1. GPCR/G Protein
  2. P2Y Receptor
  3. P2Y14R antagonist 2

P2Y14R antagonist 2 (compound 39) 是一种有效且选择性的,具有口服活性的 P2Y14R 拮抗剂,其 IC50 值为 0.40 nM。P2Y14R antagonist 2 具有抗炎活性。P2Y14R antagonist 2 具有用于研究结肠炎的潜力。

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P2Y14R antagonist 2 Chemical Structure

P2Y14R antagonist 2 Chemical Structure

CAS No. : 2989271-65-8

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

P2Y14R antagonist 2 (compound 39) is a potent, selective and orally active P2Y14R antagonist with an IC50 value of 0.40 nM. P2Y14R antagonist 2 shows anti-inflammatory activity. P2Y14R antagonist 2 has the potential for the research of colitis[1].

IC50 & Target[1]

P2Y14 Receptor

0.40 nM (IC50)

体内研究
(In Vivo)

P2Y14R antagonist 2 (50, 100 µM for 100µL per mice; rectally administered, daily for 7 days) 对患有结肠炎的小鼠表现出抗炎活性[1]
药代动力学分析[1].

Parameters dose (mg/kg) Cmax (ng/mL) T1/2 (min) Tmax (min) AUCall (min*ng/mL) CL (mL/min/kg) F (%)
iv 1.0 - 21 ± 8.4 - 27924 ± 5520 133.8 ± 33 -
po 5.0 518.25 ± 196.26 177.6 ± 24.6 15 90744 ± 21613 232.2 ± 46.2 65.0

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

Animal Model: 6-8 weeks, 20-22 g, male C57BL/6 mice (colitis) [1]
Dosage: 50, 100 µM for 100µL per mice
Administration: Rectally administered, daily for 7 days
Result: Alleviated DSS-induced body weight loss, loose stools, rectal bleeding, colon shortening, and elevated spleen weighted index.
分子量

372.37

Formula

C18H13FN2O4S

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

P2Y14R antagonist 2 相关分类

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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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