2. Neuronal Signaling
  3. Sigma Receptor
  4. PW507

PW507 是一种强效、可透过血脑屏障的和选择性的 sigma 1 受体 (S1R) 拮抗剂，对人类 S1R 的 Ki 为 7.5 nM。PW507 对 S2R 和 hERG 的结合亲和力较低。PW507 可用于研究糖尿病疼痛性神经病变 (PDN)。

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PW507 Chemical Structure

PW507 Chemical Structure

CAS No. : 2573850-59-4

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PW507 相关抗体

Top Publications Citing Use of Products

查看 Sigma Receptor 亚型特异性产品:

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Sigma 1 Receptor Sigma 2 Receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PW507 is a potent, brain-penetrant and selective sigma 1 receptor (S1R) antagonist with a Ki of 7.5 nM for human S1R. PW507 displays a low binding affinity to S2R and hERG. PW507 can be used for the study of painful diabetic neuropathy (PDN)[1].

体外研究
(In Vitro)

PW507 与人类 S1R 晶体结构的正构位点结合，并与受体发生强烈相互作用[1]。

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

PW507 相关抗体:
体内研究
(In Vivo)

PW507（20 mg/kg；腹腔注射；每日两次；持续 14 天）在缓解机械性痛觉过敏方面表现出显著疗效[1]。
PW507 在 SD 大鼠中的药代动力学特性研究[1]。
1.19

plasma PK IV PO IP
dose (mg/kg) 1 25 10
tmax (h) N/A 1.20 0.25
t1/2 (h) 0.53 0.69 0.56
Cmax (ng/mL) 193 296 671
AUC0-inf (h*ng/mL) 108 692 552
CL (mL/min/kg) 155 N/A N/A
ratio (brain/plasma, t = 0.25 h) N/A N/A 12
F (%) 100 28 51

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

Animal Model: Male SD rats injected Streptozotocin (HY-13753; STZ; 60 mg/kg)[1]
Dosage: 20 mg/kg
Administration: i.p; twice daily; for 14 days
Result: Demonstrated significant efficacy in alleviating mechanical allodynia hyperalgesia.
分子量

334.89

Formula

C18H27ClN4
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

PW507 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PW5072573850-59-4PW 507PW-507Sigma ReceptorS1R antagonistpainful diabetic neuropathybrain-penetrantInhibitorinhibitorinhibit

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目录号：
HY-161873
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