Telmisartan

Catalog No.S1738 Synonyms: BIBR 277

Telmisartan  Chemical Structure

Molecular Weight(MW): 514.62

Telmisartan is an angiotensin II receptor antagonist (ARB) used in the management of hypertension.

Size Price Stock Quantity  
In DMSO USD 90 In stock
USD 70 In stock
USD 120 In stock
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Cited by 2 Publications

1 Customer Review

  • (B) Dose-response curves of each drug for acute G protein or barr activation derived from the CellKey assay. LOS: Losartan; EXP: EXP3174; TEL: Telmisartan.

    Sci Rep, 2015, 5:8116.. Telmisartan purchased from Selleck.

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Biological Activity

Description Telmisartan is an angiotensin II receptor antagonist (ARB) used in the management of hypertension.
Targets
angiotensin II receptor [1]
In vitro

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. [1] 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. [2] 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. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CHO cells MXHGeY5kfGmxbjDhd5NigQ>? MWLBcpRi\2:waYP0JIFkfGm4aYT5JIF1KGi3bXHuJGFVOSC{ZXPldJRweiCneIDy[ZN{\WRiaX6gR2hQKGOnbHzzJI1m[XO3cnXkJIFnfGW{IH;2[ZJvcWeqdDDpcoN2[mG2aX;uJIJ6KGy3Y3nm[ZJie2VicnXwc5J1\XJiZ3Xu[UBie3OjeTygTWM2OD1yLkCwNkDPxE1? M3TKWVI1PDZ{Nk[1
HepG2 cells M{XENGZ2dmO2aX;uJIF{e2G7 MWrJcohq[mm2aX;uJI9nKGyrdnXyJJN1[WenIGDsZZNud2SrdX2gZoVz\2inaTDpcoZm[3Srb36gbY4hUGWyR{KgZ4VtdHNuIFnDOVA:OC5yMkWg{txO NX7CTZVqOjJ3OE[xNlQ>
CV1 cells MXjGeY5kfGmxbjDhd5NigQ>? NELYO5RC\2:waYP0JIFkfGm4aYT5JIF1KGi3bXHuJHBRSVKpYX3tZUBmgHC{ZYPz[YQhcW5iYX\ybYNidiCpcnXlckBud26tZYmgR3YyKGOnbHzzJIJ6KEejbESgeJJidnOjY4TpeoF1cW:wIHHzd4F6NCCHQ{WwQVIvODJizszN M3;pOFIxODd7NkO2
HEK293 cells M2j4dWZ2dmO2aX;uJIF{e2G7 NWfLV3pEUW6qaXLpeIlwdiCxZjDoeY1idiCPQWTFNU1u\WSrYYTl[EBCW1BtIIXweIFs\SCneIDy[ZN{\WRiaX6gTGVMOjl|IHPlcIx{KGGodHXyJFEvPSCvaX7zJIJ6KG[udX;y[ZNk\W6lZTDhd5NigSxiSVO1NF0yPy57IN88US=> NULnOmU4OjN{NEGwNlk>

... Click to View More Cell Line Experimental Data

In vivo Telmisartan 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. [4]

Protocol

Solubility (25°C)

In vitro DMSO 13 mg/mL (25.26 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 514.62
Formula

C33H30N4O2

CAS No. 144701-48-4
Storage powder
in solvent
Synonyms BIBR 277

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03705533 Completed Drug: Telmisartan|Drug: Micardis Bioequivalence Pharmtechnology LLC|Algorithme Pharma An Altasciences Company September 7 2018 Phase 1
NCT03461081 Completed Drug: telmisartan/amlodipine and atorvastatin Hypertension With Hyperlipidemia Jeil Pharmaceutical Co. Ltd. May 7 2017 Phase 1
NCT03116516 Completed Drug: Temisartan/Amlodipine+Rosuvastatin|Drug: YHP1604 Hypertension|Hyperlipidemia Yuhan Corporation April 21 2017 Phase 1
NCT02951962 Completed Drug: Twynsta 80/5mg|Drug: Crestor 20mg Hypertension|Hyperlipidemia Yuhan Corporation August 2016 Phase 1
NCT02608242 Terminated Drug: YH22189|Drug: Twynsta 80/10mg|Drug: Crestor 20mg Hypertension|Hyperlipidemia Yuhan Corporation November 2015 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID