959705-64-7

959705-64-7 structure

Name: TC-E 5005
Chemical Name: 2-Methoxy-6,7-dimethyl-9-propylimidazo[1,5-a]pyrido[3,2-e]pyrazin e
CAS Number: 959705-64-7
Molecular Formula: C₁₅H₁₈N₄O
Molecular Weight: 270.33000
Catalog: Signaling Pathways Metabolic Enzyme/Protease Phosphodiesterase (PDE)
Create Date: 2018-12-26 14:04:12
Modify Date: 2024-01-06 10:25:37
TC-E 5005 is a potent and selective PDE10A inhibitor with IC50 values of 7.28, 239, 779, 919, 3,100, and 3,700 nM for PDE10A, 2A, 11A, 5A, 7B and 3A, respectively. TC-E 5005 inhibits adrenergic and neurogenic smooth muscle contractions in the human prostate[1].

Name	2-Methoxy-6,7-dimethyl-9-propylimidazo[1,5-a]pyrido[3,2-e]pyrazin e
Synonyms	TC-E 5005

Description	TC-E 5005 is a potent and selective PDE10A inhibitor with IC50 values of 7.28, 239, 779, 919, 3,100, and 3,700 nM for PDE10A, 2A, 11A, 5A, 7B and 3A, respectively. TC-E 5005 inhibits adrenergic and neurogenic smooth muscle contractions in the human prostate[1].
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphodiesterase (PDE) Research Areas >> Metabolic Disease
Target	PDE10A:7.28 nM (IC50) PDE2A:239 nM (IC50) hPDE11A:779 nM (IC50) PDE5A:919 nM (IC50) PDE7B:3100 nM (IC50) PDE3A:3700 nM (IC50)
In Vitro	TC-E 5005 (500 nM) inhibits norepinephrine or phenylephrine and EFS (electric field stimulation)-induced contraction of human prostate strips[1]. TC-E 5005 (500 nM) shows amplification of treprostinil-induced relaxations, which were significant from 0.03 to 30 μM treprostinil[1].
References	[1]. Hennenberg M, et al. Inhibition of Adrenergic and Non-Adrenergic Smooth Muscle Contraction in the Human Prostate by the Phosphodiesterase 10-Selective Inhibitor TC-E 5005. Prostate. 2016 Nov;76(15):1364-74.