Survodutide
Based on 1 Customer Validation
Survodutide (BI 456906) is a potent, selective glucagon receptor/GLP-1 receptor (GCGR/GLP-1R) dual agonist with EC50s of 0.52 nM and 0.33 nM in CHO-K1 cells, respectively. Survodutide, a 29-amino-acid peptide, is a potent acylated peptide containing a C18 fatty acid. Survodutide has robust anti-obesity efficacy achieved by increasing energy expenditure and decreasing food intake.
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: 99.99%
- CAS 番号: 2805997-46-8
- 分子式: C181H270N44O59
- 分子量:4006.34
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保管条件:
Sealed storage, away from moisture and light.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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
生物活性
The EC50 is 0.36 nM for Survodutide (BI 456906) in the endogenous mouse GLP-1R in the insulinoma cell line MIN6, and the EC50 is 60 pM for GLP-1. In 0.5% human and mouse plasma, Survodutide shows a similar potency to that of endogenous GLP-1. For the GCGR, in 0.5% human and mouse plasma, Survodutide is 6-fold less potent (0.29 and 0.17 nM, respectively) in relation to endogenous glucagon (47 and 30 pM, respectively)[1].
Proteolytic stability of Survodutide is helped by C-terminal amidation and the introduction of a non-coded amino acid 1-aminocyclobutane-1-carboxylic acid (Ac4c) in position 2, well established as the site of proteolytic activity for dipeptidyl peptidase-4. The desired extended terminal half-life of Survodutide is achieved by the introduction of a glycine–serine linker in position 24, carrying a C18 di-acid[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Survodutide (1, 3, 10, 30, 100 nmol/kg; SC; single dose) dose-dependently reducesacute food intake in WT but not in GLP-1R KO mice (Three-week-old, male, lean NMRI outbred mice)[1].
Survodutide (1, 3, 10, 30, 100 nmol/kg; SC; single dose) engages the glucagon receptor in vivo upon single dosing, increases liver nicotinamide N-methyltransferase mRNA, and reduces plasma serine and glutamine[1].
Survodutide (SC injection) causes mean residence times of 44 and 140 h and Tmax values of 7 and 51 h obtained in mice and dogs, respectively[1].
Pharmacokinetic Parameters of Survodutide (BI 456906) in mice and dogs[1].
| Mice (20 nmol/kg; SC) | Dogs (10 nmol/kg; SC) | |
| Tmax (h) | 7 | 50.7 |
| Cmax (nM) | 84.9 | 62.0 |
| AUC0-∞ (nM∗h) | 4640 | 9540 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL6/J mice pre-fed with a 60% HFD (22 weeks)[1]
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Dosage:3, 10, 20, 30 nmol/kg
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Administration:SC; daily; 30 days
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Result:Dose-dependently reduced bodyweight from baseline by up to 32% at Day 28 at a dose of 30 nmol/kg.
化学情報
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CAS 番号 2805997-46-8
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性状 Solid
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分子量 4006.34
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分子式 C181H270N44O59
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Color White to off-white
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別名
BI 456906
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配列
His-{1-Aminocyclobutanecarboxylic acid}-Gln-Gly-Thr-Phe-Thr-Ser-Asp-Tyr-Ser-Lys-Tyr-Leu-Asp-Glu-Arg-Ala-Ala-Lys-Asp-Phe-Ile-{Lys(Gly-Gly-Ser-Gly-Ser-Gly-γGlu-C18 diacid)}-Trp-Leu-Glu-Ser-Ala-NH2
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シーケンスの短縮
H-{1-Aminocyclobutanecarboxylic acid}-QGTFTSDYSKYLDERAAKDFI-{Lys(GGSGSG-γGlu-C18 diacid)}-WLESA-NH2
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Sealed storage, away from moisture and light
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
溶剤 & 溶解度
DMSO : 100 mg/mL (24.96 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 (sealed storage, away from moisture and light). 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 (sealed storage, away from moisture and light). 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 (295 KB)
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SDS (254 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 (sealed storage, away from moisture and light). 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 |
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| DMSO | 1 mM | 0.2496 mL | 1.2480 mL | 2.4960 mL | 6.2401 mL |
| 5 mM | 0.0499 mL | 0.2496 mL | 0.4992 mL | 1.2480 mL | |
| 10 mM | 0.0250 mL | 0.1248 mL | 0.2496 mL | 0.6240 mL | |
| 15 mM | 0.0166 mL | 0.0832 mL | 0.1664 mL | 0.4160 mL | |
| 20 mM | 0.0125 mL | 0.0624 mL | 0.1248 mL | 0.3120 mL |
Survodutide 関連分類
HY-P4146 関連分類
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