2. GPCR/G Protein Immunology/Inflammation
  3. Prostaglandin Receptor Interleukin Related
  4. AGN 225660

AGN 225660 是一种多前列腺素受体拮抗剂，对人类 EP1、EP4、TP、DP1、FP 的 IC50 值分别为 70、70、5、220 和 180 nM。AGN 225660 可抑制 RANTES、IL-8、MCP-1、IL-12p70 和 IL-23 的分泌。AGN 225660 具有良好的眼部生物利用度，可减轻与超声乳化白内障吸除术及葡萄膜炎相关的眼部炎症。

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AGN 225660

AGN 225660 Chemical Structure

CAS No. : 1354060-46-0

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AGN 225660 相关抗体

Top Publications Citing Use of Products

查看 Prostaglandin Receptor 亚型特异性产品:

查看所有亚型
DP EP FP IP TXA2/TP TXB2

查看 Interleukin Related 亚型特异性产品:

查看所有亚型
IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AGN 225660 is a multi-prostanoid receptor antagonist with human IC50 values of 70, 70, 5, 220 and 180 nM for EP1, EP4, TP, DP1, FP. AGN 225660 inhibits secretion of RANTES, IL-8, MCP-1, IL-12p70, and IL-23. AGN 225660 exhibits good ocular bioavailability and reduces ocular inflammation linked to phacoemulsification surgery and uveitis[1].

IC50 & Target[1]

TP

5 nM (IC50)

EP1

70 nM (IC50)

EP4

70 nM (IC50)

FP

180 nM (IC50)

DP1

220 nM (IC50)

IL-8

 

IL-12

 

IL-23

 

体外研究
(In Vitro)

AGN 225660 可强效拮抗促炎性人重组前列腺素受体 (EP1、EP4、TP、DP1、FP)，在 HEK-293 转染细胞中其 IC50 值为 5 至 220 nM；而其在抗炎性受体 (EP2、EP3、IP) 上的活性较弱，IC50 值 ≥1100 nM[1]。
AGN 225660 (1-10 μM; 24 h) 可呈剂量依赖性且显著抑制人单核细胞来源巨噬细胞中由 TNFα 诱导的 IL-8、MCP-1 和 RANTES 分泌[1]。
AGN 225660 (1-10 μM; 18-20 h) 可显著抑制 LPS (HY-D1056) 诱导的人单核细胞来源树突状细胞中 IL-12p70 和 IL-23 的分泌，抑制率达 65%-75%[1]。

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

AGN 225660 相关抗体:
体内研究
(In Vivo)

AGN 225660 (1%；局部给药) 可显著减少 Lewis 大鼠中 LPS (HY-D1056) 诱导的眼部葡萄膜炎的蛋白渗出和白细胞浸润[1]。
AGN 225660 (0.1-0.3%；局部给药) 以 0.3%剂量可完全抑制 Arachidonic acid (HY-109590) 诱导的荷兰垂耳兔葡萄膜炎中的白细胞浸润[1]。
AGN 225660 (0.3%；局部给药；每日 2 次) 可使非洲绿猴因超声乳化白内障吸除术诱发的前房闪辉降低约 50%[1]。

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

Animal Model: LEW/SsNHsd (male, 180-200 g, LPS-induced)[1]
Dosage: 1%
Administration: topical
Result: Reduced aqueous humor protein concentration to <20 mg/mL vs vehicle control.
Significantly reduced leukocyte infiltration into the anterior chamber.
Animal Model: Dutch Belted pigmented (male/female, 2.5-3 kg, Arachidonic acid-induced)[1]
Dosage: 0.1%; 0.3%
Administration: topical
Result: Produced marginal inhibition of leukocyte infiltration at 0.1% dose.
Totally inhibited arachidonic acid-induced leukocyte infiltration into the anterior chamber at 0.3% dose.
Animal Model: Chlorocebus sabaeus (8 males, 7 females, 3.2-6.7 kg, phacoemulsification surgery-induced)[1]
Dosage: 0.3%
Administration: topical; twice daily
Result: Reduced laser flare responses by ~50% relative to PBS-treated controls on day 1 post-surgery.
分子量

378.89

Formula

C20H27ClN2O3
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

AGN 225660 相关分类

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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.

Keywords:

AGN 2256601354060-46-0AGN225660AGN-225660Prostaglandin ReceptorInterleukin RelatedILuveitisDP1TPIL-8MCP-1EP4EP1FPRANTESIL-12p70Inhibitorinhibitorinhibit

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产品名称：
AGN 225660
目录号：
HY-183037
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