Art. -Nr.: HY-112185

Orforglipron

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

2 Cited Publications

Kundenbewertung

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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Reinheit: 99.64%
CAS. Nr.: 2212020-52-3
Formel: C₄₈H₄₈F₂N₁₀O₅
Molecular Weight:882.96

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Orforglipron Chemical Structure

CAS. Nr.: 2212020-52-3

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (2)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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 C_max 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)	T_max (h)	C_max (ng/mL)	AUC_0-24h (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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 2212020-52-3
Appearance Solid
Molecular Weight 882.96
Formel C₄₈H₄₈F₂N₁₀O₅
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
Synonyms

LY3502970; GLP-1 receptor agonist 1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Nature

A brain reward circuit inhibited by next-generation weight-loss drugs in mice. [Abstract]

2026 Jun;654(8120):1055-1064. PMID: 42092139
bioRxiv

2024 April 30.

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.1326 mL

5.6628 mL

11.3255 mL

5 mM

0.2265 mL

1.1326 mL

2.2651 mL

10 mM

0.1133 mL

0.5663 mL

1.1326 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Pyrazolopyridine derivative having glp-1 receptor agonist effect. WO2018056453A1

[2]. Kawai T, Sun B, Yoshino H, et al. Structural basis for GLP-1 receptor activation by LY3502970, an orally active nonpeptide agonist. Proc Natl Acad Sci U S A. 2020;117(47):29959-29967. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Orforglipron

2 Cited Publications

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Orforglipron

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Publications Citing Use of MedChemExpress (MCE) Orforglipron

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Orforglipron

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

FDA-Approved Drug Library

Drug Repurposing Compound Library

Anti-diabetic Compound Library

Anti-Cardiovascular Disease Compound Library

FDA Approved & Pharmacopeial Drug Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) Orforglipron

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Orforglipron Related Classifications

HY-112185 Related Classifications