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Purity: ≥98%
Vericiguat (formerly BAY-1021189; BAY10-21189; Verquvo) is an orally bioavailable and potent soluble guanylate cyclase (sGC) stimulator that has been approved in 2021 by FDA to reduce the risk of cardiovascular death and heart failure (HF). Vericiguat targets the NO-sGC-cGMP pathway through a different mechanism by acting as an sGC stimulator, which enhances the current pharmacotherapy for HF.
| Targets |
sGC
|
|---|---|
| ln Vitro |
Vericiguat (0.01 μM to 100 μM) increases the concentration of recombinant sGC in a dependent manner, from 1.7 to 57.6 times. Vericiguat and the NO donor diethylamine/nitric oxide complex (DEA/NO) work in concert to enhance enzyme activity across a broad concentration range. The highest concentrations of DEA/NO (100 nM) and vericiguat (100 μM) result in 341.6-fold increase in specific activity of sGC compared to baseline. With an EC50 of 1005±145 nM, vericiguat stimulates the sGC reporter cell line concentration-dependently. With IC50 values of 798, 692, and 3072 nM, respectively, vericiguat inhibits the contractions of rabbit saphenous artery rings, rabbit aortic rings, and canine femoral vein rings induced by phenylephrine in a concentration-dependent manner. Vericiguat, with an IC50 of 956 nM, inhibits the concentration-dependent contractions of pig coronary artery rings induced by U46619[1].
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| ln Vivo |
Vericiguat (compound 24) (oral administration; 3 mg/kg, 10 mg/kg; once daily; 21 days) protects the kidneys and heart in a model of end-organ damage caused by hypertension in renin-transgenic rats treated with L-NAME. Comparing the Vericiguat-treated group to the control group, the former significantly lowers overall mortality[1].
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| Animal Protocol |
L-NAME-treated renin transgenic rats
3 mg/kg, 10 mg/kg Oral administration; 3 mg/kg, 10 mg/kg; once daily; 21 days |
| References |
| Molecular Formula |
C19H16F2N8O2
|
|---|---|
| Molecular Weight |
426.3795
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| Exact Mass |
426.14
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| Elemental Analysis |
C, 53.52; H, 3.78; F, 8.91; N, 26.28; O, 7.50
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| CAS # |
1350653-20-1
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| Appearance |
Solid powder
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| SMILES |
COC(=O)NC1=C(N=C(N=C1N)C2=NN(C3=C2C=C(C=N3)F)CC4=CC=CC=C4F)N
|
| InChi Key |
QZFHIXARHDBPBY-UHFFFAOYSA-N
|
| InChi Code |
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)
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| Chemical Name |
methyl N-[4,6-diamino-2-[5-fluoro-1-[(2-fluorophenyl)methyl]pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl]carbamate
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| Synonyms |
Vericiguat; BAY1021189; BAY-10-21189; BAY10-21189; BAY 1021189; BAY-1021189; BAY 10-21189
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 60~85 mg/mL (140.7~199.4 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.86 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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