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    Telmisartan (BIBR 277)
    Telmisartan (BIBR 277)

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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 #: V1775
    CAS #: 144701-48-4Purity ≥98%

    Description: Telmisartan (formerly BIBR-277; BIBR 277; BIBR277; Kinzalmono; Micardis) is a long lasting angiotensin II receptor antagonist (ARB) approved for use in the management of hypertension. Telmisartan functions as a moderately potent (EC50=4.5 μM), selective PPARγ partial agonist, activating the receptor to 25% to 30% of the maximum level achieved by the full agonists pioglitazone and rosiglitazone. Telmisartan induces adipocyte differentiation of 3T3-L1 cells and causes a 60% decrease in the expression of ACC2 in murine muscle myotubes.

    References: Hypertension. 2004 May;43(5):993-1002; Hypertension. 2006 May;47(5):1003-9.

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    Molecular Weight (MW)514.62
    FormulaC33H30N4O2
    CAS No.144701-48-4
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 13 mg/mL (25.3 mM)
    Water:<1 mg/mL
    Ethanol:<1 mg/mL
    Other info

    Chemical Name: 4'-((1,7'-dimethyl-2'-propyl-1H,3'H-[2,5'-bibenzo[d]imidazol]-3'-yl)methyl)-[1,1'-biphenyl]-2-carboxylic acid

    SMILES Code: O=C(C1=CC=CC=C1C2=CC=C(CN3C4=CC(C5=NC6=CC=CC=C6N5C)=CC(C)=C4N=C3CCC)C=C2)O

    Synonyms

    Telmisartan; BIBR277; BIBR 277; BIBR-277; Kinzalmono; Micardis;


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    In Vitro

    In vitro activity: Telmisartan functions as a moderately potent (EC50=4.5 μM), selective PPARγ partial agonist, activating the receptor to 25% to 30% of the maximum level achieved by the full agonists pioglitazone and rosiglitazone. Telmisartan induces adipocyte differentiation of 3T3-L1 cells. Telmisartan causes a 60% to 70% decrease in the expression of ACC2 in murine muscle myotubes. Telmisartan, but not candesartan, another ARB, downregulates RAGE mRNA levels in a dose-dependent manner. Telmisartan decreases basal as well as AGE-induced RAGE protein expression in Hep3B cells. Telmisartan dose-dependently inhibits AGE-induced ROS generation and subsequent CRP gene and protein induction in Hep3B cells. Telmisartan effectively facilitates differentiation of 3T3-L1 preadipocytes. Telmisartan causes a dose-dependent increase in mRNA levels for PPARgamma target genes such as aP2 and adiponectin in both differentiating adipocytes and fully differentiated adipocytes. Telmisartan attenuates 11beta-hydroxysteroid dehydrogenase type 1 mRNA level in differentiated adipocytes.  

    In VivoTelmisartan promotes increases in caloric expenditure and protects against dietary-induced weight gain in rats fed with a high-fat, high-carbohydrate diet. Telmisartan reduces the accumulation of visceral fat and decreases adipocyte size to a much greater extent than valsartan and is also associated with a significant reduction in hepatic triglyceride levels in rats fed with a high-fat, high-carbohydrate diet.
    Animal modelRats
    Formulation & Dosage
    References

    Hypertension. 2004 May;43(5):993-1002; Hypertension. 2006 May;47(5):1003-9.


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

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