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    Olmesartan Medoxomil (CS 866)
    Olmesartan Medoxomil (CS 866)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1781
    CAS #: 144689-63-4 Purity ≥98%

    Description: Olmesartan Medoxomil (formerly CS-866; Olmetec; Azor; Benicar; Olsertain), the medoxomil ester prodrug form of Olmesartan, is a potent and selective angiotensin II type 1/AT1 receptor antagonist with anti-hypertensive effects. It has been approved for use in the treatment of high blood pressure. It also inhibits the negative regulatory feedback on renin secretion. The result of receptor inhibition is vasodilation and a reduction in peripheral resistance. Olmesartan Medoxomil significantly reduces liver hydroxyproline content, and TGF-beta1.

    References: Br J Pharmacol. 2003 Jul;139(6):1085-94; J Hypertens Suppl. 2001 Jun;19(1):S3-14.

    Related CAS#: 144689-24-7 (Olmesartan); 1420880-41-6 (Olmesartan D4, RNH-6270 D4; CS-088 D4, the deuterium labeled form of Olmesartan)

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    Molecular Weight (MW)558.59 
    CAS No.144689-63-4 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 89 mg/mL (159.3 mM) 
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Other infoChemical Name: 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
    InChi Code: InChI=1S/C29H30N6O6/c1-5-8-23-30-25(29(3,4)38)24(27(36)39-16-22-17(2)40-28(37)41-22)35(23)15-18-11-13-19(14-12-18)20-9-6-7-10-21(20)26-31-33-34-32-26/h6-7,9-14,38H,5,8,15-16H2,1-4H3,(H,31,32,33,34)
    SMILES Code: O=C(C1=C(C(C)(O)C)N=C(CCC)N1CC2=CC=C(C3=CC=CC=C3C4=NN=NN4)C=C2)OCC5=C(C)OC(O5)=O 
    SynonymsOlsertain; CS866; Olmesartan medoxomil; CS 866; CS-866; Olmetec; Azor; Benicar;

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    In Vitro

    In vitro activity: Olmesartan Medoxomil significantly reduces liver hydroxyproline content, the mRNA expression of collagen alpha1(I) and alpha-smooth muscle actin (alpha-SMA), and plasma levels of transforming growth factor-beta1 (TGF-beta1). Olmesartan Medoxomil is a pro-drug containing an ester moiety that, after oral administration, is rapidly cleaved to release the active form Olmesartan (RNH-6270). Olmesartan is a highly potent, competitive and selective All AT1 receptor antagonist with almost no antagonistic activity on AT2 and AT4 receptors.

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

    In VivoOlmesartan produces a rapid and long-lasting inhibition of All-induced pressor responses in conscious rats. Oralolmesartan medoxomil also inhibits All-pressor response but onset of the action is slower compared with intravenous administration. Olmesartan Medoxomil exhibits dose-dependent antihypertensive effects in several rat and dog models, with the most marked effects seen in high plasma renin models, when compared with normal or low renin types. Olmesartan medoxomil exhibits, beside antihypertensive effects, beneficial effects in animal models of various types of nephrosis and heart failure, and anti-atherogenic effects in hyperlipidaemic animals. Olmesartan Medoxomil dose-dependently ameliorates the colonic histopathological and biochemical injuries in rats, an effect that is comparable or even better than that of the standard Sulfasalazine. Olmesartan medoxomil significantly reduces the induction of hypoxic cor pulmonale not only on echocardiographical observations but also in brain natriuretic peptide (BNP) in chronic hypoxic rats, TGF-beta and endothelin gene expressions in molecular studies. 
    Animal modelMice
    Formulation & Dosage10 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.
    ReferencesBr J Pharmacol. 2003 Jul;139(6):1085-94; J Hypertens Suppl. 2001 Jun;19(1):S3-14; Toxicol Appl Pharmacol. 2013 Aug 15;271(1):106-13.  

    These protocols are for reference only. InvivoChem does not independently validate these methods.


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