Name | Valsartan |
Synonyms | Valsartan ent-Valsartan VALSARTAN IMP C Valsartan(Diovan) Valsartan R-enantiomer Valsartan Related Compound A Ambroxol Hydrochloride Imp.D (R)-2-(N-((2'-(1H-tetrazol-5-yl) N-pentanoyl-N-{[2'-(2H-tetrazol-5-yl)biphenyl-4-yl]methyl}valine (S)-N-Valeryl-N-([2'-(1H-tetrazole-5-yl)biphen-4-yl]methyl)valine N-pentanoyl-N-{[2'-(2H-tetrazol-5-yl)biphenyl-4-yl]methyl}-L-valine N-pentanoyl-N-{[2'-(2H-tetrazol-5-yl)biphenyl-4-yl]methyl}-D-valine N-((2'-(1H-Tetrazol-5-yl)-[1,1'-biphenyl]-3-yl)methyl)-N-pentanoyl-L-valine N-(1-Oxopentyl)-N-[[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-3-yl]methyl]-L-valine N-(1-OXOPENTYL)-N-[[2'-(1H-TETRAZOL-5-YL)[1,1'-BIPHENYL]-4-YL]METHYL]-L-VALINE L-Valine, N-(1-oxopentyl)-N-[[2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]- L-VALINE,N-(1-OXOPENTYL)-N-[[2''-(1H-TETRAZOL-5-YL)[1,1''-BIPHENYL]-3-YL]METHYL]- (R)-2-[N-[[2'-(5-Tetrazolyl)-4-biphenylyl]methyl]pentanamido]-3-methylbutanoic Acid D-Valine, N-(1-oxopentyl)-N-[[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]- (9CI) L-Valine, N-(1-oxopentyl)-N-[[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-3-yl]methyl]- (9CI) 3-Methyl-2-[pentanoyl-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]amino]-butanoic aci 3-methyl-2-[pentanoyl-[[4-[2-(2h-tetrazol-5-yl)phenyl]phenyl]methyl]amino]-butanoic acid (S)-2-(N-((2'-(1H-Tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)pentanamido)-3-methylbutanoic aci (R)-2-(N-((2'-(1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)pentanamido)-3-methylbutanoic acid (S)-N-(1-carboxy-2-methyl-prop-1-yl)-N-pentanoyl-N-[(2'-(1H-tetrazol-5-yl)biphenyl-4-yl)methyl]amine |
CAS | 137862-53-4 137863-60-6 137862-87-4 |
EINECS | 1592732-453-0 |
InChI | InChI=1/C24H29N5O3/c1-4-5-10-21(30)29(22(16(2)3)24(31)32)15-17-11-13-18(14-12-17)19-8-6-7-9-20(19)23-25-27-28-26-23/h6-9,11-14,16,22H,4-5,10,15H2,1-3H3,(H,31,32)(H,25,26,27,28)/t22-/m1/s1 |
InChIKey | ACWBQPMHZXGDFX-QFIPXVFZSA-N |
Molecular Formula | C24H29N5O3 |
Molar Mass | 435.52 |
Density | 1.212±0.06 g/cm3(Predicted) |
Melting Point | 116-117°C |
Boling Point | 684.9±65.0 °C(Predicted) |
Flash Point | 368°C |
Water Solubility | 84.99mg/L(25 ºC) |
Solubility | Soluble in Ethanol and Methanol |
Vapor Presure | 1.06E-19mmHg at 25°C |
Appearance | White to Brown Powder |
Color | white to tan |
Merck | 14,9916 |
pKa | 3.56±0.10(Predicted) |
Storage Condition | 2-8°C |
Stability | Hygroscopic |
Sensitive | Easily absorbing moisture |
Refractive Index | 1.586 |
MDL | MFCD00865840 |
Physical and Chemical Properties | Melting point 116-117°C |
Use | For the treatment of hypertension |
In vitro study | Valsartan dose-dependently inhibits angiotensin II-induced vasoconstriction, reducing blood pressure in a renin-dependent model of hypertension. Valsartan is at least as potent as ACE inhibitors, diuretics, beta-blockers and calcium antagonists. |
In vivo study | Valsartan resulted in improved glucose tolerance, reduced fasting blood glucose levels, and reduced serum insulin levels in Western-style diet mice. Valsartan treatment inhibits Western-style diet-induced increases in serum cytokines interferon gamma and monocyte chemoattractant protein -1. In the islets of mice, Valsartan enhances mitochondrial function and prevents the Western-style diet-induced decrease in glucose-stimulated insulin secretion. In isolated adipocytes, Valsartan blocked or attenuated changes in the expression of several key inflammatory signals caused by the Western diet: interleukin-12 p40, interleukin-12 p35, tumor necrosis factor-alpha, interferon-gamma, adiponectin, platelet 12-lipoxygenase, collagen 6, inducible NO synthase and AT1R. Valsartan significantly increases insulin-mediated 2-[3H] deoxy-d-glucose (2-[3H],DG) glucose and insulin concentrations and plasma glucose concentrations after ingestion into skeletal muscle and attenuation of glucose load. Valsartan treatment promoted insulin-induced phosphorylation of IRS-1, binding of IRS-1 to the P85 regulatory subunit of phosphoinositide 3-kinase (PI3-k), PI3-K activity, and translocation of GLUT4 to the plasma membrane. Valsartan also reduced tumor necrosis factor-α(TNF-α) expression and hyperoxidation in skeletal muscle of KK-AY mice. |
Hazard Symbols | Xi - Irritant |
Risk Codes | 36/37/38 - Irritating to eyes, respiratory system and skin. |
Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S37/39 - Wear suitable gloves and eye/face protection |
WGK Germany | 3 |
RTECS | YV9455000 |
HS Code | 29339900 |
Reference Show more | 1. Niu, Guanghao, et al. "Marein ameliorates Ang II/hypoxia‐induced abnormal glucolipid metabolism by modulating the HIF‐1α/PPARα/γ pathway in H9c2 cells." Drug Development Research 82.4 (2021): 523-532.https://doi.org/10.1002/ddr.21770 2. Niu, Guanghao, et al. "Marein ameliorates Ang II/hypoxia‐induced abnormal glucolipid metabolism by modulating the HIF‐1α/PPARα/γ pathway in H9c2 cells." Drug Development Research 82.4 (2021): 523-532.https://doi.org/10.1002/ddr.21770 3. Zhu, Zeng-Yan, et al. "Apigenin-induced HIF-1α inhibitory effect improves abnormal glucolipid metabolism in AngⅡ/hypoxia-stimulated or HIF-1α-overexpressed H9c2 cells." Phytomedicine 62 (2019): 152713.https://doi.org/10.1016/j.phymed.2018.10.010 |