Setanaxib GKT137831; GKT831|cas:1218942-37-0|西域试剂

Setanaxib GKT137831; GKT831,99.45%

产品编号：Bellancom-12298| CAS NO：1218942-37-0| 分子式：C₂₁H₁₉ClN₄O₂| 分子量：394.85

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-12298	￥730.00	杭州北京（现货）
Bellancom-12298	￥1100.00	杭州北京（现货）
Bellancom-12298	￥1850.00	杭州北京（现货）
Bellancom-12298	￥6000.00	杭州北京（现货）
Bellancom-12298	￥8100.00	杭州北京（现货）

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Setanaxib GKT137831; GKT831

产品介绍

Setanaxib (GKT137831) 是选择性的NADPH氧化酶 (NOX1/4) 抑制剂，K_i 分别为140和110nM。

生物活性

Setanaxib (GKT137831) is a selective NADPH oxidase (NOX1/4) inhibitor with K_is of 140 and 110 nM, respectively.

体外研究

Setanaxib (GKT137831) is a potent Nox1/4 inhibitor (K_is=140±40/110±30 nM). Administration of Setanaxib (GKT137831) throughout the 72-hour period of normoxia or hypoxia exposure attenuates HPASMC proliferation under normoxic conditions at the 20 μM concentration but had no effect on proliferation in normoxic HPAECs. In the prevention paradigm, Setanaxib (GKT137831) attenuates hypoxia-induced HPASMC and HPAEC proliferation at 5 and 20 μM. Complementary assays of cell proliferation measuring the expression of PCNA or manual cell counting confirmed that Setanaxib (GKT137831) attenuates hypoxia-induced pulmonary vascular cell proliferation.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

During the last half of CCl₄ injections, some mice are treated with Setanaxib (GKT137831) daily. CCl₄-induced liver fibrosis is more pronounced in SOD1mu compared to WT mice. Liver fibrosis in both SOD1mu and WT mice is attenuated by Setanaxib (GKT137831) treatment. The increased hepatic α-SMA expression is markedly decreased in SOD1mu mice treated with Setanaxib (GKT137831), to a level similar to that of WT mice given the NOX1/4 inhibitor.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

性状

Solid

溶解性数据

In Vitro:

DMSO : 125 mg/mL (316.58 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.5326 mL	12.6630 mL	25.3261 mL
5 mM	0.5065 mL	2.5326 mL	5.0652 mL
10 mM	0.2533 mL	1.2663 mL	2.5326 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： 5% DMSO 40% PEG300 5% Tween-80 50% saline
Solubility: ≥ 2.5 mg/mL (6.33 mM); Clear solution
2.

请依序添加每种溶剂： 5% DMSO 95% (20% SBE-β-CD in saline)
Solubility: 2.5 mg/mL (6.33 mM); Suspended solution; Need ultrasonic
3.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 1.43 mg/mL (3.62 mM); Clear solution

此方案可获得 ≥ 1.43 mg/mL (3.62 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 14.3 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液