Vericiguat

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Vericiguat

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1350653-20-1

包装与价格：

包装	价格(元)
10 mM * 1 mL in DMSO	电议
2mg	电议
5mg	电议
10mg	电议
50mg	电议
100mg	电议

产品名称

维利西呱
BAY1021189

产品介绍

Vericiguat (BAY1021189) 是有效的，有口服活性的，可溶的鸟苷酸环化酶 (guanylate cyclase) 刺激物。

生物活性

Vericiguat (BAY1021189) is a potent, orally available and solubleguanylate cyclasestimulator.

体外研究
(In Vitro)

Vericiguat (0.01 μM to 100 μM) stimulates recombinant sGC concentration dependently, by 1.7-fold to 57.6-fold. When combined with the NO donor diethylamine/nitric oxide complex (DEA/NO), vericiguat and DEA/NO have a synergistic effect on the enzyme activity over a wide range of concentrations. At highest concentrations of vericiguat (100 μM) and DEA/NO (100 nM), the specific activity of sGC is 341.6-fold above baseline. Vericiguat stimulates the sGC reporter cell line concentration dependently, with an EC₅₀of 1005±145 nM. Vericiguat inhibits phenylephrine-induced contractions of rabbit saphenous artery rings, rabbit aortic rings, and canine femoral vein rings concentration dependently, with IC₅₀values of 798, 692, and 3072 nM, respectively. Vericiguat inhibits the U46619-induced contractions of porcine coronary artery rings concentration dependently, with an IC₅₀of 956 nM^[1].

体内研究
(In Vivo)

Vericiguat (compound 24) (oral administration; 3 mg/kg, 10 mg/kg; once daily; 21 days) maintains heart and kidney function in a model of hypertension-induced end-organ damage in L-NAME-treated renin transgenic rats. Additionally,Vericiguat-treated group substantially reduces overall mortality when compared to the control group^[1].

Animal Model:	L-NAME-treated renin transgenic rats^[1]
Dosage:	3 mg/kg, 10 mg/kg
Administration:	Oral administration; 3 mg/kg, 10 mg/kg; once daily; 21 days
Result:	Resulted in a significant attenuation of blood pressure increase, however the overall rise of blood pressure increase was not halted in the 3/10 mg/kg treatment groups. Resulted a significant and dose-dependent reduction of heart hypertrophy, in both the right and left ventricle. With respect to kidney damage, Vericiguat Led to a significant reduction in kidney injury molecule Kim-1 and osteopontin expression which are used as biomarkers for renal injury and dysfunction. Resulted in a significant and dose-dependent increase in survival rates. The rat survival rate was 70% and 90%, respectively in the 3 and 10 mg/kg qd treatment groups. In contrast, the survival rate in the placebo group was only 25% after 21 days.

Clinical Trial

分子量

426.38

性状

Solid

Formula

C₁₉H₁₆F₂N₈O₂

CAS 号

1350653-20-1

中文名称

维利西呱；威利西呱

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 : 60 mg/mL(140.72 mM;Need ultrasonic)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	2.3453 mL	11.7266 mL	23.4533 mL
5 mM	0.4691 mL	2.3453 mL	4.6907 mL
10 mM	0.2345 mL	1.1727 mL	2.3453 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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 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: ≥ 2.5 mg/mL (5.86 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.86 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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

*以上所有助溶剂都可在本网站选购。