Orforglipron
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MedKoo CAT#: 465530

CAS#: 2212020-52-3 (free)

Description: 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.

Chemical Structure

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Orforglipron
CAS# 2212020-52-3 (free)
Instruction

Theoretical Analysis

MedKoo Cat#: 465530
Name: Orforglipron
CAS#: 2212020-52-3 (free)
Chemical Formula: C48H48F2N10O5
Exact Mass: 882.38
Molecular Weight: 882.974
Elemental Analysis: C, 65.29; H, 5.48; F, 4.30; N, 15.86; O, 9.06

Price and Availability

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5mg USD 4650 2 Weeks
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Related CAS #: 2212020-52-3 (free)   2415797-61-2 (calcium)   2212021-26-4 (calcium hydrate)    

Synonym: LY3502970; LY 3502970; LY-3502970; OWL833; OWL 833; OWL-833; 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

InChi Key: USUWIEBBBWHKNI-KHIFEHGGSA-N

InChi Code: 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

SMILES Code: 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

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

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.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: To be determined

Shelf Life: >2 years if stored properly

Drug Formulation: To be determined

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 882.97 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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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.