计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
为什么选择此级别
，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
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 (a 1 G) and Cav3.2 (a 1 H) channels with IC 50 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
In Vitro
TTA-A2 exhibits a state-dependent inhibition of α 1 I with potencies of 98 nM and 3.7 μM at membrane holding potentials of -80 and -100 mV, respectively in astandard voltage-clamp electrophysiology assay. It also exhibits excellent selectivity against the Cav1.2 (L-type), Cav2.1 (P/Q-type), Cav2.2 (N-type), and Cav2.3 (R-type) channels which all had IC 50 values of >30 μM at 80 mV. TTA-A2 exhibits high affinity in the α 1 I binding assay with a K i of 1.2 nM and has excellent selectivity over the hERG potassium channel and L-type calcium channel (both IC 50 >10 μM). MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 . 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Wild-type and double Cav3.1/Cav3.3 knockout C57BL6/Sv129 background micesDosage: 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.
IC50& Target:IC50: 98 nM ( α 1 I at membrane holding potentials of -80 mV) IC50: 3.7 μM (α 1 I at membrane holding potentials of -100 mV)
规格
规格或纯度
10mM in DMSO
英文名称
TTA-A2
生化机理
TTA-A2 是一种强效、具有选择性和口服活性的 t 型电压门控钙xa0 通道拮抗剂，可减少孕烷 X 受体（PXR）的激活。TTA-A2 对 Cav3.1 (a 1 G) 和 Cav3.2 (a 1 H) 通道同样有效，IC 50 值为 89 nM。
储存条件
-80℃储存
运输条件
特低温运输
名称和识别符
分子类型
小分子
Isomeric SMILES
C[C@H](C1=NC=C(C=C1)OCC(F)(F)F)NC(=O)CC2=CC=C(C=C2)C3CC3
PubChem CID
MeSH Entry Terms
2-(4-cyclopropylphenyl)-N-(1-(5-((2,2,2-trifluoroethyl)oxo)pyridin-2-yl)ethyl)acetamide;TTA-A2
分子量
378.39
技术文档
高级数据
关联靶点（人）
CACNA1H
Tclin
电压依赖性T型钙通道亚基α-1H(Voltage-dependent T-type calcium channel subunit alpha-1H)
(0 活性数据)
CACNA1G
Tclin
电压依赖性T型钙通道亚基α-1G(Voltage-dependent T-type calcium channel subunit alpha-1G)
(0 活性数据)
CACNA1I
Tclin
电压依赖性T型钙通道亚基α-1I(Voltage-dependent T-type calcium channel subunit alpha-1I)
(0 活性数据)
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
常见问题
本产品应如何储存？
请于?80 °C条件下保存。需超低温保存以维持规定的有效期。
本产品如何运输？
本产品采用干冰配冷袋冷冻运输。收货后请立即拆包，并按上述储存条件保存；处理干冰时请戴隔热手套并保持通风。
本产品的 CAS 号、分子式和分子量是多少？
本产品的 CAS 号为 953778-63-7，分子式为 C20H21F3N2O2，分子量为 378.39 g/mol。
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