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LY3502970

Cat. No. M21288
LY3502970 Structure
Synonym:

GLP-1 receptor agonist 1; Orforglipron

Size Price Availability Quantity
5mg USD 640  USD640 In stock
10mg USD 860  USD860 In stock
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Quality Control & Documentation
Biological Activity

LY3502970 (GLP-1 receptor agonist 1) is an orally active glucagon-like peptide (GLP-1) receptor partial agonist for studies related to type 2 diabetes and obesity.

Chemical Information
Molecular Weight 882.96
Formula C48H48F2N10O5
CAS Number 2212020-52-3
Solubility (25°C) DMSO ≥ 100 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Hui-Jun Liao, et al. Metabolites. 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

[2] Zhaotong Cong, et al. Proc Natl Acad Sci U S A. Structural basis of peptidomimetic agonism revealed by small- molecule GLP-1R agonists Boc5 and WB4-24

[3] Zhaotong Cong, et al. Nat Commun. Molecular insights into ago-allosteric modulation of the human glucagon-like peptide-1 receptor

[4] Hun Jee Choe, et al. Endocrinol Metab (Seoul). Peptidyl and Non-Peptidyl Oral Glucagon-Like Peptide-1 Receptor Agonists

[5] Takahiro Kawai, et al. Proc Natl Acad Sci U S A. Structural basis for GLP-1 receptor activation by LY3502970, an orally active nonpeptide agonist

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Keywords: LY3502970, GLP-1 receptor agonist 1; Orforglipron supplier, GLP Receptor, inhibitors, activators


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