Deziglipel
Based on 1 Customer Validation
Deziglipel (MKP10241) is an orally active GPR119 agonist (human EC50: 3.7 nM; IC50 > 7.2 μM). Deziglipel activates GPR119 to increase cAMP levels, promotes active GLP-1 release, reduces blood glucose and HbA1c, decreases body weight and feed intake, and resolves MASH via altered lipid, cytokine, and liver enzyme levels. Deziglipel shows low hERG channel inhibition, minimal CYP450 inhibition, no PXR activation, and no significant transporter inhibition. Deziglipel can be used for the research of type 2 diabetes mellitus, obesity, MASH/MASLD, and metabolic disorders.
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 : 98.06%
- CAS 番号: 2137977-29-6
- 分子式: C24H27FN6O3S2
- 分子量:530.64
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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
- プロトコル
- 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
体外実験
Deziglipel (> 30 μM) exhibits minimal hERG channel inhibition, with an IC50 > 30 μM, indicating low potential for cardiotoxicity[1].
Deziglipel (> 7.2 μM) does not inhibit major CYP450 enzymes, with IC50 values > 7.2 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | AUC0-last | Tmax | Bioavailability | T1/2 | CL | Vss | Cmax |
|---|---|---|---|---|---|---|---|---|---|
| Mice[1] | 2 mg/kg | i.v. | / | / | / | 5.31 h | 5.71 mL/min/kg | 1.38 L/kg | / |
| Mice[1] | 10 mg/kg | p.o. | 14738.22 ng/mL·h | 0.50 h | 58 % | 5.3 h | / | / | 3700 ng/mL |
| Rat[1] | 2 mg/kg | i.v. | / | / | / | 11.95 h | 5.76 mL/min/kg | 3.96 L/kg | / |
| Rat[1] | 10 mg/kg | p.o. | 11722.5 ng/mL·h | 0.42 h | 46 % | / | / | / | / |
| Dog[1] | 2 mg/kg | i.v. | / | / | / | 20.72 h | 4.50 mL/min/kg | 6.62 L/kg | / |
| Dog[1] | 10 mg/kg | p.o. | 35300 ng/mL·h | 3.00 h | 60 % | / | / | / | / |
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:db/db (male, 8-10 weeks of age)[1]
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Dosage:10 mg/kg; 30 mg/kg
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Administration:p.o.; once daily for 21 days
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Result:Produced glucose AUC reductions of 25% on day 1 and 38% on day 22 at 10 mg/kg relative to vehicle control.
Produced 12% reduction in FPG and 2.6% reduction in HbA1c after 21 days at 10 mg/kg relative to vehicle control.
Produced glucose AUC reductions of 31% on day 1 and 28% on day 22 at 30 mg/kg relative to vehicle control.
Produced 20% reduction in FPG and 3.0% reduction in HbA1c after 21 days at 30 mg/kg relative to vehicle control.
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Animal Model:C57BL/6J diet-induced obese (DIO) (male, 17-18 weeks of age, 11-12 weeks on high-fat diet)[1]
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Dosage:51.25 mg/kg; 102.45 mg/kg
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Administration:p.o.; once daily for 56 days
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Result:Inhibited body weight gain from day 1, reduced feed intake, decreased total cholesterol, LDL cholesterol, epididymal fat weight, subcutaneous fat pad weight, and liver weight, and increased plasma leptin levels at 51.25 mg/kg relative to vehicle control.
Produced significant body weight loss starting on day 10 (maximum reduction on day 14), prevented further weight gain throughout the study, reduced feed intake by a maximum of 35%, decreased total cholesterol, LDL cholesterol, epididymal fat weight, subcutaneous fat pad weight, and liver weight, and increased plasma leptin levels at 102.45 mg/kg relative to vehicle control.
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Animal Model:C57BL/6J STAM (male, metabolic dysfunction-associated steatohepatitis model)[1]
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Dosage:30 mg/kg
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Administration:p.o.; once daily for 112 days
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Result:Significantly reduced fasting blood glucose, plasma ALT levels, plasma TNF-α levels, plasma cholesterol levels, and plasma LDL levels relative to disease control.
Significantly reduced liver steatosis, inflammation, fibrosis, and the NAFLD Activity Score relative to disease control.
化学情報
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CAS 番号 2137977-29-6
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性状 Solid
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分子量 530.64
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分子式 C24H27FN6O3S2
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Color White to off-white
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SMILES
C[C@@H](C1CCN(CC1)C2=NC=C(C=N2)CC)OC(S3)=NN4C3=NC(C5=CC=C(C=C5F)S(C)(=O)=O)=C4
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別名
MKP10241
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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
体外:
DMSO : 25 mg/mL (47.11 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)
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 (280 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- 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 | 1.8845 mL | 9.4226 mL | 18.8452 mL | 47.1129 mL |
| 5 mM | 0.3769 mL | 1.8845 mL | 3.7690 mL | 9.4226 mL | |
| 10 mM | 0.1885 mL | 0.9423 mL | 1.8845 mL | 4.7113 mL | |
| 15 mM | 0.1256 mL | 0.6282 mL | 1.2563 mL | 3.1409 mL | |
| 20 mM | 0.0942 mL | 0.4711 mL | 0.9423 mL | 2.3556 mL | |
| 25 mM | 0.0754 mL | 0.3769 mL | 0.7538 mL | 1.8845 mL | |
| 30 mM | 0.0628 mL | 0.3141 mL | 0.6282 mL | 1.5704 mL | |
| 40 mM | 0.0471 mL | 0.2356 mL | 0.4711 mL | 1.1778 mL |
Deziglipel 関連分類
HY-178780 関連分類
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