1. GPCR/G Protein
  2. Prostaglandin Receptor
  3. ACT-774312

ACT-774312 是一种强效的、选择性的 CRTH2 拮抗剂,其 IC50 为 4 nM。ACT-774312 可阻断 CRTH2 受体的活性与内化过程,并抑制 PGD2 诱导的嗜酸性粒细胞形态改变。ACT-774312 可用于鼻息肉以及 2 型炎症性疾病的研究。

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ACT-774312

ACT-774312 Chemical Structure

CAS No. : 1809863-68-0

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查看 Prostaglandin Receptor 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ACT-774312 is a potent and selective CRTH2 antagonist with an IC50 of 4 nM. ACT-774312 blocks the activity and internalization of the CRTH2 receptor, and inhibits PGD2-induced morphological changes in eosinophils. ACT-774312 can be used in the research of nasal polyps and type 2 inflammatory diseases.[1][2]

体外研究
(In Vitro)

ACT-774312 可在含 50% 人血浆的条件下强效抑制 PGD2 诱导的嗜酸性粒细胞形态改变,其 IC50 为 3 nM[1][2]

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

药代动力学
(Parmacokinetics)
Species Dose Route AUC0-∞ CL Vss T1/2 Cmax Tmax F
Rat[1] 1 mg/kg i.v. 4.05 μg·h/mL 4.1 0.45 L/kg 3.2 h / / /
Rat[1] 2 mg/kg p.o. 8.43 μg·h/mL / / / 1.29 μg/mL 0.3 h 104 %
Dog[1] 1 mg/kg i.v. 9.24 μg·h/mL 1.8 0.45 L/kg 5.7 h / / /
Dog[1] 2 mg/kg p.o. 7.24 μg·h/mL / / / 2.41 μg/mL 1 h 78 %
分子量

389.81

Formula

C18H17ClFN5O2

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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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.

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产品名称:
ACT-774312
目录号:
HY-182637
需求量: