tcsc0002653 Temanogrel

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Product Description

Temanogrel is a highly selective 5-HT2A receptor antagonist with a Ki of 4.9 nM.

IC50 & Target: Ki: 4.9 nM (5-HT2A receptor)

In Vitro: Temanogrel is a highly selective 5-HT2A receptor antagonist with a Ki of 4.9 nM. Temanogrel inhibits inositol phosphate accumulation with an IC50 of 5.2 nM. Temanogrel exhibits potent inhibition of serotonin mediated amplification of ADP-stimulated human and dog platelet aggregation (IC50=8.7 and 23.1 nM, respectively)[1]. 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 with an IC50 of 13±7 nM[3].

In Vivo: There are no differences in heart rate or mean arterial pressure between saline-treated and Temanogrel-treated groups at any time during the experiment (that is, for mean arterial pressure, P=0.508 between groups, and P=0.540 for group-time interaction). In dogs assigned to receive Temanogrel, 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[3].


CAS No887936-68-7
Clinical Informationclinicalinformation
PathwayNeuronal Signaling
GPCR/G Protein
Target5-HT Receptor
5-HT Receptor


Purity / Grade>98%
SolubilityDMSO : 125 mg/mL (286.37 mM; Need ultrasonic)

Misc Information

Alternative NamesAPD791
Observed Molecular Weight436.5
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