orforglipron
Orforglipron, also known as LY3502970, and OWL-833, is a Novel Non-Peptidyl Oral Glucagon-Like Peptide-1 (GLP-1) Receptor Agonist. LY3502970 is a partial agonist, biased toward G protein activation over β-arrestin recruitment at the GLP-1R. The molecule is highly potent and selective against other class B G protein-coupled receptors (GPCRs) with a pharmacokinetic profile favorable for oral administration. In efficacy studies, oral administration of LY3502970 resulted in glucose lowering in humanized GLP-1R transgenic mice and insulinotropic and hypophagic effects in nonhuman primates, demonstrating an effect size in both models comparable to injectable exenatide.
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Chemical Information
| Name | orforglipron |
|---|---|
| Iupac Chemical Name | 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 |
| Synonyms | LY3502970; LY 3502970; LY-3502970; OWL833; OWL 833; OWL-833; Orforglipron; |
| Molecular Formula | C48H48F2N10O5 |
| Molecular Weight | 882.96 |
| Smile | O=C1NC([C@@]2(N3C(C(N4CCC5=NN(C6=CC(C)=C(F)C(C)=C6)C(N7C=CN(C8=C(F)C9=C(N(C)N=C9)C=C8)C7=O)=C5[C@@H]4C)=O)=CC%10=C3C=CC([C@@H]%11CC(C)(C)OCC%11)=C%10)[C@@H](C)C2)=NO1 |
| InChiKey | USUWIEBBBWHKNI-KHIFEHGGSA-N |
| InChi | InChI=1S/C48H48F2N10O5/c1-25-18-32(19-26(2)40(25)49)60-42(58-16-15-57(46(58)63)37-11-10-36-33(41(37)50)24-51-55(36)7)39-28(4)56(14-12-34(39)53-60)43(61)38-21-31-20-29(30-13-17-64-47(5,6)23-30)8-9-35(31)59(38)48(22-27(48)3)44-52-45(62)65-54-44/h8-11,15-16,18-21,24,27-28,30H,12-14,17,22-23H2,1-7H3,(H,52,54,62)/t27-,28-,30-,48-/m0/s1 |
| CAS Number | 2212020-52-3 |
| Related CAS |
Ordering Information
| Packaging | Price | Availability | Purity | Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| Formulation | Solid powder |
|---|---|
| Purity | 98% Min. |
| Storage | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Solubility | Soluble in DMSO |
| Handling | |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
| HS Code |
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| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
1: Liao HJ, Tzen JTC. Investigating Potential GLP-1 Receptor Agonists in Cyclopeptides from Pseudostellaria heterophylla, Linum usitatissimum, and Drymaria diandra, and Peptides Derived from Heterophyllin B for the Treatment of Type 2 Diabetes: An In Silico Study. Metabolites. 2022 Jun 15;12(6):549. doi: 10.3390/metabo12060549. PMID: 35736482; PMCID: PMC9227353. 2: Cong Z, Zhou Q, Li Y, Chen LN, Zhang ZC, Liang A, Liu Q, Wu X, Dai A, Xia T, Wu W, Zhang Y, Yang D, Wang MW. Structural basis of peptidomimetic agonism revealed by small- molecule GLP-1R agonists Boc5 and WB4-24. Proc Natl Acad Sci U S A. 2022 May 17;119(20):e2200155119. doi: 10.1073/pnas.2200155119. Epub 2022 May 13. PMID: 35561211; PMCID: PMC9171782. 3: Cong Z, Chen LN, Ma H, Zhou Q, Zou X, Ye C, Dai A, Liu Q, Huang W, Sun X, Wang X, Xu P, Zhao L, Xia T, Zhong W, Yang D, Eric Xu H, Zhang Y, Wang MW. Molecular insights into ago-allosteric modulation of the human glucagon-like peptide-1 receptor. Nat Commun. 2021 Jun 18;12(1):3763. doi: 10.1038/s41467-021-24058-z. PMID: 34145245; PMCID: PMC8213797. 4: Choe HJ, Cho YM. Peptidyl and Non-Peptidyl Oral Glucagon-Like Peptide-1 Receptor Agonists. Endocrinol Metab (Seoul). 2021 Feb;36(1):22-29. doi: 10.3803/EnM.2021.102. Epub 2021 Feb 24. PMID: 33677922; PMCID: PMC7937847. 5: Kawai T, Sun B, Yoshino H, Feng D, Suzuki Y, Fukazawa M, Nagao S, Wainscott DB, Showalter AD, Droz BA, Kobilka TS, Coghlan MP, Willard FS, Kawabe Y, Kobilka BK, Sloop KW. Structural basis for GLP-1 receptor activation by LY3502970, an orally active nonpeptide agonist. Proc Natl Acad Sci U S A. 2020 Nov 24;117(47):29959-29967. doi: 10.1073/pnas.2014879117. Epub 2020 Nov 11. PMID: 33177239; PMCID: PMC7703558.
Chemical Structure
