1. GPCR/G Protein Neuronal Signaling
  2. 5-HT Receptor
  3. EGIS-7625 free base

EGIS-7625 free base 是一种具有口服活性和选择性 5-HT2B 受体竞争性拮抗剂,对人源 Ki 为 1 nM。 EGIS-7625 free base 对 5-HT2A 和 5-HT2C 受体的亲和力较低。EGIS-7625 free base 对人源 5-HT2B、5-HT2A 和 5-HT2C 的 pKi 分别为 9.0、6.2 和 7.7。EGIS-7625 free base 可缓解 mCPP 诱导的运动减退。

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EGIS-7625 free base

EGIS-7625 free base Chemical Structure

CAS No. : 751462-86-9

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Other Forms of EGIS-7625 free base:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

EGIS-7625 free base is an orally active and selective competitive antagonist of 5-HT2B receptor, with a human Ki value of 1 nM. EGIS-7625 free base shows low affinity for 5-HT2A and 5-HT2C receptors. The pKi values of EGIS-7625 free base for human 5-HT2B, 5-HT2A and 5-HT2C are 9.0, 6.2 and 7.7, respectively. EGIS-7625 free base alleviates mCPP-induced hypoactivity[1].

体外研究
(In Vitro)

EGIS-7625 (1-10 nM) free base 是大鼠胃底条中 5-HT2B 受体介导收缩的强效竞争性拮抗剂,其 pA2 值为 9.4[1]
EGIS-7625 (1-30 μM; 30 minutes) free base可作为兔肺动脉条中 5-HT2A 受体介导收缩的弱竞争性拮抗剂,其 pA2 值为 6.7[1]

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

体内研究
(In Vivo)

EGIS-7625 (30 mg/kg;皮下注射;单次给药) free base 不会拮抗大鼠中 mCPP 诱导的 5-HT2C 受体介导的摄食抑制[1]
EGIS-7625 (3-30 mg/kg;口服;单次给药) free base 在 30.0 mg/kg 最高剂量下可拮抗大鼠中 mCPP 诱导的 5-HT2C 受体介导的运动减退,而较低剂量无显著作用[1]

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

Animal Model: Wistar (male, 180-240 g)[1]
Dosage: 3, 10, 30 mg/kg
Administration: p.o.; single dose
Result: Significantly diminished mCPP-induced hypomotility at 30 mg/kg p.o.
Did not produce a significant effect at 3.0 mg/kg and 10.0 mg/kg p.o.
分子量

326.39

Formula

C18H22N4O2

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
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  • 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.

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产品名称:
EGIS-7625 free base
目录号:
HY-123480A
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