
Temanogrel
CAS No. 887936-68-7
Temanogrel( APD791 )
Catalog No. M24910 CAS No. 887936-68-7
Temanogrel is a highly selective antagonist of the 5-HT2A receptor (Ki: 4.9 nM).
Purity : >98% (HPLC)






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Biological Information
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Product NameTemanogrel
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NoteResearch use only, not for human use.
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Brief DescriptionTemanogrel is a highly selective antagonist of the 5-HT2A receptor (Ki: 4.9 nM).
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DescriptionTemanogrel is a highly selective antagonist of the 5-HT2A receptor (Ki: 4.9 nM). (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). 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.(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.
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In VitroTemanogrel 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). 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.
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In VivoThere 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.
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SynonymsAPD791
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PathwayEndocrinology/Hormones
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Target5-HT Receptor
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Recptor5-HT2A
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Research Area——
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Indication——
Chemical Information
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CAS Number887936-68-7
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Formula Weight436.5
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Molecular FormulaC24H28N4O4
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Purity>98% (HPLC)
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SolubilityDMSO:125 mg/mL (286.37 mM; Need ultrasonic)
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SMILESCn1nccc1-c(cc(cc1)NC(c2cc(OC)ccc2)=O)c1OCCN1CCOCC1
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1.Xiong Y, et al. Discovery and structure-activity relationship of 3-methoxy-N-(3-(1-methyl-1H-pyrazol-5-yl)-4-(2-morpholinoethoxy)phenyl)benzamide (APD791): a highly selective 5-hydroxytryptamine2A receptor inverse agonist for the treatment of arterial thrombosis. J Med Chem. 2010 Jun 10;53(11):4412-21.
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