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Valsartan

Cat. No. M3507
Valsartan Structure
Synonym:

CGP 48933

Size Price Availability Quantity
10mg USD 35  USD35 In stock
50mg USD 100  USD100 In stock
100mg USD 140  USD140 In stock
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Quality Control & Documentation
Biological Activity

Valsartan (Diovan) is an angiotensin II receptor antagonist with IC50 of ranging from 39.5 to116 uM. By blocking the action of angiotensin, valsartan dilates blood vessels and reduces blood pressure. In the Value trial, the angiotensin II receptor blocker valsartan produced a statistically significant 19% (p=0.02) relative increase in the prespecified secondary end point of myocardial infarction (fatal and non-fatal) compared with amlodipine. The CHARM-alternative trial showed a significant +52% (p=0.025) increase in myocardial infarction with candesartan (versus placebo) despite a reduction in blood pressure.

Product Citations
Chemical Information
Molecular Weight 435.52
Formula C24H29N5O3
CAS Number 137862-53-4
Solubility (25°C) DMSO 77 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Alberto Aimo, et al. Relative Efficacy of Sacubitril-Valsartan, Vericiguat, and SGLT2 Inhibitors in Heart Failure with Reduced Ejection Fraction: a Systematic Review and Network Meta-Analysis

[2] Kieran F Docherty, et al. Sacubitril/Valsartan: Neprilysin Inhibition 5 Years After PARADIGM-HF

[3] John J V McMurray, et al. Effects of Sacubitril-Valsartan Versus Valsartan in Women Compared With Men With Heart Failure and Preserved Ejection Fraction: Insights From PARAGON-HF

[4] Renato De Vecchis, et al. Antihypertensive effect of sacubitril/valsartan: a meta-analysis

[5] Jelena P Seferovic, et al. Effect of sacubitril/valsartan versus enalapril on glycaemic control in patients with heart failure and diabetes: a post-hoc analysis from the PARADIGM-HF trial

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Keywords: Valsartan, CGP 48933 supplier, Angiotensin Receptor, inhibitors, activators


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