| Identification | Back Directory | [Name]
"(R)-2-(4-cyclopropylphenyl)-N-(1-(5-(2,2,2-trifluoroethoxy)pyridin-2-yl)ethyl)acetamide " | [CAS]
953778-63-7 | [Synonyms]
TTA-A2
(R)-2-(4-cyclopropylphenyl)-N-(1-(5-(2,2,2-trifluoroethoxy)pyridin-2-yl)ethyl)acetamid
2-(4-cyclopropylphenyl)-N-[(1R)-1-[5-(2,2,2-trifluoroethoxy)pyridin-2-yl]ethyl]acetamide
Benzeneacetamide, 4-cyclopropyl-N-[(1R)-1-[5-(2,2,2-trifluoroethoxy)-2-pyridinyl]ethyl]-
"(R)-2-(4-cyclopropylphenyl)-N-(1-(5-(2,2,2-trifluoroethoxy)pyridin-2-yl)ethyl)acetamide "
Pregnane X receptor,TTA-A2,neurological diseases,T-type calcium channel,Inhibitor,Ca2+ channels,Ca channels,Electrocorticogram,TTAA2,sleep disorders,TTA-A-2,inhibit,TTA A2,Epilepsy,Calcium Channel | [Molecular Formula]
C20H21F3N2O2 | [MOL File]
953778-63-7.mol | [Molecular Weight]
378.39 |
| Chemical Properties | Back Directory | [Boiling point ]
538.5±50.0 °C(Predicted) | [density ]
1.258±0.06 g/cm3(Predicted) | [solubility ]
DMSO: Soluble: =10 mg/ml
Ethanol: Soluble: =10 mg/ml | [form ]
Solid | [pka]
14.29±0.46(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
TTA-A2 is a potent, selective and orally active t-type voltage gated calcium channel antagonist with reduced pregnane X receptor (PXR) activation. TTA-A2 is equally potent against the Cav3.1 (a1G) and Cav3.2 (a1H) channels with IC50 values of 89 nM and 92 nM, respectively, at -80 and -100 mV holding potentials. TTA-A2 can be used for the research of a variety of human neurological diseases, including sleep disorders and epilepsy[1][2]. | [in vivo]
TTA-A2 (oral gavage; 3 mg/kg; single dose) produces significant changes in sleep architecture in rats. A reduction in active wake soon after dosing with a concurrent increase in delta sleep and decrease in REM sleep. Additionally, these effects persists for up to 4 h post-dose in rats[1].TTA-A2 (oral gavage; 10 mg/kg; once daily; 5 days) shows selective effect on recurrent thalamocortical network activity, it suppresses active wake and promotes slow-wave sleep in wild-type mice but not in mice lacking both Cav3.1 and Cav3.3[2]. | Animal Model: | Wild-type and double Cav3.1/Cav3.3 knockout C57BL6/Sv129 background mices[2] | | Dosage: | 10?mg/kg | | Administration: | Oral gavage; 10?mg/kg; once daily; 5 days | | Result: | Blocked active wake and promotes slow-wave sleep in wild-type mice but not mutant mice. |
| [IC 50]
T-type calcium channel | [References]
[1] Thomas S Reger, et al.Pyridyl amides as potent inhibitors of T-type DOI:10.1016/j.bmcl.2011.01.089
[2] Richard L Kraus, et al.In vitro characterization of T-type calcium channel antagonist TTA-A2 and in vivo effects on arousal in mice. J Pharmacol Exp Ther. 2010 Nov;335(2):409-17. DOI:10.1124/jpet.110.171058 |
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Cool Pharm, Ltd
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021-60455363 18019463053 |
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www.coolpharm.com |
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