Telmisartan - Moligand™, 10mM in DMSO , Type-1 angiotensin II receptor antagonist, CAS No.144701-48-4, Type-1 angiotensin II receptor antagonist

CAS: 144701-48-4 Cat. No.: T408976 Molecular Weight: 514.62 EC Number: 620-494-7 PubChem CID: 65999

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

BIBR 277 | 4'-​[(1,​4'-​dimethyl-​2'-​propyl[2,​6'-​bi-​1H-​benzimidazol]​-​1'-​yl)​methyl]​-[1,​1'-​biphenyl]​-​2-​carboxylic acid

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

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

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥98%

Specifications

Synonyms

BIBR 277 | 4'-​[(1, ​4'-​dimethyl-​2'-​propyl[2, ​6'-​bi-​1H-​benzimidazol]​-​1'-​yl)​methyl]​-[1, ​1'-​biphenyl]​-​2-​carboxylic acid

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

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

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

ANTAGONIST

Mechanism of action

Type-1 angiotensin II receptor antagonist

Product Properties

• ALogP: 6.9

Names and Identifiers

• Isomeric SMILES: CCCC1=NC2=C(N1CC3=CC=C(C=C3)C4=CC=CC=C4C(=O)O)C=C(C=C2C)C5=NC6=CC=CC=C6N5C
• WGK Germany: 2
• RTECS: DV2037500
• PubChem CID: 65999
• Molecular Weight: 514.62
• Reaxy-Rn: 6624054

Associated Targets(Human)

CYP2J2 Tchem Cytochrome P450 2J2 (5 Activities)

Discover Target: CYP2J2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

SLCO1B3 Tchem Solute carrier organic anion transporter family member 1B3 (1 Activities)

Discover Target: SLCO1B3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AGTR1 Tclin Type-1 angiotensin II receptor (9 Activities)

Discover Target: AGTR1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AGTR2 Tchem Type-2 angiotensin II receptor (1 Activities)

Discover Target: AGTR2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

GLRA1 Tclin Glycine receptor subunit alpha-1 (1 Activities)

Discover Target: GLRA1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemical and Physical Properties

• Melt Point(°C): 269 °C

References

1. Siyu Wu, Jiayi Ma, Jun Liu, Chun Liu, Su Ni, Ting Dai, Yan Wang, Yiping Weng, Hongbin Zhao, Dong Zhou, Xiubo Zhao.  (2022)  Immunomodulation of Telmisartan-Loaded PCL/PVP Scaffolds on Macrophages Promotes Endogenous Bone Regeneration.  ACS Applied Materials & Interfaces,      [PMID:35353482] [10.1021/acsami.1c24748]

2. Qingran Guan, Qisan Ma, Yanna Zhao, Xinxin Jiang, Huaizhen Zhang, Min Liu, Zhengping Wang, Jun Han.  (2021)  Cellulose derivatives as effective recrystallization inhibitor for ternary ritonavir solid dispersions: In vitro-in vivo evaluation.  CARBOHYDRATE POLYMERS,      [PMID:34560973] [10.1016/j.carbpol.2021.118562]

3. Zhuoling Zheng, Shuyu Zhang, Wudi Ma, Lingyi Zhang, Ling Huang, Wenqi Huang, Min Huang, Zhongxing Wang, Jiali Li.  (2018)  Determination of dexmedetomidine by UHPLC–MS/MS and its application to evaluate the effect of dexmedetomidine concentration on the target-controlled infusion concentration of propofol.  JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS,      [PMID:29579636] [10.1016/j.jpba.2018.03.015]

4. Lili Wang, Zhuang Ding, Zhengping Wang, Yanna Zhao, Hengqian Wu, Qipeng Wei, Lingfeng Gao, Jun Han.  (2024)  The Development of an Oral Solution Containing Nirmatrelvir and Ritonavir and Assessment of Its Pharmacokinetics and Stability.  Pharmaceutics,  16  (1): (109).  [PMID:38258119] [10.3390/pharmaceutics16010109]