CAS 144689-63-4|Olmesartan medoxomil

Introduction:Basic information about CAS 144689-63-4|Olmesartan medoxomil, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
Common NameOlmesartan medoxomil
CAS Number144689-63-4Molecular Weight558.585
Density1.4±0.1 g/cm3Boiling Point804.2±75.0 °C at 760 mmHg
Molecular FormulaC29H30N6O6Melting Point180°C
MSDSChineseUSAFlash Point440.2±37.1 °C

Names

NameOlmesartan medoxomil
SynonymMore Synonyms

Olmesartan medoxomil BiologicalActivity

DescriptionOlmesartan medoxomil is a potent and selective angiotensin AT1 receptor inhibitor with IC50 of 66.2 μM.
Related CatalogSignaling Pathways >>GPCR/G Protein >>Angiotensin ReceptorResearch Areas >>Cardiovascular Disease
Target

IC50: 66.2 μM (angiotensin II receptor)[1]

In VitroInhibition of Arachidonic acid (AA) metabolism by angiotensin II receptor blockers (ARBs) is detected in a concentration-dependent manner with IC50 of Olmesartan (66.2 μM)[1]. Olmesartan medoxomil (OLM) is a potent and selective angiotensin AT1 receptor blocker[2].
In VivoThe efficacy of Olmesartan (20 mg/kg) studied in db/db diabetic mice for a period of 12 weeks starting from week 10 to 12 of age. The db/db mice have 11.7 fold increased albuminuria in comparison to control mice at week 22 to 24 of age. Twelve weeks Olmesartan administration significantly reduces albuminuria in db/db mice by 77% as compared with placebo treated db/db mice. The albumin/creatinine ratio (ACR) is increased in db/db mice in comparison to control mice by 7.1 fold and Olmesartan treatment significantly decreases ACR by 59% in db/db mice[3].
Animal AdminMice[3] 10 to 12-week old male db/db diabetic mice with background strain C57BL/KsJ and their age-matched non-diabetic lean control mice (C57BL) are used.10 non-diabetic control mice and 10 diabetic mice are fed with placebo (0.5% sodium CMC/saline solution), and 10 diabetic mice are fed with 20 mg/kg Olmesartan (MB5704) by daily gavage for 12 weeks. Mice are monitored for blood glucose, body weight and urine output every two weeks. After treatment, mice are euthanized and trunk blood is collected and is centrifuged to obtain plasma which is aliquoted and stored at -80°C. Kidney tissues are removed from mice. For protein extraction slices of the kidney tissue are frozen in liquid nitrogen, and stored at -80°C. Other parts of the kidney tissue are fixed with 4% paraformaldehyde and embedded in paraffin for immunostaining.
References

[1]. Senda A, et al. Effects of Angiotensin II Receptor Blockers on Metabolism of Arachidonic Acid via CYP2C8. Biol Pharm Bull. 2015;38(12):1975-9.

[2]. Shah S, et al. Simultaneous Quantitative Analysis of Olmesartan Medoxomil and Amlodipine Besylate in Plasma by High-performance Liquid Chromatography Technique. J Young Pharm. 2012 Apr;4(2):88-94.

[3]. Gu J, et al. Olmesartan Prevents Microalbuminuria in db/db Diabetic Mice Through Inhibition of Angiotensin II/p38/SIRT1-Induced Podocyte Apoptosis. Kidney Blood Press Res. 2016 Nov 21;41(6):848-864.

Chemical & Physical Properties

Density1.4±0.1 g/cm3
Boiling Point804.2±75.0 °C at 760 mmHg
Melting Point180°C
Molecular FormulaC29H30N6O6
Molecular Weight558.585
Flash Point440.2±37.1 °C
Exact Mass558.222656
PSA162.16000
LogP5.23
Vapour Pressure0.0±3.0 mmHg at 25°C
Index of Refraction1.661
InChIKeyUQGKUQLKSCSZGY-UHFFFAOYSA-N
SMILESCCCc1nc(C(C)(C)O)c(C(=O)OCc2oc(=O)oc2C)n1Cc1ccc(-c2ccccc2-c2nn[nH]n2)cc1
Storage condition-20°C Freezer

Safety Information

Hazard CodesXi
Risk PhrasesR36/38:Irritating to eyes and skin . R41:Risk of serious damage to eyes. R38:Irritating to the skin.
Safety PhrasesS37/39-S26-S39
RIDADRNONH for all modes of transport
RTECSNI4014200
HS Code2934999090

Customs

HS Code2934999090
Summary2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

Articles3

More Articles
Olmesartan medoxomil reverses glomerulosclerosis in renal tissue induced by myocardial infarction without changes in renal function.

Exp. Ther. Med. 8(1) , 105-109, (2014)

The aim of the present study was to investigate the effect of olmesartan medoxomil (OLM) on renal injury in mice with myocardial infarction (MI). A total of 33 male C57/BL/6 mice were divided into a s...

Linear mixed-effects model of QTc prolongation for olmesartan medoxomil.

J. Clin. Pharmacol. , doi:10.1002/jcph.572, (2015)

The new oral angiotensin II antagonist olmesartan medoxomil: a concise overview.

J. Hum. Hypertens. 16 Suppl 2 , S13-6, (2002)

The new orally active angiotensin II (A II) type-1 receptor antagonist olmesartan medoxomil is a prodrug, which is rapidly converted in vivo to the active metabolite, olmesartan. The pharmacology, ant...

Synonyms

Benicar
MFCD00914967
(5-Methyl-2-oxo-1,3-dioxol-4-yl)methyl-4-(1-hydroxy-1-methylethyl)-2-propyl-1-{[2'-(2H-tetrazol-5-yl)biphenyl-4-yl]methyl}-1H-imidazol-5-carboxylat
1H-imidazole-5-carboxylic acid, 4-(1-hydroxy-1-methylethyl)-2-propyl-1-[[2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-, (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl ester
(5-Methyl-2-oxo-1,3-dioxol-4-yl)methyl 4-(2-hydroxy-2-propanyl)-2-propyl-1-{[2'-(1H-tetrazol-5-yl)-4-biphenylyl]methyl}-1H-imidazole-5-carboxylate
(5-Methyl-2-oxo-1,3-dioxol-4-yl)methyl 4-(2-hydroxypropan-2-yl)-2-propyl-1-{[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl}-1H-imidazole-5-carboxylate
(5-Methyl-2-oxo-1,3-dioxol-4-yl)methyl 4-(2-hydroxypropan-2-yl)-2-propyl-1-{[2'-(2H-tetrazol-5-yl)biphenyl-4-yl]methyl}-1H-imidazole-5-carboxylate
4-(1-hydroxy-1-méthyléthyl)-2-propyl-1-{[2'-(2H-tétrazol-5-yl)biphényl-4-yl]méthyl}-1H-imidazole-5-carboxylate de (5-méthyl-2-oxo-1,3-dioxol-4-yl)méthyle
Olmetec
(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl 4-(1-hydroxy-1-methylethyl)-2-propyl-1-{[2'-(2H-tetrazol-5-yl)biphenyl-4-yl]methyl}-1H-imidazole-5-carboxylate
1H-Imidazole-5-carboxylic acid, 4-(1-hydroxy-1-methylethyl)-2-propyl-1-[[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-, (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl ester
Benevas
Olmesartan Medoxomil
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