ChemicalBook CAS DataBase List 2212020-52-3

2212020-52-3

Name	GLP-1 receptor agonist 1
CAS	2212020-52-3
EINECS(EC#)	278-636-5
Molecular Formula	C48H48F2N10O5
Molecular Weight	882.97
MOL File	2212020-52-3.mol

Chemical Properties

density	1.50±0.1 g/cm3(Predicted)
storage temp.	Store at -20°C
solubility	DMSO : 125 mg/mL (141.57 mM)
form	Solid
pka	7.33±0.20(Predicted)
color	Off-white to light yellow
InChIKey	USUWIEBBBWHKNI-BBGRWQLENA-N

Hazard Information

Description

Orforglipron (LY3502970) (GLP-1 receptor agonist 1) is GLP-1 receptor agonist extracted from patent WO2018056453A1, Compound 67.

History

Orforglipron is an oral, non-peptide, small-molecule glucagon-like peptide-1 receptor agonist developed by Eli Lilly and Company as a weight-loss drug. Currently, the drug is still in Phase III clinical trials and has not yet received approval from the U.S. Food and Drug Administration (FDA). Eli Lilly's CEO expects the FDA to approve its investigational oral weight-loss drug, orforglipron, by March 2026, and to submit an application for the treatment of type 2 diabetes by the end of 2026.

Uses

Glucagon-like peptide-1 (GLP-1) agonists (also known as GLP-1 receptor agonists, incretin mimetics, or GLP-1 analogs) represent a class of medications used to treat type 2 diabetes mellitus and, in some cases, obesity.

in vivo

Orforglipron (0.94-4.8 nM in plasma concentration, i.v., or 0.05-0.1 mg/mL, i.g. for 5 days) suppresses food intake in a dose-dependent manner, promotes insulin secretion and decreases blood glucose in cynomolgus monkey model^[1].
Orforglipron (0.05-1.35 mg/kg, i.g.) reaches C_max 2 hours after administration at all doses, exhibits proportional ratio of increase in plasma drug exposure to dose increase, indicates a dose-dependent absorption in the gastrointestinal tract^[1].

Pharmacokinetic Analysis of Orforglipron in cynomolgus monkey ^[1]

route	Dose (mg/kg)	T_max (h)	C_max (ng/mL)	AUC_0-24h (ng·h/mL)
i.g.	0.05	2.0	4.78	23.7
i.g.	0.15	2.0	20.7	135
i.g.	0.45	2.0	32.0	208
i.g.	1.35	2.0	148	1040

Animal Model:	cynomolgus monkey model^[1]
Dosage:	0.9-4.8 nM; 0.05-0.1 mg/mL
Administration:	continuous i.v. administration for 30 minutes until a plasma concentration of 0.9-4.8 nM at steady state; i.g. for 5 days with dose of 0.05-0.1 mg/mL
Result:	Increased insulin secretion and decreased plasma-glucose. Suppressed food intake in a dose-dependent manner.

Spectrum Detail

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