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Temanogrel

Temanogrel
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Purity:98.74%
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Temanogrel

Catalog No. T17033Cas No. 887936-68-7
Temanogrel (APD791) is a highly selective antagonist of the 5-HT2A receptor (Ki: 4.9 nM).
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Pack SizePriceAvailabilityQuantity
1 mg$105In Stock
5 mg$263In Stock
10 mg$393In Stock
25 mg$658In Stock
50 mg$937In Stock
100 mg$1,270In Stock
1 mL x 10 mM (in DMSO)$288In Stock
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Product Introduction

Bioactivity
Description
Temanogrel (APD791) is a highly selective antagonist of the 5-HT2A receptor (Ki: 4.9 nM).
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].
AliasAPD791
Chemical Properties
Molecular Weight436.5
FormulaC24H28N4O4
Cas No.887936-68-7
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
DMSO: 125 mg/mL (286.37 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.2910 mL11.4548 mL22.9095 mL114.5475 mL
5 mM0.4582 mL2.2910 mL4.5819 mL22.9095 mL
10 mM0.2291 mL1.1455 mL2.2910 mL11.4548 mL
20 mM0.1145 mL0.5727 mL1.1455 mL5.7274 mL
50 mM0.0458 mL0.2291 mL0.4582 mL2.2910 mL
100 mM0.0229 mL0.1145 mL0.2291 mL1.1455 mL

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