Naperiglipron
Based on 1 Customer Validation
Naperiglipron (LY3549492) is an orally active Glucagon-like peptide 1 receptor (GLP-1R) agonist with an EC50 of 1.14 nM for hGLP-1R. Naperiglipron significantly decreases the level of blood glucose in GLP-1R knock-in mouse models. Naperiglipron inhibits PDE10A1 enzyme activity (IC50: 7.43 μM) with a weak hERG inhibitory activity. Naperiglipron can be used for type II diabetes mellitus (T2DM) and obesity research.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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。
- 純度: 99.43%
- CAS 番号: 2572566-11-9
- 分子式: C33H26F2N4O4
- 分子量:580.58
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保管条件: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]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
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PDE10A1 7.43 μM (IC50) |
Naperiglipron (Example 2) causes an increase in cAMP levels in HEK293 cells, with its EC50 being 3.97 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | Vd | CL |
|---|---|---|---|---|
| Monkey1 | 0.5 mg/kg | i.v. | 1.1 L/kg | 11 mL/min/kg |
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 2572566-11-9
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性状 Solid
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分子量 580.58
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分子式 C33H26F2N4O4
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Color White to off-white
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SMILES
FC(C=C(C=C1)C#N)=C1COC2=NC(C(C(C)=C3)=CC(F)=C3CC4=NC5=CC=C(C(O)=O)C=C5N4C[C@H]6OCC6)=CC=C2
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別名
LY3549492
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 50 mg/mL (86.12 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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (272 KB)
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SDS (252 KB)
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- Français - FR (252 KB)
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- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
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 | 1.7224 mL | 8.6121 mL | 17.2242 mL | 43.0604 mL |
| 5 mM | 0.3445 mL | 1.7224 mL | 3.4448 mL | 8.6121 mL | |
| 10 mM | 0.1722 mL | 0.8612 mL | 1.7224 mL | 4.3060 mL | |
| 15 mM | 0.1148 mL | 0.5741 mL | 1.1483 mL | 2.8707 mL | |
| 20 mM | 0.0861 mL | 0.4306 mL | 0.8612 mL | 2.1530 mL | |
| 25 mM | 0.0689 mL | 0.3445 mL | 0.6890 mL | 1.7224 mL | |
| 30 mM | 0.0574 mL | 0.2871 mL | 0.5741 mL | 1.4353 mL | |
| 40 mM | 0.0431 mL | 0.2153 mL | 0.4306 mL | 1.0765 mL | |
| 50 mM | 0.0344 mL | 0.1722 mL | 0.3445 mL | 0.8612 mL | |
| 60 mM | 0.0287 mL | 0.1435 mL | 0.2871 mL | 0.7177 mL | |
| 80 mM | 0.0215 mL | 0.1077 mL | 0.2153 mL | 0.5383 mL |
Naperiglipron 関連分類
HY-177295 関連分類
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