"(R)-2-(4-cyclopropylphenyl)-N-(1-(5-(2,2,2-trifluoroethoxy)pyridin-2-yl)ethyl)acetamide "
- Product Name
- "(R)-2-(4-cyclopropylphenyl)-N-(1-(5-(2,2,2-trifluoroethoxy)pyridin-2-yl)ethyl)acetamide "
- CAS No.
- 953778-63-7
- Chemical Name
- "(R)-2-(4-cyclopropylphenyl)-N-(1-(5-(2,2,2-trifluoroethoxy)pyridin-2-yl)ethyl)acetamide "
- Synonyms
- TTA-A2;TTA-A2, 10 mM in DMSO;(R)-2-(4-cyclopropylphenyl)-N-(1-(5-(2,2,2-trifluoroethoxy)pyridin-2-yl)ethyl)acetamid;Benzeneacetamide, 4-cyclopropyl-N-[(1R)-1-[5-(2,2,2-trifluoroethoxy)-2-pyridinyl]ethyl]-;2-(4-cyclopropylphenyl)-N-[(1R)-1-[5-(2,2,2-trifluoroethoxy)pyridin-2-yl]ethyl]acetamide;"(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
- CBNumber
- CB43120851
- Molecular Formula
- C20H21F3N2O2
- Formula Weight
- 378.39
- MOL File
- 953778-63-7.mol
"(R)-2-(4-cyclopropylphenyl)-N-(1-(5-(2,2,2-trifluoroethoxy)pyridin-2-yl)ethyl)acetamide " Property
- 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
N-Bromosuccinimide Price
- Product number
- CS-0093037
- Product name
- TTA-A2
- Purity
- ≥99.0%
- Packaging
- 1mg
- Price
- $250
- Updated
- 2021/12/16
- Product number
- CD11004405
- Product name
- (R)-2-(4-Cyclopropylphenyl)-N-(1-(5-(2,2,2-trifluoroethoxy)pyridin-2-yl)ethyl)acetamide
- Purity
- 97%
- Packaging
- 100mg
- Price
- $980
- Updated
- 2021/12/16
"(R)-2-(4-cyclopropylphenyl)-N-(1-(5-(2,2,2-trifluoroethoxy)pyridin-2-yl)ethyl)acetamide " Chemical Properties,Usage,Production
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
[3] NEEMA KUMARI Subha N R Anamika Bhargava. T-type calcium channel antagonist, TTA-A2 exhibits anti-cancer properties in 3D spheroids of A549, a lung adenocarcinoma cell line[J]. Life sciences, 2020, 260: Article 118291. DOI: 10.1016/j.lfs.2020.118291
[4] VICTOR N UEBELE. Antagonism of T-type calcium channels inhibits high-fat diet-induced weight gain in mice.[J]. The Journal of clinical investigation, 2009: 1659-1667. DOI: 10.1172/jci36954
[5] JASON M. USLANER . T-type calcium channel antagonism produces antipsychotic-like effects and reduces stimulant-induced glutamate release in the nucleus accumbens of rats[J]. Neuropharmacology, 2012, 62 3: Pages 1413-1421. DOI: 10.1016/j.neuropharm.2010.11.015
[6] MARC CHEVALIER. T-type calcium channels are involved in hypoxic pulmonary hypertension.[J]. Cardiovascular Research, 2014, 103 4: 597-606. DOI: 10.1093/cvr/cvu166
"(R)-2-(4-cyclopropylphenyl)-N-(1-(5-(2,2,2-trifluoroethoxy)pyridin-2-yl)ethyl)acetamide " Preparation Products And Raw materials
Raw materials
Preparation Products
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