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Tirzepatide

Chemical Structure : Tirzepatide

CAS No.: 2023788-19-2

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Tirzepatide (LY3298176)

Catalog No.: PC-72629Not For Human Use, Lab Use Only.

Tirzepatide (LY3298176) is a novel dual glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptor agonist, binds both receptor with high affinity (GIPR Ki=0.135; GLP-1R Ki=4.23 nM).

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Tirzepatide (LY3298176) is a novel dual glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptor agonist, binds both receptor with high affinity (GIPR Ki=0.135; GLP-1R Ki=4.23 nM).
Tirzepatide (LY3298176) is comparable to native GIP for the GIPR and approximately 5-fold weaker than native GLP-1 for the GLP-1R.
Tirzepatide (LY3298176) potently stimulates cAMP accumulation by either receptor (GIPR EC50=0.0224 nM; GLP-1R EC50=0.934 nM) in signaling studies using cell lines with recombinantly expressed GIPR or GLP-1R.
Tirzepatide (LY3298176) is less potent than the selective GLP-1RA semaglutide (Cat. PC-73177) (GLP-1R Ki=1.97 nM; cAMP EC50=0.0571 nM), and has minimal activity on the closely related glucagon receptor.
Tirzepatide (LY3298176) can induce glucose-dependent insulin secretion in vitro and in vivo through either the GIPR or the GLP-1R.

Physicochemical Properties

M.Wt 4813.45
Formula C225H348N48O68
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
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Solubility

10 mM in DMSO
Chemical Name/SMILES

Y-{Aib}-EGTFTSDYSI-{Aib}-LDKIAQ-{diacid-gamma-Glu-(AEEA)2-Lys}-AFVQWLIAGGPSSGAPPPS-NH2

References

1. Frias JP, et al. Lancet. 2018 Nov 17;392(10160):2180-2193.

2. Frias JP, et al. Diabetes Obes Metab. 2020 Jun;22(6):938-946.

3. Coskun T, et al. Mol Metab. 2018 Dec;18:3-14.

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