NAPHTHO[1,2-D]THIAZOL-2-AMINE
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- CAS号:
- 40172-65-4
- 英文名:
- 2-AMINO-BETA-NAPHTHOTHIAZOLE
- 英文别名:
- SKA 31;-2-amine;AKOS BBS-00006561;IFLAB-BB F1386-0401;naphtho[1,2-d]thiazoL;LABOTEST-BB LT00154570;2-Amino-β-naphthothiazole;2-AMINONAPHTHO-1,2-THIAZOLE;2-AMINO-BETA-NAPHTHOTHIAZOLE;naphtho[1,2-d]thiazol-2-amine
- 中文名:
- NAPHTHO[1,2-D]THIAZOL-2-AMINE
- 中文别名:
- 化合物SKA-31;萘并[1,2-D]噻唑-2-胺;SKA-31,K CA 3.1和K CA 2通道激活剂
- CBNumber:
- CB5244427
- 分子式:
- C11H8N2S
- 分子量:
- 200.26
- MOL File:
- 40172-65-4.mol
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NAPHTHO[1,2-D]THIAZOL-2-AMINE化学性质
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熔点:
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184-188°C
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沸点:
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417.1±28.0 °C(Predicted)
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密度:
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1.403±0.06 g/cm3(Predicted)
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储存条件:
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Keep in dark place,Sealed in dry,2-8°C
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溶解度:
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DMSO: ≥30mg/mL
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形态:
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solid
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酸度系数(pKa):
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3.50±0.30(Predicted)
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颜色:
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Off-white
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稳定性:
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Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.
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CAS 数据库:
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40172-65-4(CAS DataBase Reference)
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EPA化学物质信息:
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Naphtho[1,2-d]thiazol-2-amine (40172-65-4)
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NAPHTHO[1,2-D]THIAZOL-2-AMINE性质、用途与生产工艺
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。
EC50: 2.9 μM (KCa2.1), 1.9 μM (KCa2.2), 2.9 μM (KCa2.3), 260 nM (KCa3.1)
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
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Cell Line:
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HCT-116 cells, HCT-8 cells
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Concentration:
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Incubation Time:
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24 hours
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Result:
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Reduced cell viability with IC
50s
of 5.3 μM , 46.9 μM in HCT-116 and HCT-8, respectively.
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Cell Proliferation Assay
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Cell Line:
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HCT-116 cells
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Concentration:
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5.3 μM
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Incubation Time:
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0-96 hours
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Result:
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Reduced HCT-116 cells proliferation when added at time zero at IC
50S
value.
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Apoptosis Analysis
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Cell Line:
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HCT-116 cells, HCT-8 cells
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Concentration:
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5 μM (HCT-116 cells), 45 μM (HCT-8 cells)
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Incubation Time:
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24 hours
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Result:
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Triggered apoptosis in HCT-116 cells, and the effect was smaller in HCT-8 cells.
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Cell Cycle Analysis
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Cell Line:
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HCT-116 cells, HCT-8 cells
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Concentration:
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5 μM (HCT-116), 45 μM (HCT-8)
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Incubation Time:
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24 hours
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Result:
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Increased the percentage of cells in G0/G1 phase in HCT-116 and HCT-8 cell lines.
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Western Blot Analysis
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Cell Line:
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HCT-116 cells
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Concentration:
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Incubation Time:
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24 hours
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Result:
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Further activated Caspase 3 and reduced Akt phosphorylation when co-treatment with CDDP in HCT-116 cells.
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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 (-/-).
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Animal Model:
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16-25 weeks mice
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Dosage:
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1 mg/kg, 10 mg/kg, and 30 mg/kg
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Administration:
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Intraperitoneal injection
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Result:
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Lower MAP over 24 hours in normotensive wild-type mice but not in KCa3.1(-/-) mice (-/-).
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NAPHTHO[1,2-D]THIAZOL-2-AMINE
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/01/25 | HY-111655 | NAPHTHO[1,2-D]THIAZOL-2-AMINE
SKA-31 | 40172-65-4 | 5mg | 600元 |
| 2024/01/25 | HY-111655 | NAPHTHO[1,2-D]THIAZOL-2-AMINE
SKA-31 | 40172-65-4 | 10mM * 1mLin DMSO | 770元 |
NAPHTHO[1,2-D]THIAZOL-2-AMINE
生产厂家
40172-65-4, NAPHTHO[1,2-D]THIAZOL-2-AMINE 相关搜索:
- BENZOTHIAZOLE
- 合成有机化合物配体
- 有机化工原料
- 合成
- SKA-31,K CA 3.1和K CA 2通道激活剂
- 化合物SKA-31
- 萘并[1,2-D]噻唑-2-胺
- 40172-65-4
- inhibit,Potassium Channel,SKA-31,KcsA,Inhibitor
- benzo[e][1,3]benzothiazol-2-amine
- Naphtho[1,2-d]thiazol-2(1H)-imine
- naphtho[1,2-d]thiazoL
- -2-amine
- 2-(2-amino-5,6-dihydro-4H-pyrimidin-1-yl)acetic acid
- SKA 31
- 2-Amino-β-naphthothiazole
- Naphtho[1,2-d]thiazol-2-amine (9CI)
- naphtho[1,2-d]thiazol-2-amine
- LABOTEST-BB LT00154570
- IFLAB-BB F1386-0401
- AKOS BBS-00006561
- 2-AMINONAPHTHO-1,2-THIAZOLE
- 2-AMINO-NAPHTHO[1,2-D]THIAZOLE
- 2-AMINO-BETA-NAPHTHOTHIAZOLE
- NAPHTHO[1,2-D]THIAZOL-2-YLAMINE
- NAPHTHO[1,2-D][1,3]THIAZOL-2-AMINE