详情描述
Vericiguat (BAY1021189, Verquvo) is a potent, orally available and soluble guanylate cyclase (sGC) stimulator.
Product information
CAS Number: 1350653-20-1
Molecular Weight: 426.38
Formula: C19H16F2N8O2
Chemical Name: methyl (4,6-diamino-2-(5-fluoro-1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl)pyrimidin-5-yl)carbamate
Smiles: COC(=O)NC1C(N)=NC(=NC=1N)C1=NN(CC2=CC=CC=C2F)C2=NC=C(F)C=C12
InChiKey: QZFHIXARHDBPBY-UHFFFAOYSA-N
InChi: InChI=1S/C19H16F2N8O2/c1-31-19(30)25-14-15(22)26-17(27-16(14)23)13-11-6-10(20)7-24-18(11)29(28-13)8-9-4-2-3-5-12(9)21/h2-7H,8H2,1H3,(H,25,30)(H4,22,23,26,27)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO: 85 mg/mL(199.35 mM).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
The stimulation of sGC by Vericiguat is examined with a recombinant CHO cell line overexpressing rat sGC. Vericiguat stimulates the sGC reporter cell line concentration dependently with an EC50 of 1005 ± 145 nM. In the presence of the NO donor S-nitroso-N-acetyl-D, L-penicillamine (SNAP) (30 and 100 nM), the EC50 value shifts to 39.0 ± 5.1 and 10.6 ± 1.7 nM, respectively. In the presence of ODQ, pretreatment of the sGC reporter cell line with 10 μM ODQ for 3 h results in a significantly reduced efficacy of Vericiguat, with an EC50 of 256 ± 40 nM being observed.
In Vivo:
Vericiguat can maintain heart and kidney function in a model of hypertension-induced end-organ damage with substantially reduced overall mortality.
References:
- Markus Follmann, et al. J Med Chem. 2017 Jun 22;60(12):5146-5161.
Products are for research use only. Not for human use.