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Temanogrel (APD791) is a highly selective antagonist of the 5-HT2A receptor (Ki: 4.9 nM).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $63 | In Stock | |
5 mg | $158 | In Stock | |
10 mg | $236 | In Stock | |
25 mg | $395 | In Stock | |
50 mg | $562 | In Stock | |
100 mg | $762 | In Stock | |
200 mg | $987 | In Stock | |
1 mL x 10 mM (in DMSO) | $173 | In Stock |
Description | Temanogrel (APD791) is a highly selective antagonist of the 5-HT2A receptor (Ki: 4.9 nM). |
Targets&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]. |
Alias | APD791 |
Molecular Weight | 436.5 |
Formula | C24H28N4O4 |
Cas No. | 887936-68-7 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 125 mg/mL (286.37 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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