Tirzepatide (LY3298176) sodium

Tirzepatide (LY3298176, GIP/GLP-1 RA, TZP) sodium is a dual GIP/GLP-1 receptor agonist. Tirzepatide differentially induces internalization of the GIP and GLP-1 receptors with EC50 values of 18.2 nM and 18.1 nM, respectively.

Tirzepatide (LY3298176) sodium Chemical Structure

Tirzepatide (LY3298176) sodium Chemical Structure

CAS: 2023788-19-2 (free base)

Selleck's Tirzepatide (LY3298176) sodium has been cited by 4 publications

Purity & Quality Control

Batch: Purity: 99.96%
99.96

Choose Selective Glucagon Receptor Inhibitors

Biological Activity

Description Tirzepatide (LY3298176, GIP/GLP-1 RA, TZP) sodium is a dual GIP/GLP-1 receptor agonist. Tirzepatide differentially induces internalization of the GIP and GLP-1 receptors with EC50 values of 18.2 nM and 18.1 nM, respectively.
Targets
GLP-1 receptor [1] GIP receptor [1]
18.1 nM(EC50) 18.2 nM(EC50)
In vitro
In vitro

In HEK293 cells, Tirzepatide induces internalization of the GIPR and has a propensity toward partial agonism, and this ultimately reflects in signaling bias toward the cAMP pathway versus β-arrestin recruitment.[1]

In Vivo
In vivo

LY3298176 shows glucose-dependent insulin secretion and improves glucose tolerance by acting on both GIP and GLP-1 receptors in mice. Chronic treatment with LY3298176 results in a significant dose-dependent decrease in body weight that is more pronounced than that observed with semaglutide.[2]

Chemical lnformation & Solubility

Molecular Weight 4813.45 Formula

C225H348N48O68• XNa

CAS No. 2023788-19-2 (free base) SDF --
Density 95.0~105.0%
Storage (From the date of receipt) 3 years-20°C powder Solutions are unstable. Prepare fresh or purchase small, pre-packaged sizes. Repackage upon receipt.

In vitro
Batch:

DMSO : 100 mg/mL ( (20.77 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 3 mg/mL

Water : Insoluble


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In vivo
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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.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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