Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Temanogrel (APD791) is a highly selective antagonist of the 5-HT2A receptor (Ki: 4.9 nM).
パッケージサイズ | 在庫状況 | 単価(税別) | |||
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1 mg | 在庫あり | ¥ 24,000 | |||
5 mg | 在庫あり | ¥ 60,500 | |||
10 mg | 在庫あり | ¥ 90,500 | |||
25 mg | 在庫あり | ¥ 151,000 | |||
50 mg | 在庫あり | ¥ 215,000 | |||
100 mg | 在庫あり | ¥ 291,500 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 66,000 |
説明 | Temanogrel (APD791) is a highly selective antagonist of the 5-HT2A receptor (Ki: 4.9 nM). |
ターゲット&IC50 | 5-HT2A:4.9 nM (ki) |
In vitro | 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]. |
In vivo | 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]. |
別名 | APD791 |
分子量 | 436.5 |
分子式 | C24H28N4O4 |
CAS No. | 887936-68-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 125 mg/mL (286.37 mM), Sonication is recommended.
You can also refer to dose conversion for different animals. 詳細
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Temanogrel 887936-68-7 GPCR/G Protein Neuroscience 5-HT Receptor inhibit Serotonin Receptor Inhibitor 5-hydroxytryptamine Receptor APD 791 APD791 APD-791 inhibitor