Vericiguat (BAY1021189)

A stimulator of soluble guanylyl cyclase

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2mg

￥1200.00

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5mg

￥2375.00

1900.00

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10mg

￥3737.00

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50mg

￥10162.00

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100mg

￥14825.00

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货号: ajce49186
CAS: 1350653-20-1
别名: 维利西呱; BAY1021189
分子式: C19H16F2N8O2
分子量: 426.38
纯度: >98%
溶解度: DMSO : 60 mg/mL (140.72 mM);Water : < 0.1 mg/mL (insoluble)
储存: Store at -20°C
库存: 现货

Background

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)

Protocol

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].

参考文献:

[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.