Temanogrel

产品编号 T17033Cas号 887936-68-7

别名 APD791

Temanogrel (APD791) 是一种高度选择性的 5-HT2A 受体拮抗剂，Ki 值为 4.9 nM。

产品编号 T17033别名 APD791Cas号 887936-68-7

Temanogrel (APD791) 是一种高度选择性的 5-HT2A 受体拮抗剂，Ki 值为 4.9 nM。

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生物活性

产品描述	Temanogrel (APD791) is a highly selective antagonist of the 5-HT2A receptor (Ki: 4.9 nM).
靶点活性	5-HT2A:4.9 nM (ki)
体外活性	Temanogrel inhibits inositol phosphate accumulation (IC50: 5.2 nM). Temanogrel shows effective inhibition of serotonin mediated amplification of ADP-stimulated human and dog platelet aggregation (IC50=8.7 and 23.1 nM, respectively). 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 (IC50: 13±7 nM) [1][3].
体内活性	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 in dogs assigned to receive Temanogrel. There are no differences in heart rate or mean arterial pressure between saline-treated and Temanogrel-treated groups at any time during the experiment [3].
别名	APD791

化学信息

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

溶解度信息

DMSO: 125 mg/mL (286.37 mM), Sonication is recommended.

溶液配制表

DMSO