GKT136901 hydrochloride|cas:1254507-01-1|西域试剂

GKT136901 hydrochloride,98.02%

产品编号：Bellancom-101499A| CAS NO：1254507-01-1| 分子式：C₁₉H₁₆Cl₂N₄O₂| 分子量：403.26

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-101499A	￥500.00	杭州北京（现货）
Bellancom-101499A	￥750.00	杭州北京（现货）
Bellancom-101499A	￥1400.00	杭州北京（现货）
Bellancom-101499A	￥2000.00	杭州北京（现货）
Bellancom-101499A	￥2800.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

GKT136901 hydrochloride

产品介绍

GKT136901 hydrochloride 是一种有效的，选择性的和具有口服活性的 NADPH 氧化酶 NOX-1/4 抑制剂，K_i 值分别为 160 和 165 nM。GKT136901 hydrochloride 也是一种选择性和直接的过氧亚硝酸清除剂。GKT136901 hydrochloride 可用于糖尿病肾病，中风和神经退行性疾病的研究。GKT136901 hydrochloride 还具有抗炎症活性。

生物活性

GKT136901 hydrochloride is a potent, selective and orally active inhibitor of NADPH oxidase (NOX1/4), with K_is of 160 and 165 nM, respectively. GKT136901 hydrochloride is also a selective and direct scavenger of peroxynitrite. GKT136901 hydrochloride can be used for the research of diabetic nephropathy, stroke, and neurodegeneration. GKT136901 hydrochloride also has anti-inflammatory activity.

体外研究

GKT136901 (10 μM; 30 min) significantly attenuates high-D-glucose-induced increase in O₂^•− production and in H₂O₂ generation in MPT cells^[4].
GKT136901 (10 μM; 30 min) abolishes the effect of high D-glucose on p38MAP kinase activation in MPT cells^[4].
GKT136901 (10 μM; 2 h) attenuates methamphetamine (METH)-induced oxidative stress in HBMECs^[5].
GKT136901 (10 μM; 2 h) protects HBMECs against METH-induced blood-brain barrier (BBB) dysfunction^[5].

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

体内研究

GKT136901 (30-90 mg/kg; daily p.o. for 16 weeks) has renoprotective effects in a mouse model of Type 2 diabetes^[6].

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

Animal Model:	Male db/db and db/m mice (8 weeks)^[6]
Dosage:	30, 90 mg/kg
Administration:	Daily p.o. for 16 weeks
Result:	Reduced albuminuria, thiobarbituric acid-reacting substances (TBARS) and renal ERK1/2 phosphorylation and preserved renal structure in diabetic mice. Had no effect on plasma glucose, BP (blood pressure), and body weight.

体内研究

GKT136901 (30-90 mg/kg; daily p.o. for 16 weeks) has renoprotective effects in a mouse model of Type 2 diabetes^[6].

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

Animal Model:	Male db/db and db/m mice (8 weeks)^[6]
Dosage:	30, 90 mg/kg
Administration:	Daily p.o. for 16 weeks
Result:	Reduced albuminuria, thiobarbituric acid-reacting substances (TBARS) and renal ERK1/2 phosphorylation and preserved renal structure in diabetic mice. Had no effect on plasma glucose, BP (blood pressure), and body weight.

性状

Solid

溶解性数据

In Vitro:

DMSO : 62.5 mg/mL (154.99 mM; Need ultrasonic)

H₂O : 4 mg/mL (9.92 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.4798 mL	12.3989 mL	24.7979 mL
5 mM	0.4960 mL	2.4798 mL	4.9596 mL
10 mM	0.2480 mL	1.2399 mL	2.4798 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 (sealed storage, away from moisture)。-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 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (5.16 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.16 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (5.16 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.16 mM，饱和度未知) 的澄清溶液。
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 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明