research use only

Tirzepatide (LY3298176) sodium

Cat.No.P1206

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.

Amino-acid Sequence

CAS No. 2023788-19-2 (free base)

Selleck's Tirzepatide (LY3298176) sodium Has Been Cited by 10 Publications

Quality Control

Batch: Purity: 99.96%

99.96

Chemical Information & Solubility

Storage (From the date of receipt)	3 years-20°C powder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
			1 month-20°Cin solvent

In vitro
Batch:

DMSO : 100 mg/mL (20.77 mM)；
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 3 mg/mL

Water : Insoluble

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.					In vivo Formulation Calculator
	Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.	In vivo Formulation Calculator
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	5.000mg/ml (1.04mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil	0.650mg/ml (0.14mM)	Taking the 1 mL working solution as an example, add 50 μL of 13 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

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/IC₅₀/Ki	GLP-1 receptor GIP receptor

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.

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.

References
https://pubmed.ncbi.nlm.nih.gov/32730231/ https://pubmed.ncbi.nlm.nih.gov/30473097/

References

https://pubmed.ncbi.nlm.nih.gov/32730231/
https://pubmed.ncbi.nlm.nih.gov/30473097/

Product Information

Molecular Formula	C₂₂₅H₃₄₈N₄₈O₆₈• XNa
Molecular Weight	4813.45
CAS No.	2023788-19-2 (free base)
Appearance	White Powder
Peptide Content (by %N)	≥80%
Single Impurity (by HPLC)	≤1.0%
Assay (By Anhydrous, Acetic Acid-free)	95.0~105.0%
MS	Consistent
Packing	plastic vial(dedicated for peptide packing) or glass vial, quantity according to customer's detail requirement.
Storage (From the date of receipt)	3 years-20°C powder
Shipping	Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)