Olmesartan medoxomil

Modify Date: 2024-01-02 14:29:32

Olmesartan medoxomil Structure
Olmesartan medoxomil structure
 Common Name Olmesartan medoxomil
CAS Number 144689-63-4 Molecular Weight 558.585
Density 1.4±0.1 g/cm3 Boiling Point 804.2±75.0 °C at 760 mmHg
Molecular Formula C29H30N6O6 Melting Point 180°C
MSDS Chinese USA Flash Point 440.2±37.1 °C

 Use of Olmesartan medoxomil


Olmesartan medoxomil is a potent and selective angiotensin AT1 receptor inhibitor with IC50 of 66.2 μM.

 Names

Name Olmesartan medoxomil
Synonym More Synonyms

 Olmesartan medoxomil Biological Activity

Description Olmesartan medoxomil is a potent and selective angiotensin AT1 receptor inhibitor with IC50 of 66.2 μM.
Related Catalog
Target

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

In Vitro Inhibition 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 Vivo The 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 Admin Mice[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

Density 1.4±0.1 g/cm3
Boiling Point 804.2±75.0 °C at 760 mmHg
Melting Point 180°C
Molecular Formula C29H30N6O6
Molecular Weight 558.585
Flash Point 440.2±37.1 °C
Exact Mass 558.222656
PSA 162.16000
LogP 5.23
Vapour Pressure 0.0±3.0 mmHg at 25°C
Index of Refraction 1.661
Storage condition -20°C Freezer

 Safety Information

Hazard Codes Xi
Risk Phrases R36/38:Irritating to eyes and skin . R41:Risk of serious damage to eyes. R38:Irritating to the skin.
Safety Phrases S37/39-S26-S39
RIDADR NONH for all modes of transport
RTECS NI4014200
HS Code 2934999090

 Synthetic Route

 Customs

HS Code 2934999090
Summary 2934999090. 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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Olmesartan Medoxomil-d6
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Trityl Olmesartan Medoxomil
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Trityl Olmesartan Medoxomil
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Dehydro Olmesartan Medoxomil
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Olmesartan Medoxomil Impurity 7
2101308-74-9
OlMesartan MedoxoMil iMpurity V
157356-74-6
olmesartan medoxomil impurity V
172875-98-8
Olmesartan medoxomil impurity 2
896419-17-3
Olmesartan Medoxomil Impurity 10
2101308-73-8
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