Product Description
Diovan (Valsartan) was launched in Germany and the UK as an angiotensin Ⅱ antagonist for use as an antihypertensive agent. Biphenylbromomethyl nitrite serves as the starting material for a three step synthesis of the compound, in which the (S)- enantiomer is more active than the (R)-enantiomer. Valsartan is a nonpeptide drug which is a highly specific antagonist of the AT1 receptor and is potent and orally active. This receptor is responsible for angiotensin Ⅱ cardiovascular effects (aldosterone and catecholamine secretion, vascular constriction, positive inotropic response and renal effects). Unlike losartan, it is not a prodrug and a single daily dose is comparible in activity to the ACE drug enalapril. It also did not exhibit the coughing side effect observed with ACE inhibitors. Diovan(Valsartan) is slowly metabolized (long lasting) with its main metabolite being significantly less active. There was no evidence of rebound hypertension when drug treatment was terminated and was as effective as the dihydropyridine Ca antagonist anlodipine.
Valsartan Chemical Properties
|
Melting point |
116-117°C |
|
Boiling point |
684.9±65.0°C (Predicted) |
|
Density |
1.212±0.06 g/cm3 (Predicted) |
|
Vapor pressure |
0-0Pa at 20-25℃ |
|
Storage temp. |
2-8°C |
|
Solubility |
DMSO: ≥20mg/mL |
|
Form |
Powder |
|
pKa |
3.56±0.10 (Predicted) |
|
Color |
White to tan |
|
Optical activity |
[α]/D -55 to -70°, c = 1 in methanol |
|
Water Solubility |
84.99mg/L (25℃) |
|
Merck |
14,9916 |
|
BCS Class |
2 |
|
Stability |
Hygroscopic |
|
InChIKey |
ACWBQPMHZXGDFX-QFIPXVFZSA-N |
|
LogP |
1.2-2.8 at 25℃ and pH2.5-7 |
|
Surface tension |
59.6-68.1mN/m at 10-100mg/L and 20℃ |
|
Dissociation constant |
3.76-4.38 at 25℃ |
|
CAS DataBase Reference |
137862-53-4 (CAS DataBase Reference) |
|
EPA Substance Registry System |
L-Valine, N-(1-oxopentyl)-N-[[2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]- (137862-53-4) |
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