Vericiguat (BAY1021189) (Synonyms: BAY-1021189, MK-1242) |
| Catalog No.GC32472 |
Vericiguat(BAY1021189)(BAY1021189)는 강력한 경구 가용성 구아닐레이트 사이클라제 자극제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1350653-20-1
Sample solution is provided at 25 µL, 10mM.
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Vericiguat (BAY1021189) is a potent, orally available and soluble guanylate cyclase stimulator.
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 EC50 of 1005±145 nM. Vericiguat inhibits phenylephrine-induced contractions of rabbit saphenous artery rings, rabbit aortic rings, and canine femoral vein rings concentration dependently, with IC50 values of 798, 692, and 3072 nM, respectively. Vericiguat inhibits the U46619-induced contractions of porcine coronary artery rings concentration dependently, with an IC50 of 956 nM[1].
Chronic oral treatment with 3 or 10 mg/kg vericiguat qd results in a significant attenuation of blood pressure increase during the course of the study. However, the overall rise of blood pressure increase is not halted in the 3 and 10 mg/kg treatment groups. Vericiguat treatment at 3 or 10 mg/kg leads to a significant reduction in kidney injury molecule Kim-1 and osteopontin expression which are used as biomarkers for renal injury and dysfunction. Vericiguat results in a significant and dose-dependent increase in survival rates. In the 3 and 10 mg/kg qd treatment groups, the rat survival rate is 70% and 90%, respectively, at the study end[1].
[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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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 | |
| Synonyms | BAY-1021189, MK-1242 | ||
| Canonical SMILES | O=C(OC)NC1=C(N)N=C(C2=NN(CC3=CC=CC=C3F)C4=NC=C(F)C=C42)N=C1N | ||
| Formula | C19H16F2N8O2 | M.Wt | 426.38 |
| Solubility | DMSO : 60 mg/mL (140.72 mM);Water : < 0.1 mg/mL (insoluble) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 6 reference(s) in Google Scholar.)
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