Orforglipron
Based on 2 publication(s) in Google Scholar
Orforglipron (LY3502970) (Compound 67) is an orally active agonist for Glucagon-like peptide-1 receptor (GLP-1R), which exhibits potency in ameliorates the type 2 diabete.
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- Pureza: 99.64%
- No. CAS: 2212020-52-3
- Fòrmula: C48H48F2N10O5
- Peso molecular:882.96
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) Orforglipron
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Actividad biológica
GLP-1 receptor[1]
Orforglipron is an incretin secreted from L cells of the small intestine when nutrients pass through the digestive tract, and glucose is transmitted via the GLP-1 receptor. Orforglipron exhibits various actions such as dependent gastric emptying delay, and feeding suppression[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Orforglipron (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 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 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:cynomolgus monkey model[1]
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Dosage:0.9-4.8 nM; 0.05-0.1 mg/mL
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Administration:continuous i.v. administration for 30 minutes until a plasma concentration of 0.9-4.8 nM at steady state;
i.g. for 5 days with dose of 0.05-0.1 mg/mL -
Result:Increased insulin secretion and decreased plasma-glucose. Suppressed food intake in a dose-dependent manner.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 2212020-52-3
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Appearance Solid
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Peso molecular 882.96
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Fòrmula C48H48F2N10O5
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Color White to light yellow
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SMILES
C[C@@H]1[C@](N2C3=CC=C([C@]4([H])CC(C)(OCC4)C)C=C3C=C2C(N5[C@H](C6=C(N7C(N(C8=CC=C(N(N=C9)C)C9=C8F)C=C7)=O)N(C%10=CC(C)=C(C(C)=C%10)F)N=C6CC5)C)=O)(C(N%11)=NOC%11=O)C1
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Synonyms
LY3502970; GLP-1 receptor agonist 1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Nature
2026 Jun;654(8120):1055-1064. PMID: 42092139 -
Solvente y solubilidad
DMSO : 50 mg/mL (56.63 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2 mg/mL (2.27 mM); Clear solution
This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (282 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
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- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.1326 mL | 5.6628 mL | 11.3255 mL | 28.3139 mL |
| 5 mM | 0.2265 mL | 1.1326 mL | 2.2651 mL | 5.6628 mL | |
| 10 mM | 0.1133 mL | 0.5663 mL | 1.1326 mL | 2.8314 mL | |
| 15 mM | 0.0755 mL | 0.3775 mL | 0.7550 mL | 1.8876 mL | |
| 20 mM | 0.0566 mL | 0.2831 mL | 0.5663 mL | 1.4157 mL | |
| 25 mM | 0.0453 mL | 0.2265 mL | 0.4530 mL | 1.1326 mL | |
| 30 mM | 0.0378 mL | 0.1888 mL | 0.3775 mL | 0.9438 mL | |
| 40 mM | 0.0283 mL | 0.1416 mL | 0.2831 mL | 0.7078 mL | |
| 50 mM | 0.0227 mL | 0.1133 mL | 0.2265 mL | 0.5663 mL |
Orforglipron Related Classifications
HY-112185 Related Classifications
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