Orforglipron hemicalcium hydrate (LY3502970, OWL-833) is a potent, selective, orally active non-peptide agonist of glucagon-like peptide-1 (GLP-1) receptor (GLP-1R) with Ki of 1 nM.
Orforglipron hemicalcium hydrate (LY3502970, OWL-833) is a potent, selective, orally active non-peptide agonist of glucagon-like peptide-1 (GLP-1) receptor (GLP-1R) with Ki of 1 nM. Orforglipron has low intrinsic efficacy for effector activation and negligible β-arrestin recruitment. Orforglipron is highly potent, displaying pharmacological bias toward the cAMP second messenger signalling pathway. Orforglipron exhibits full efficacy at reducing hyperglycaemia in experimental animals.
物理化学性质&存储条件
分子量
921.02
分子式
C48H48F2N10O5.1/2Ca.H2O
外观性状
Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility
10 mM in DMSO
Chemical Name/SMILES
3-((1S,2S)-1-(5-((S)-2,2-Dimethyltetrahydro-2H-pyran-4-yl)-2-((S)-3-(3-(4-fluoro-1-methyl-1H-indazol-5-yl)-2-oxo-2,3-dihydro-1H-imidazol-1-yl)-2-(4-fluoro-3,5-dimethylphenyl)-4-methyl-4,5,6,7-tetrahydro-2H-pyrazolo[4,3-c]pyridine-5-carbonyl)-1H-indol-1-yl)-2-methylcyclopropyl)-1,2,4-oxadiazol-5(4H)-one calcium salt hydrate (2:1:2)
参考文献
1. Kawai T, et al. Proc Natl Acad Sci U S A. 2020 Nov 24;117(47):29959-29967.
2. Cong Z, et al. Nat Commun. 2021 Jun 18;12(1):3763.
3. Kyle W Sloop, et al. Sci Transl Med. 2024 Dec 18;16(778):eadp5765.
