CAS NO: | 116649-85-5 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | Ramatroban is a selectivethromboxane A2(TxA2,IC50=14 nM) antagonist, which also antagonizesCRTH2(IC50=113 nM) by inhibitingPGD2binding. | ||||||||||||||||
IC50& Target[1] |
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体外研究 (In Vitro) | Ramatroban is a potent human thromboxane receptor (hTP) antagonist with an IC50of 18 nM in a human TP binding assay. Ramatroban inhibits prostaglandin D2receptor DP2 (CRTH2) with an IC50of 113 nM in a human DP2 binding assay. Ramatroban also inhibits human CYP isoform CYP2C9 with an IC50of 15 μM[1]. Ramatroban is a selective thromboxane-type prostanoid (TP) receptor antagonist. PGD2-stimulated human eosinophil migration is shown to be mediated exclusively through activation of CRTH2, and surprisingly, these effects are completely inhibited by Ramatroban. Ramatroban is an antagonist for CRTH2, and inhibits PGD2-induced migration of eosinophils via CRTH2 blockade.3H-labeled PGD2binds to a single site on CRTH2 transfectants with high affinity (KD=6.3 nM, Bmax=450 pM). Nonlabeled PGD2inhibits the binding of3H-labeled PGD2to CRTH2 transfectants in a concentration-dependent manner with an EC50value of 2.7 nM. Ramatroban shows significant inhibitory effects on the binding of3H-labeled PGD2to CRTH2, albeit with much lower potency (IC50=100 nM). Ramatroban also inhibits PGD2-induced Ca2+mobilization in CRTH2 transfectants to almost the same extent with an IC50value of 30 nM. Ramatroban completely inhibits the PGD2-induced migration of eosinophils in a concentration-dependent manner with an IC50value of 170 nM[2]. | ||||||||||||||||
体内研究 (In Vivo) | 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[3]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 416.47 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C21H21FN2O4S | ||||||||||||||||
CAS 号 | 116649-85-5 | ||||||||||||||||
中文名称 | 雷马曲班 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 125 mg/mL(300.14 mM;Need ultrasonic) 配制储备液
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以下溶剂前显示的百
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