1. Metabolic Enzyme/Protease Immunology/Inflammation
  2. Phosphatase FAP
  3. CL 118326

CL 118326 是一种强效、选择性、竞争性的哺乳动物胰腺磷脂酶 A2 (PLA2) 抑制剂和弱的血小板活化因子受体 (PAF receptor) 拮抗剂。CL 118326 可竞争性抑制哺乳动物胰腺 PLA2 (猪:IC50 = 1.55 μg/mL),对蛇毒或蜂毒 PLA2 无活性。CL 118326 可抑制 PAF 诱导和凝血酶诱导的血小板聚集、嗜碱性粒细胞富集白细胞中白三烯 (LTC4) 和组胺的释放。CL 118326 可用于研究炎症和过敏反应。

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CL 118326

CL 118326 Chemical Structure

CAS No. : 97012-61-8

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CL 118326 is a potent, selective, competitive inhibitor of mammalian pancreatic phospholipase A2 (PLA2) and a weak antagonist of platelet-activating factor receptor (PAF receptor). CL 118326 competitively inhibits mammalian pancreatic PLA2 (porcine: IC50 = 1.55 μg/mL), and shows no activity against snake venom or bee venom PLA2. CL 118326 inhibits PAF-induced and thrombin-induced platelet aggregation, as well as the release of leukotriene (LTC4) and histamine from basophil-enriched leukocytes. CL 118326 can be used for research on inflammation and allergic reactions[1].

体外研究
(In Vitro)

CL 118326 (5 min) 可抑制凝血酶诱导 (IC50 = 7.9 μM) 及 PAF 诱导 (IC50 = 5.8 μM) 的兔血小板聚集,但不抑制花生四烯酸或 ADP 诱导的聚集,且无 PAF 激动剂活性[1]
CL 118326 (70 min) 可抑制抗原和离子载体刺激的人嗜碱性粒细胞富集白细胞释放组胺和 LTC4,其 IC50 值范围为 1.36 至 2.34 μg/mL[1]

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

体内研究
(In Vivo)

CL 118326 (10-20 μg;皮内注射;单次给药) 可剂量依赖性地抑制猪胰腺磷脂酶 A2 诱导的豚鼠皮肤毛细血管渗漏,其中 10 μg 剂量对病灶面积的抑制率最高可达 87.2%[1]

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

Animal Model: Hartly (male, 250-350 g)[1]
Dosage: 10 μg; 20 μg
Administration: i.d.; single coinjection with PLA2
Result: Reduced porcine pancreatic PLA2-induced skin lesion size by 60.4% (from 83.0 mm2 to 32.8 mm2) and 51.0% (from 36.4 mm2 to 17.0 mm2) in one experiment, and by 84.4% (from 124.0 mm2 to 19.3 mm2) and 87.2% (from 56.2 mm2 to 7.2 mm2) in a second experiment, for 50-unit and 25-unit PLA2 challenges respectively.
Reduced lesion size relative to controls across multiple PLA2 dose levels at 20 μg.
分子量

615.73

Formula

C28H58INO3S

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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  • 稀释计算器

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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:
CL 118326
目录号:
HY-182434
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