Home GPCR & G Protein Angiotensin Receptor antagonist Telmisartan

Telmisartan

Catalog No.S1738 Synonyms: BIBR 277

For research use only.

Telmisartan (BIBR 277) is an angiotensin II receptor antagonist (ARB) used in the management of hypertension.

Telmisartan Chemical Structure

CAS No. 144701-48-4

Selleck's Telmisartan has been cited by 7 Publications

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Biological Activity

Description Telmisartan (BIBR 277) 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 NFPzeWtHfW6ldHnvckBie3OjeR?= MXLBcpRi\2:waYP0JIFkfGm4aYT5JIF1KGi3bXHuJGFVOSC{ZXPldJRweiCneIDy[ZN{\WRiaX6gR2hQKGOnbHzzJI1m[XO3cnXkJIFnfGW{IH;2[ZJvcWeqdDDpcoN2[mG2aX;uJIJ6KGy3Y3nm[ZJie2VicnXwc5J1\XJiZ3Xu[UBie3OjeTygTWM2OD1yLkCwNkDPxE1? MW[yOFQ3OjZ4NR?=
HepG2 cells Mo\FSpVv[3Srb36gZZN{[Xl? NHPCWlJKdmirYnn0bY9vKG:oIHzpeoVzKHO2YXflJHBt[XOvb3TpeY0h[mW{Z3jlbUBqdm[nY4Tpc44hcW5iSHXwS|Ih[2WubIOsJGlEPTB;MD6wNlUh|ryP MYqyNlU5PjF{NB?=
CV1 cells MX3GeY5kfGmxbjDhd5NigQ>? M4H4dWFod26rc4SgZYN1cX[rdImgZZQhcHWvYX6gVHBCWmejbX3hJIV5eHKnc4Pl[EBqdiCjZoLpZ4FvKGe{ZXXuJI1wdmuneTDDWlEh[2WubIOgZpkhT2GuNDD0doFve2GldHn2ZZRqd25iYYPzZZktKEWFNUC9Nk4xOiEQvF2= MX2yNFA4QTZ|Nh?=
HEK293 cells NFrjUHZHfW6ldHnvckBie3OjeR?= NF\3b45KdmirYnn0bY9vKG:oIHj1cYFvKE2DVFWxMY1m\GmjdHXkJGFUWCtidYD0ZYtmKGW6cILld5Nm\CCrbjDISWszQTNiY3XscJMh[W[2ZYKgNU42KG2rboOgZpkh\my3b4Lld4NmdmOnIHHzd4F6NCCLQ{WwQVE4NjlizszN MYCyN|I1OTB{OR?=
Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot p-eNOS / eNOS / p-AMPKα / AMPKα ; p-CREB / CREB / p-p38 MAPK / p38 MAPK ; Cyclin D1 / CDK4 / CDK6 / CDK2 / Cylcin E / E2F2 24827148 28052030
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 (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 514.62
Formula

C33H30N4O2
CAS No. 144701-48-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCCC1=NC2=C(N1CC3=CC=C(C=C3)C4=CC=CC=C4C(=O)O)C=C(C=C2C)C5=NC6=CC=CC=C6N5C

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05223101 Recruiting Drug: Telminone 80 mg|Drug: Drug: Micardis 80 mg Hypertension HK inno.N Corporation January 19 2022 Phase 1
NCT05040880 Completed Drug: Telmione plus 80/12.5mg|Drug: Micardis plus 80/12.5mg Hypertension HK inno.N Corporation July 8 2021 Phase 1
NCT04736329 Recruiting Drug: Telmisartan Heart Failure With Reduced Ejection Fraction|Renal Insufficiency Cairo University February 1 2021 Not Applicable
NCT05322889 Recruiting Drug: Telmisartan tablets Neuropathic Pain|Chemotherapy Effect Dr. Frank Behrens|Johann Wolfgang Goethe University Hospital|Fraunhofer Institute for Molecular Biology and Applied Ecology April 9 2020 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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