2. GPCR/G Protein
  3. GHSR
  4. PF-6870961

PF-6870961 是 GHSR1a 的反向激动剂，Ki 值分别为 73.6 nM（人 GHSR）、239 nM（大鼠 GHSR）和 217 nM（狗 GHSR）。PF-6870961 抑制组成型 GHSR1a 诱导的 IP 积累，IC50 值为 300 nM。 PF-6870961 还抑制组成型 GHSR1a β-arrestin 动员，IC50 值为 1.10 nM。

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PF-6870961 Chemical Structure

PF-6870961 Chemical Structure

CAS No. : 2857112-06-0

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PF-6870961 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-6870961 is an inverse agonist of GHSR1a with Ki values of 73.6 nM (human GHSR), 239 nM (rat GHSR), and 217 nM (dog GHSR), respectively. PF-6870961 inhibits the constitutive GHSR1a-induced IP accumulation with an IC50 value of 300 nM. PF-6870961 also inhibits constitutive GHSR1a β-arrestin mobilization with an IC50 value of 1.10 nM[1].

体内研究
(In Vivo)

PF-6870961 (40 mg/kg; i.p.) suppresses food intake in both satiated and fasted rats[1].

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

Animal Model: Satiated and fasted rats model[1]
Dosage: 2.5 mg/kg, 10 mg/kg, and 40 mg/kg
Administration: Intraperitoneal injection
Result: Significantly reduced food intake at 40 mg/kg.
分子量

528.67

Formula

C29H32N6O2S
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-6870961 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

PF-68709612857112-06-0PF6870961PF 6870961GHSRGrowth hormone secretagogue receptorGhrelin receptorInhibitorinhibitorinhibit

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目录号：
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