CAS NO: | 887936-68-7 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
1mg | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
生物活性 | Temanogrel is a highly selective5-HT2Areceptorantagonist with aKiof 4.9 nM. | ||||||||||||||||
IC50& Target |
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体外研究 (In Vitro) | Temanogrel is a highly selective 5-HT2Areceptor antagonist with a Kiof 4.9 nM. Temanogrel inhibits inositol phosphate accumulation with an IC50of 5.2 nM. Temanogrel exhibits potent inhibition of serotonin mediated amplification of ADP-stimulated human and dog platelet aggregation (IC50=8.7 and 23.1 nM, respectively)[1]. Pretreatment of aortic rings with Temanogrel prevents the vasoconstriction caused by 20 μM 5-HT in a concentration-dependent manner. Preincubation with Temanogrel also significantly inhibits the 5-HT-stimulated DNA synthesis with an IC50of 13±7 nM[3]. | ||||||||||||||||
体内研究 (In Vivo) | There are no differences in heart rate or mean arterial pressure between saline-treated and Temanogrel-treated groups at any time during the experiment (that is, for mean arterial pressure, P=0.508 between groups, and P=0.540 for group-time interaction). In dogs assigned to receive Temanogrel, plasma Temanogrel levels show a rapid and sustained increase, averaging 25.5±4.1, 28.7±4.6 and 31.2±4.5 ng/mL, respectively, at 10 min, 1.25 h and 2.25 h after the start of treatment[3]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 436.50 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C24H28N4O4 | ||||||||||||||||
CAS 号 | 887936-68-7 | ||||||||||||||||
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(286.37 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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