PSI-697(Synonyms: P-Selectin Inhibitor)

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PSI-697 (Synonyms: P-Selectin Inhibitor) 纯度: 99.70%

PSI-697 是一种口服的 P-selectin 抑制剂，IC50 值为 125 μM。

PSI-697(Synonyms: P-Selectin Inhibitor)

PSI-697 Chemical Structure

CAS No. : 851546-61-7

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥2832 In-stock
1 mg ￥1400 In-stock
5 mg ￥3500 In-stock
10 mg ￥5000 In-stock
50 mg ￥15000 In-stock
100 mg ￥21000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

PSI-697 相关产品

•相关化合物库:

  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus

生物活性

PSI-697 is an oral P-selectin inhibitor with an IC50 of 125 μM[1].

IC50 & Target

IC50: 125 μM (P-selectin)[1]
体外研究
(In Vitro)

PSI-697 inhibits the binding of a soluble human P-selectin to PSGL-1, in a reproducible concentration-dependent manner inhibiting 50% of binding at a concentration of 125 μM in vitro[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

PSI-697 (0-50 mg/kg; p.o.) significantly reduces the number of rolling leukocytes by 39% versus vehicle control[1].
PSI-697 (100 mg/kg; p.o.) reduces thrombus weight by 18% relative to vehicle, without prolonging bleeding time in a rat venous thrombosis model[1].
PSI-697 (30 mg/kg; p.o.; daily; 6 days) promotes thrombus resolution and decreases inflammation in a baboon model of venous thrombosis[2].
PSI-697 ((30 mg/kg; i.g.; daily) decreases vein wall injury in a rat stenosis model of venous thrombosis[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 4-5 weeks male Sprague-Dawley rat (50-100 g)[1]
Dosage: 0 mg/kg, 30 mg/kg, 50 mg/kg
Administration: Oral administration
Result: At an oral dose of 50 mg/kg reduced the number of rolling leukocytes by 39% versus vehicle control.

Clinical Trial

分子量

367.83

Formula

C21H18ClNO3
CAS 号

851546-61-7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 45.8 mg/mL (124.51 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7186 mL 13.5932 mL 27.1865 mL
5 mM 0.5437 mL 2.7186 mL 5.4373 mL
10 mM 0.2719 mL 1.3593 mL 2.7186 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [1]. Bedard PW et al. Characterization of the novel P-selectin inhibitor PSI-697 [2-(4-chlorobenzyl)-3-hydroxy-7,8,9,10-tetrahydrobenzo[h] quinoline-4-carboxylic acid] in vitro and in rodent models of vascular inflammation and thrombosis. J Pharmacol Exp Ther.

    [2]. Myers DD Jr et al. Resolution of venous thrombosis using a novel oral small-molecule inhibitor of P-selectin (PSI-697) without anticoagulation. Thromb Haemost. 2007 Mar;97(3):400-7.

    [3]. Myers DD Jr et al. Treatment with an oral small molecule inhibitor of P selectin (PSI-697) decreases vein wall injury in a rat stenosis model of venous thrombosis. J Vasc Surg. 2006 Sep;44(3):625-32.

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