Vericiguat (BAY1021189)
(Synonyms: 维利西呱; BAY1021189) 目录号 : GC32472
A stimulator of soluble guanylyl cyclase
Cas No.:1350653-20-1
Sample solution is provided at 25 µL, 10mM.
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Vericiguat is a stimulator of soluble guanylyl cyclase (sGC).1 It stimulates the formation of cGMP in CHO cells expressing recombinant rat sGC in the absence and presence of the nitric oxide (NO) donor SNAP , an effect that can be reversed by the sGC inhibitor ODQ . Vericiguat inhibits phenylephrine-induced contractions in isolated rabbit saphenous artery rings, rabbit aortic rings, and canine femoral vein rings (IC50s = 798, 692, and 3,072 nM, respectively), as well as decreases the coronary perfusion pressure in isolated perfused rat hearts in a concentration-dependent manner. It decreases proteinuria and increases survival in rats expressing mouse renin ((mRenR2)27), a transgenic model for hypertension, when administered at doses of 3 or 10 mg/kg. Formulations containing vericiguat have been used in the treatment of heart failure.
1.Follmann, M., Ackerstaff, J., Redlich, G., et al.Discovery of the soluble guanylate cyclase stimulator vericiguat (BAY 1021189) for the treatment of chronic heart failureJ. Med. Chem.60(12)5146-5161(2017)
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Animal experiment: |
Rats: Rat are randomly allocated to three study groups: placebo (control), 24 low dose, and 24 high dose (3 and 10 mg/kg per day, respectively, administered po by gavage qd). Blood pressure is measured via the tail-cuff method once before the start of the study (day 0) to exclude preexisting differences between the groups and on day 7, 14, and 21. Body weight and survival are assessed on day 1, 8, and 15 and at the study end. At the end of the study (day 22), all animals are anesthetized, blood is collected, and animals are sacrificed; blood is taken in order to assess plasma parameters, and the heart is dissected into the left and right ventricles and is weighed to assess potential heart hypertrophy. Creatinine, urea, and renin activity in plasma are determined after extraction[1]. |
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References: [1]. Follmann M, et al. Discovery of the Soluble Guanylate Cyclase Stimulator Vericiguat (BAY 1021189) for the Treatment of Chronic Heart Failure. J Med Chem. 2017 Jun 22;60(12):5146-5161. |
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| Cas No. | 1350653-20-1 | SDF | |
| 别名 | 维利西呱; BAY1021189 | ||
| Canonical SMILES | O=C(OC)NC1=C(N)N=C(C2=NN(CC3=CC=CC=C3F)C4=NC=C(F)C=C42)N=C1N | ||
| 分子式 | C19H16F2N8O2 | 分子量 | 426.38 |
| 溶解度 | DMSO : 60 mg/mL (140.72 mM);Water : < 0.1 mg/mL (insoluble) | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet