathy^[1]^[2].

IC₅₀& Target

IC50: 11 nM (hNa_v1.7), 12 nM (cynNa_v1.7), 13 nM (dogNa_v1.7), 171 nM (ratNa_v1.7), 8 nM (musNa_v1.7)^[1]^[2].

体外研究
(In Vitro)

PF-05089771 is determined to be more than 1000-fold selective over tetrodotoxin-resistant (TTX-R) Na_v1.5 and Na_v1.8 channels (IC₅₀s >10 μM) and exhibited a range of selectivity over TTX-sensitive (TTX-S) channels (10-fold for Na_v1.2 to 900-fold for Na_v1.3 and Na_v1.4)^[1].
PF-05089771 (30 nM) blocks the majority of TTX-S current (75.5 ± 10.5%, n = 5) whilst 100 nM resulted in complete block^[1].

Clinical Trial

分子量

672.56

Formula

C₂₅H₂₀Cl₂FN₅O₆S₃

CAS 号

1430806-04-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.