ATX inhibitor 5
目录号 : KM8598 CAS No. : 2402772-45-4 纯度 : 98%

ATX inhibitor 5 是有效的口服活性 autotaxin (ATX) 抑制剂,IC50 为 15.3 nM。AATX inhibitor 5 具有抗肝纤维化作用,并显着降低 CCl4 诱导的肝纤维化水平。

规格 价格 是否有货 数量
5mg
In-stock
10mg
In-stock
25mg
In-stock
50mg
In-stock
100mg
In-stock
200mg 询价 In-stock
500mg 询价 In-stock

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生物活性

ATX inhibitor 5 is a potent and orally active autotaxin (ATX) inhibitor, with an IC50 of 15.3 nM. ATX inhibitor 5 shows anti-hepatofibrosis effects and reduces CCl4-induced hepatic fibrosis level prominently.

体外研究

ATX inhibitor 5 (compound 10g) (IC50s=1.21 and 0.78 μM) displays activities against cardiac fibroblasts (CFs) and hepatic stellate cell (HSC).
ATX inhibitor 5 at 10 μM successfully suppresses collagen content induced by TGF-β.

Cell Proliferation Assay

Cell Line: CFs and t-HSC/Cl-6 cells
Concentration: 0.0001, 0.01, 1, 100, 10000 µM
Incubation Time: 48 hours
Result: Displayed activities against CFs and t-HSC/Cl-6 cells with IC50s of 1.21 and 0.78 µM, respectively.
体内研究

ATX inhibitor 5 (20-40 mg/kg; p.o.; once daily for two weeks) reduces CCl4-induced hepatic fibrosis level prominently.

Animal Model: Male Konmin mice (8-week old, 22-25 g)
Dosage: 20, 40 mg/kg
Administration: Orally; once daily for two weeks
Result: Prominently reduced CCl4-induced hepatic fibrosis level.
分子式
C22H18ClF3N6O
分子量
474.87
CAS号
2402772-45-4
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 250 mg/mL (526.46 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1058 mL 10.5292 mL 21.0584 mL
5 mM 0.4212 mL 2.1058 mL 4.2117 mL
10 mM 0.2106 mL 1.0529 mL 2.1058 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.38 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.38 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
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