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Orforglipron  (Synonyms: LY3502970; GLP-1 receptor agonist 1)

Cat. No.: HY-112185 Purity: 99.80%
COA Handling Instructions

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.

For research use only. We do not sell to patients.

Orforglipron Chemical Structure

Orforglipron Chemical Structure

CAS No. : 2212020-52-3

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 233 In-stock
Solution
10 mM * 1 mL in DMSO USD 233 In-stock
Solid
5 mg USD 150 In-stock
10 mg USD 240 In-stock
25 mg USD 450 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Orforglipron:

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Orforglipron

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1].

IC50 & Target

GLP-1 receptor[1]

In Vitro

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.

In Vivo

Orforglipron (0.94-4.8 nM in plasma concentration, i.v., or 0.05-0.1 mg/mL, i.g. for 5 days) suppresses food intake in a dose-dependent manner, promotes insulin secretion and decreases blood glucose in cynomolgus monkey model[1].
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.

Animal Model: cynomolgus monkey model[1]
Dosage: 0.9-4.8 nM; 0.05-0.1 mg/mL
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.
Clinical Trial
Molecular Weight

882.96

Formula

C48H48F2N10O5

CAS No.
Appearance

Solid

Color

White to light yellow

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (113.26 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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.1326 mL 5.6628 mL 11.3255 mL
5 mM 0.2265 mL 1.1326 mL 2.2651 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2 mg/mL (2.27 mM); Clear solution

    This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.80%

References

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
60 mM 0.0189 mL 0.0944 mL 0.1888 mL 0.4719 mL
80 mM 0.0142 mL 0.0708 mL 0.1416 mL 0.3539 mL
100 mM 0.0113 mL 0.0566 mL 0.1133 mL 0.2831 mL
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Orforglipron Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Orforglipron
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