1. GPCR/G Protein Neuronal Signaling
  2. CGRP Receptor
  3. CGRP antagonist 7

CGRP antagonist 7 是一种有效的降钙素基因相关肽受体 (CGRP) 拮抗剂,其 Ki 值为 0.029 nM。CGRP antagonist 7 可抑制 CGRP 受体介导的环磷酸腺苷 (cAMP) 产生,其 IC50 值为 1.5 nM。CGRP antagonist 7 可用于偏头痛的研究。

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CGRP antagonist 7

CGRP antagonist 7 Chemical Structure

CAS No. : 2173508-07-9

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  • 生物活性

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生物活性

CGRP antagonist 7 is a potent calcitonin gene-related peptide receptor (CGRP) antagonist with a Ki of 0.029 nM. CGRP antagonist 7 Inhibit the production of cyclic adenosine monophosphate (cAMP) with an IC50 of 1.5 nM. CGRP antagonist 7 can be used for the study of migraine[1].

体外研究
(In Vitro)

CGRP antagonist 7 (Compound 15) (0.1-10 μM, 0-60 min) 在人类肝细胞癌 (HepaRG) 细胞中的 IC50 值超过 100 μM,并且对 CYP3A 有中等程度的抑制作用 (IC50 = 6.6 μM)[1]

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

体内研究
(In Vivo)

CGRP antagonist 7 (Compound 15) (1 mg/kg, i,p., 单次给药) 在 CGRP 诱导的狨猴面部血流模型中显著抑制血流增加[1]

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

Animal Model: Marmoset facial blood flow mode induced by intravenous administration of hαCGRP at a dose of 10 μg/kg administered at −15, 15, 45, and 90 min[1]
Dosage: 1 mg/kg
Administration: Intraperitoneal injection (i.p.), single dose
Result: Significantly inhibited the increase in facial blood flow induced by CGRP (Emax = 84% at 45 min).
分子量

529.61

Formula

C30H32FN5O3

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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CGRP antagonist 7
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HY-174986
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