Catalog No.: PC-28324Not For Human Use, Lab Use Only.
Tirzepatide hydrochloride (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 hydrochloride (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 (free base)
Formula
C225H348N48O68.xHCl
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
Shipping
Solubility
10 mM in DMSO
Chemical Name/SMILES
Y-{Aib}-EGTFTSDYSI-{Aib}-LDKIAQ-{diacid-gamma-Glu-(AEEA)2-Lys}-AFVQWLIAGGPSSGAPPPS-NH2 hydrochloride salt
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.
