Elecoglipron
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.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 3011682-49-5
- 分子式: C48H46F2N10O5
- 分子量:880.94
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
IC50 & Target
[3]|
GLP-1 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
2.1 nM
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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.
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39495140 |
| CHO-K1 | EC50 |
45 nM
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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%.
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39495140 |
体外実験
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 |
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:cynomolgus monkeys (male; mean age 17.7 years; mean weight 11.4 kg; glucose disposal rate Kg below 2%)[3]
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Dosage:5 μg/kg; 15 μg/kg; 33 μg/kg; 100 μg/kg; 160 μg/kg; 330 μg/kg
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Administration:i.v.; single dose
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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.
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Animal Model:cynomolgus monkeys (male and female; 6 per sex per main group, 2 per sex per recovery group)[3]
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Dosage:10 mg/kg/day; 30 mg/kg/day; 30 mg/kg/day followed by 50 mg/kg/day
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Administration:p.o.; daily; 39 weeks; 14 days followed by weeks 3-39 (for 30 mg/kg/day then 50 mg/kg/day group)
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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.
化学情報
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CAS 番号 3011682-49-5
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分子量 880.94
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分子式 C48H46F2N10O5
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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
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別名
ECC5004; AZD5004
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Elecoglipron 関連分類
HY-159055 関連分類
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