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Temanogrel

Temanogrel
Temanogrel (APD791) is a highly selective antagonist of the 5-HT2A receptor (Ki: 4.9 nM).
Catalog No. T17033Cas No. 887936-68-7
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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).
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
Pack SizePriceAvailabilityQuantity
1 mg$63In Stock
5 mg$158In Stock
10 mg$236In Stock
25 mg$395In Stock
50 mg$562In Stock
100 mg$762In Stock
200 mg$987In Stock
1 mL x 10 mM (in DMSO)$173In 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).
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].
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 | Shipping with blue ice.
Solubility Information
DMSO: 125 mg/mL (286.37 mM), Sonication is recommended.
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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