Elecoglipron
Based on 1 Customer Validation
Elecoglipron (AZD5004) is an orally active small-molecule GLP-1R agonist. Its IC50 against human GLP-1R is 2.4 nM. It activates the cAMP signaling pathway in HEK293 cells overexpressing human GLP-1R with a potency of 2.1 nM, and enhances glucose-stimulated insulin secretion in EndoC-βH5 cells with an EC50 of 5.9 nM, with no detectable β-arrestin-2 recruitment or GLP-1R internalization. Elecoglipron can be used in research related to obesity, overweight and type 2 diabetes.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté : 98.26%
- CAS No.: 3011682-49-5
- Formule: C48H46F2N10O5
- Masse moléculaire:880.94
-
Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Activité biologique
-
Chemical Information
-
Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
-
Help & FAQs
Activité biologique
Description
IC50 & Target
[3]|
GLP-1 |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
2.1 nM
|
Induction of cAMP accumulation in HEK293 cells overexpressing human GLP-1R, acting as a full agonist.
Induction of cAMP accumulation in HEK293 cells overexpressing human GLP-1R, acting as a full agonist.
|
39495140 |
| CHO-K1 | EC50 |
45 nM
|
Induction of cAMP accumulation in CHO-K1 cells overexpressing human GLP-1R, acting as a partial agonist with a maximal efficacy of 30%.
Induction of cAMP accumulation in CHO-K1 cells overexpressing human GLP-1R, acting as a partial agonist with a maximal efficacy of 30%.
|
39495140 |
In Vitro
Elecoglipron acts as a full agonist of human GLP-1R in HEK293 cells, inducing cAMP accumulation with a potency of 2.1 nM[3].
Elecoglipron is a partial agonist of human GLP-1R in CHO-K1 cells, which induces cAMP accumulation with an EC50 of 45 nM and a maximum efficacy of 30%[3].
Elecoglipron does not induce β-arrestin-2 recruitment by human GLP-1R[3].
Elecoglipron does not induce internalization of human GLP-1R in U2OS cells[3].
Elecoglipron potently induces cAMP accumulation in cells expressing cynomolgus monkey GLP-1R, with an EC50 of 7.7 nM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | T1/2 | CLplasma | Vd |
|---|---|---|---|---|---|
| Cynomolgus Monkey[3] | 0.5 mg/kg | i.v. | 1.72 h | 14.4 mL/min/kg | 0.651 L/kg |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:cynomolgus monkeys (male; mean age 17.7 years; mean weight 11.4 kg; glucose disposal rate Kg below 2%)[3]
-
Dosage:5 μg/kg; 15 μg/kg; 33 μg/kg; 100 μg/kg; 160 μg/kg; 330 μg/kg
-
Administration:i.v.; single dose
-
Result:Significantly increased insulin responses and glucose disposal at 33-330 μg/kg.
Insulin AUC changes from baseline were 29998, 45067, 44721, and 37209 μU/mL*min at 33, 100, 160, and 330 μg/kg, respectively.
Kg changes were 0.31%, 0.52%, 0.52%, and 0.45%, respectively.
The exposure-based in vivo EC50 was 0.022 nM.
Glucose AUC was not significantly changed.
-
Animal Model:cynomolgus monkeys (male and female; 6 per sex per main group, 2 per sex per recovery group)[3]
-
Dosage:10 mg/kg/day; 30 mg/kg/day; 30 mg/kg/day followed by 50 mg/kg/day
-
Administration:p.o.; daily; 39 weeks; 14 days followed by weeks 3-39 (for 30 mg/kg/day then 50 mg/kg/day group)
-
Result:Dose-dependently decreased body-weight gain relative to control.
At study end, body-weight gain was reduced by 15.8%, 31.3%, and 36.5% in males and by 10.3%, 8.5%, and 11.4% in females at 10, 30, and 50 mg/kg/day, respectively.
Chemical Information
-
CAS No. 3011682-49-5
-
Appearance Solid
-
Masse moléculaire 880.94
-
Formule C48H46F2N10O5
-
Color White to off-white
-
SMILES
O=C(N1[C@H](C2=C(N3C(N(C4=CC=C(N(N=C5)C)C5=C4F)C=C3)=O)N(C6=CC(C7CC7)=C(C=C6)F)N=C2CC1)C)C8=C(N9C(C=C([C@@H]%10CC(C)(OCC%10)C)C=C9)=C8)C%11(C%12=NOC(N%12)=O)CC%11
-
Synonyms
ECC5004; AZD5004
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 50 mg/mL (56.76 mM; Need ultrasonic; 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
-
Fiche technique (299 KB)
-
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
-
Instruction de manipulation (2659 KB)
Références
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.1352 mL | 5.6758 mL | 11.3515 mL | 28.3788 mL |
| 5 mM | 0.2270 mL | 1.1352 mL | 2.2703 mL | 5.6758 mL | |
| 10 mM | 0.1135 mL | 0.5676 mL | 1.1352 mL | 2.8379 mL | |
| 15 mM | 0.0757 mL | 0.3784 mL | 0.7568 mL | 1.8919 mL | |
| 20 mM | 0.0568 mL | 0.2838 mL | 0.5676 mL | 1.4189 mL | |
| 25 mM | 0.0454 mL | 0.2270 mL | 0.4541 mL | 1.1352 mL | |
| 30 mM | 0.0378 mL | 0.1892 mL | 0.3784 mL | 0.9460 mL | |
| 40 mM | 0.0284 mL | 0.1419 mL | 0.2838 mL | 0.7095 mL | |
| 50 mM | 0.0227 mL | 0.1135 mL | 0.2270 mL | 0.5676 mL |
Elecoglipron Related Classifications
HY-159055 Related Classifications
Powered by Bioz