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
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ChemicalBook  CAS数据库列表  NAPHTHO[1,2-D]THIAZOL-2-AMINE

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
NAPHTHO[1,2-D]THIAZOL-2-AMINE,40172-65-4,结构式
NAPHTHO[1,2-D]THIAZOL-2-AMINE
  • 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

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 (-/-).
NAPHTHO[1,2-D]THIAZOL-2-AMINE上下游产品信息
上游原料
下游产品
NAPHTHO[1,2-D]THIAZOL-2-AMINE 试剂级价格
  • 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
NAPHTHO[1,2-D]THIAZOL-2-AMINE生产厂家
  • 公司名称：UKRORGSYN-BB
  • 联系电话：--
  • 电子邮件：y.barysheva@ukrorgsynth.com
  • 国家：乌克兰
  • 产品数：6230
  • 优势度：38
  • 公司名称：ENAMINE-CHI
  • 联系电话：--
  • 电子邮件：enamine@enamine.net
  • 国家：乌克兰
  • 产品数：6216
  • 优势度：67
  • 公司名称：FDICHEM
  • 联系电话：--
  • 电子邮件：sales@fdichem.com
  • 国家：乌克兰
  • 产品数：1186
  • 优势度：39
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