S80136
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- 公司名稱 上海源葉生物科技有限公司
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- 產(chǎn)品描述： Ramatroban is a selective thromboxane A2 (TxA2, IC50=14 nM) antagonist, which also antagonizes CRTH2 (IC50=113 nM) by inhibiting PGD2 binding.
- 靶點(diǎn)： hTP:14 nM (IC50);hDP2:113 nM (IC50);hDP2:33.4 μM (IC50)
- 體內(nèi)研究： Ramatroban is an orally bioavailable small molecule antagonist of CRTH2. Systemic administration of Ramatroban (30 mg/kg) in CRTH2+/+ mice produces the same effects as seen in CRTH2 deficiency. Ramatroban completely blocks LPS-induced decreases in social and object exploratory behavior (p<0.01). in="" addition,="" tumor-impaired="" social="" interaction="" and="" object="" exploratory="" behavior="" in="" crth2+/+="" mice="" are="" completely="" reversed="" by="" a="" single="" injection="" of="" ramatroban,="" even="" when="" the="" tumor="" is="" enlarged="">
- 參考文獻(xiàn)：
1. Stearns BA, et al. Novel tricyclic antagonists of the prostaglandin D2 receptor DP2 with efficacy in a murine modelof allergic rhinitis. Bioorg Med Chem Lett. 2009 Aug 15;19(16):4647-51. 2. Sugimoto H, et al. An orally bioavailable small molecule antagonist of CRTH2, ramatroban (BAY u3405), inhibits prostaglandin D2-induced eosinophil migration in vitro. J Pharmacol Exp Ther. 2003 Apr;305(1):347-52. 3. Haba R, et al. Central CRTH2, a second prostaglandin D2 receptor, mediates emotional impairment in the lipopolysaccharide and tumor-induced sickness behavior model. J Neurosci. 2014 Feb 12;34(7):2514-23.
- 溶解度： DMSO : 125 mg/mL (300.14 mM; Need ultrasonic)
- 保存條件： 2-8℃
- 配置溶液濃度參考：
1mg 5mg 10mg 1 mM 2.401 ml 12.006 ml 24.012 ml 5 mM 0.48 ml 2.401 ml 4.802 ml 10 mM 0.24 ml 1.201 ml 2.401 ml 50 mM 0.048 ml 0.24 ml 0.48 ml
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