Telmisartan

Name: Telmisartan
Brand: Selleck Chemicals
SKU: S1738
Rating: 5 (4 reviews)

For research use only.

Catalog No.S1738 Synonyms: BIBR 277

4 publications

CAS No. 144701-48-4

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

Selleck's Telmisartan has been cited by 4 publications

Sci Rep, 2019, 9(1):18177

PubMed: 31796785 ( click the link to review the publication )

Neurotherapeutics, 2018, 15(2):500-510

PubMed: 29464572 ( click the link to review the publication )

Nat Commun, 2017, 8(1):573

PubMed: 28924171 ( click the link to review the publication )

Sci Rep, 2015, 5:8116

PubMed: 25631300 ( click the link to review the publication )

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.

Purity & Quality Control

Choose Selective Angiotensin Receptor Inhibitors

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	Activity Description	PMID
CHO cells	NUS3RZRnTnWwY4Tpc44h[XO\|YYm=	NWHwXpZsSW62YXfvcol{fCCjY4Tpeol1gSCjdDDoeY1idiCDVEGgdoVk\XC2b4Kg[ZhxemW\|c3XkJIlvKEOKTzDj[YxteyCvZXHzeZJm\CCjZoTldkBwfmW{bnnnbJQhcW6ldXLheIlwdiCkeTDseYNq\mW{YYPlJJJmeG:{dHXyJIdmdmViYYPzZZktKEmFNUC9NE4xODJizszN	Ml;LNlQ1PjJ4NkW=
HepG2 cells	M1\BR2Z2dmO2aX;uJIF{e2G7	M4fT[2lvcGmkaYTpc44hd2ZibHn2[ZIhe3SjZ3WgVIxie22xZHn1cUBj\XKpaHXpJIlv\mWldHnvckBqdiCKZYDHNkBk\WyuczygTWM2OD1yLkCyOUDPxE1?	NULaRVVkOjJ3OE[xNlQ>
CV1 cells	NITu[IJHfW6ldHnvckBie3OjeR?=	M3uxUGFod26rc4SgZYN1cX[rdImgZZQhcHWvYX6gVHBCWmejbX3hJIV5eHKnc4Pl[EBqdiCjZoLpZ4FvKGe{ZXXuJI1wdmuneTDDWlEh[2WubIOgZpkhT2GuNDD0doFve2GldHn2ZZRqd25iYYPzZZktKEWFNUC9Nk4xOiEQvF2=	NILlUlAzODB5OU[zOi=>
HEK293 cells	NGfGOJRHfW6ldHnvckBie3OjeR?=	M4DmWWlvcGmkaYTpc44hd2ZiaIXtZY4hVUGWRUGtcYVlcWG2ZXSgRXNRMyC3cIThb4Uh\XiycnXzd4VlKGmwIFjFT\|I6OyClZXzsd{Bi\nSncjCxMlUhdWmwczDifUBndHWxcnXzZ4Vv[2ViYYPzZZktKEmFNUC9NVcvQSEQvF2=	NXzISFdnOjN{NEGwNlk>

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	p-eNOS / eNOS / p-AMPKα / AMPKα ; PubMed: 24827148 PLoS One HUVECs were incubated with the vehicle (DMSO) or telmisartan (0.1, 1, and 10 µM) for 2 h. A representative blot is shown. p-CREB / CREB / p-p38 MAPK / p38 MAPK; PubMed: 24827148 PLoS One HUVECs were incubated with telmisartan for 15 min to 4 h to evaluate the phosphorylation levels of p38MAPK Thr180/Tyr182 and CREB Ser133. Cyclin D1 / CDK4 / CDK6 / CDK2 / Cylcin E / E2F2 ; PubMed: 28052030 Oncotarget Western blot analysis of cyclin D1, Cdk4, Cdk6, Cdk2, cyclin E, and E2F2 in OE19 and SKGT-4 cells treated with 100 μM telmisartan.	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

References

[4] Sugimoto K et al. Hypertension, 2006, 47(5), 1003-1009.

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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 Download Telmisartan SDF

Molecular Weight	514.62
Formula	C₃₃H₃₀N₄O₂
CAS No.	144701-48-4
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	BIBR 277
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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Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL， Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH₂O，mix and clarify.

Note：1.Please make sure the liquid is clear before adding the next solvent.
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Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2020-01-06)

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

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Telmisartan