Orforglipron hemicalcium hydrate

• CAT Number: I040027
• CAS Number: 3008544-96-2
• Molecular Formula: C48H48F2N10O5.1/2Ca.H2O
• Molecular Weight: 921.02
• Purity: ≥95%

Orforglipron hemicalcium hydrate (LY3502970 hemicalcium hydrate; GLP-1 receptor agonist 1 hemicalcium hydrate) is the calcium salt hydrate form of Orforglipron (HY-112185). Orforglipron is an orally active agonist for Glucagon-like peptide-1 receptor (GLP-1R), which exhibits potency in ameliorating the type 2 diabete[1].
Orforglipron hemicalcium hydrate (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 blood glucose reduction in cynomolgus monkey model[1].
Orforglipron hemicalcium hydrate (0.05-1.35 mg/kg, i.g.) reaches Cmax 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 hemicalcium hydrate in cynomolgus monkey [1]

route
Dose (mg/kg)
Tmax (h)
Cmax (ng/mL)
AUC0-24h (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

Reference

[1]. Pyrazolopyridine derivative having glp-1 receptor agonist effect. WO2018056453A1