NAPHTHO[1,2-D]THIAZOL-2-AMINE
![NAPHTHO[1,2-D]THIAZOL-2-AMINE,40172-65-4,结构式](https://www.chemicalbook.com/CAS/GIF/40172-65-4.gif)
- CAS号:40172-65-4
- 英文名:2-AMINO-BETA-NAPHTHOTHIAZOLE
- 中文名:NAPHTHO[1,2-D]THIAZOL-2-AMINE
- CBNumber:CB5244427
- 分子式:C11H8N2S
- 分子量:200.26
- MOL File:40172-65-4.mol
- 熔点 :184-188°C
- 沸点 :417.1±28.0 °C(Predicted)
- 密度 :1.403±0.06 g/cm3(Predicted)
- 储存条件 :Keep in dark place,Sealed in dry,2-8°C
- 溶解度 :DMSO: ≥30mg/mL
- 形态 :solid
- 酸度系数(pKa) :3.50±0.30(Predicted)
- 颜色 :Off-white
- 稳定性 :Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.
- CAS 数据库 :40172-65-4(CAS DataBase Reference)
- EPA化学物质信息 :Naphtho[1,2-d]thiazol-2-amine (40172-65-4)
- 危险品标志 :Xn
- 危险类别码 :20/21/22-36/37/38-36-22
- 安全说明 :22-36/37/39-26
NAPHTHO[1,2-D]THIAZOL-2-AMINE性质、用途与生产工艺
- 生物活性 SKA-31 是钾离子通道 (potassium channel) 激活剂，作用于 KCa3.1，KCa2.2，KCa2.1 和 KCa2.3 的 EC50 值分别为 260 nM，1.9 μM，2.9 μM，2.9 μM，能增强内皮源性超极化因子反应，降低血压。
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靶点
EC50: 2.9 μM (KCa2.1), 1.9 μM (KCa2.2), 2.9 μM (KCa2.3), 260 nM (KCa3.1)
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体外研究
SKA-31 activates KCa2/3 channels more potently than PK 26124, and is more selective over other Ion channels.
SKA-31 reduces cell viability with IC 50s of 5.3 μM , 46.9 μM in HCT-116 cells and HCT-8 cells, respectively.
SKA-31 (5.3 μM; 0-96 hours) reduces HCT-116 cells proliferation when added at time zero at 5.3 μM.
SKA-31 triggers apoptosis in HCT-116 cells at 5 μM, and the effect is smaller in HCT-8 cells at 45 μM.
SKA-31 increases the percentage of cells in G0/G1 phase in HCT-116 and HCT-8 cell lines at 5 μM and 45 μM, respectively.
SKA-31 further activates Caspase 3 and reduces Akt phosphorylation induced by CDDP.
SKA-31 has a synergic effect with CDDP also on the inhibition of HCT-116 cell proliferation.
Cell Viability Assay
Cell Line: HCT-116 cells, HCT-8 cells Concentration: Incubation Time: 24 hours Result: Reduced cell viability with IC 50s of 5.3 μM , 46.9 μM in HCT-116 and HCT-8, respectively. Cell Proliferation Assay
Cell Line: HCT-116 cells Concentration: 5.3 μM Incubation Time: 0-96 hours Result: Reduced HCT-116 cells proliferation when added at time zero at IC 50S value. Apoptosis Analysis
Cell Line: HCT-116 cells, HCT-8 cells Concentration: 5 μM (HCT-116 cells), 45 μM (HCT-8 cells) Incubation Time: 24 hours Result: Triggered apoptosis in HCT-116 cells, and the effect was smaller in HCT-8 cells. Cell Cycle Analysis
Cell Line: HCT-116 cells, HCT-8 cells Concentration: 5 μM (HCT-116), 45 μM (HCT-8) Incubation Time: 24 hours Result: Increased the percentage of cells in G0/G1 phase in HCT-116 and HCT-8 cell lines. Western Blot Analysis
Cell Line: HCT-116 cells Concentration: Incubation Time: 24 hours Result: Further activated Caspase 3 and reduced Akt phosphorylation when co-treatment with CDDP in HCT-116 cells. -
体内研究
SKA-31 is not acutely toxic and has good pharmacokinetic properties.
SKA-31 potentiates native KCa3.1 and KCa2.3 in murine carotid endothelium with EC 50 values of 225 nM and 1.6 μM for KCa3.1 and KCa2.3, respectively.
SKA-31 stimulates KCa3.1 and KCa2.3 in vascular endothelial cells and increases acetylcholine-induced endothelium-derived hyperpolarizing factor (EDHF) -mediated vasodilation.
SKA-31 potentiates EDHF-type vasodilations and lowers blood pressure in mice. Injections of SKA-31 (1-30 mg/kg; i.p.) lower MAP over 24 hours in normotensive wild-type mice but not in KCa3.1(-/-) mice (-/-).
Animal Model: 16-25 weeks mice Dosage: 1 mg/kg, 10 mg/kg, and 30 mg/kg Administration: Intraperitoneal injection Result: Lower MAP over 24 hours in normotensive wild-type mice but not in KCa3.1(-/-) mice (-/-).
- 更新日期：2024/11/08
- 产品编号：HY-111655
- 产品名称：NAPHTHO[1,2-D]THIAZOL-2-AMINE SKA-31
- CAS编号：40172-65-4
- 包装：5mg
- 价格：600元
- 更新日期：2024/11/08
- 产品编号：HY-111655
- 产品名称：NAPHTHO[1,2-D]THIAZOL-2-AMINE SKA-31
- CAS编号：40172-65-4
- 包装：10mM * 1mLin DMSO
- 价格：770元
- 公司名称：CHEMSTEP
- 联系电话：--
- 电子邮件：info@chemstep.com
- 国家：欧洲
- 产品数：6143
- 优势度：51
