2. Membrane Transporter/Ion Channel
  3. Sodium Channel
  4. PF 05089771 tosylate

PF 05089771 tosylate 是有效的、具有口服活性的、选择性的 Nav1.7 丙烯酰胺抑制剂，其对 hNav1.7、cynNav1.7、dogNav1.7、ratNav1.7 和 musNav1.7 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。

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PF 05089771 tosylate Chemical Structure

PF 05089771 tosylate Chemical Structure

CAS No. : 1430806-04-4

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PF 05089771 tosylate 的其他形式现货产品:

Customer Review

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PF 05089771 tosylate 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PF 05089771 tosylate is a potent, orally active and selective arylsulfonamide Nav1.7 inhibitor, with IC50 values of 11 nM, 12 nM, 13 nM, 171 nM and 8 nM for hNav1.7, cynNav1.7, dogNav1.7, ratNav1.7, and musNav1.7, respectively. PF 05089771 is under the study for pain and diabetic neuropathy[1][2].

IC50 & Target

IC50: 11 nM (hNav1.7), 12 nM (cynNav1.7), 13 nM (dogNav1.7), 171 nM (ratNav1.7), 8 nM (musNav1.7)[1][2].
体外研究
(In Vitro)

PF-05089771 is determined to be more than 1000-fold selective over tetrodotoxin-resistant (TTX-R) Nav1.5 and Nav1.8 channels (IC50s >10 μM) and exhibited a range of selectivity over TTX-sensitive (TTX-S) channels (10-fold for Nav1.2 to 900-fold for Nav1.3 and Nav1.4)[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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

PF 05089771 tosylate 相关抗体:
Clinical Trial
分子量

672.56

Formula

C25H20Cl2FN5O6S3
CAS 号
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.
纯度 & 产品资料
参考文献

PF 05089771 tosylate 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

PF 050897711430806-04-4PF05089771PF-05089771Sodium ChannelNa channelsNa+ channelspaindiabeticneuropathytetrodotoxinTTX-RInhibitorinhibitorinhibit

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