NAPHTHO[1,2-D]THIAZOL-2-AMINE

生物活性靶点体外研究体内研究 NAPHTHO[1,2-D]THIAZOL-2-AMINE 试剂级价格

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

NAPHTHO[1,2-D]THIAZOL-2-AMINE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 :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)

安全信息

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。
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 (-/-).