40172-65-4

中文名称 NAPHTHO[1,2-D]THIAZOL-2-AMINE

英文名称 2-AMINO-BETA-NAPHTHOTHIAZOLE

CAS 40172-65-4

EINECS 编号 254-822-1

分子式 C11H8N2S

MDL 编号 MFCD00051329

分子量 200.26

MOL 文件 40172-65-4.mol

更新日期 2024/04/14 10:33:09

40172-65-4 结构式

基本信息物理化学性质安全数据图谱信息 NAPHTHO[1,2-D]THIAZOL-2-AMINE价格(试剂级) 常见问题列表

基本信息

中文别名

化合物SKA-31
萘并[1,2-D]噻唑-2-胺

英文别名

2-AMINO-BETA-NAPHTHOTHIAZOLE

所属类别

化学试剂：多环化合物

物理化学性质

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

溶解度二甲基亚砜：≥30mg/mL

酸度系数(pKa)3.50±0.30(Predicted)

形态固体

颜色米白色

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)

安全数据

危险性符号(GHS)

GHS07

警示词警告

危险性描述H302-H319

防范说明P264-P270-P280-P301+P312-P305+P351+P338-P337+P313

危险品标志Xn

危险类别码20/21/22-36/37/38-36-22

危险类别码R20/21/22-R36/37/38

安全说明22-36/37/39-26

安全说明S22-S36/37/39

图谱信息

NAPHTHO[1,2-D]THIAZOL-2-AMINE(40172-65-4)核磁图(¹HNMR)
NAPHTHO[1,2-D]THIAZOL-2-AMINE(40172-65-4)红外图谱(IR1)
NAPHTHO[1,2-D]THIAZOL-2-AMINE(40172-65-4)红外图谱(IR2)

NAPHTHO[1,2-D]THIAZOL-2-AMINE价格(试剂级)

报价日期	产品编号	产品名称	CAS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
2024/01/25	HY-111655	NAPHTHO[1,2-D]THIAZOL-2-AMINE SKA-31	40172-65-4	10mg	1000元

常见问题列表

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。

靶点

EC50: 2.9 μM (KCa2.1), 1.9 μM (KCa2.2), 2.9 μM (KCa2.3), 260 nM (KCa3.1)

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 (-/-).