Efsubaglutide alfa
Based on 1 Customer Validation
Efsubaglutide alfa is a long-acting humanised GLP-1 receptor agonist. Efsubaglutide alfa binds specifically to the GLP-1 receptor, enhancing glucose-dependent insulin secretion, suppressing glucagon release, and promoting β-cell proliferation and increased β-cell mass. Efsubaglutide alfa improves glucose tolerance, increases pancreatic insulin content, and enhances β-cell secretory responses in isolated human islets. Efsubaglutide alfa reduces liver steatosis, lowers NAFLD Activity Scores, improves perisinusoidal collagen features, reduces serum ALT and AST levels, improves fasting glucose and triglyceride levels, and reduces body weight, liver weight and liver-to-body weight ratio. Efsubaglutide alfa can be used for the research of type 2 diabetes. Efsubaglutide alfa can be used for the research of metabolic dysfunction-associated steatohepatitis.
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 : 95.67%
- CAS 番号: 2803875-75-2
- 分子量:59.695 kDa
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
Isotype
[GCG (glucagon) (Pr98-127)]2 - IGHG2 Fc
Species Reactivity
Human
IC50 & Target
GLP-1 receptor[1]
体外実験
Efsubaglutide alfa enhances β-cell secretory responses, elevates β-cell proliferation, and increases β-cell mass in isolated human islets in culture[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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:C57BL/6J (male, 18 weeks old, diet-induced obese, body weight >40 g)[2]
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Dosage:0.290 mg/kg (low dose); 0.290 mg/kg (days 0-6) then 0.871 mg/kg (days 7-41) (medium dose); 0.290 mg/kg (days 0-6) then 0.871 mg/kg (days 7-13) then 1.306 mg/kg (days 14-41) (high dose)
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Administration:s.c.; twice weekly; 41 days
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Result:Reduced body weight by 18.93% (low dose), 25.54% (medium dose), 27.99% (high dose) by day 41.
Reduced liver weight and liver-to-body weight ratio across all doses; medium and high doses resulted in lower liver weights (839.4 mg and 839.7 mg, respectively) and liver-to-body weight ratios (2.53% and 2.64%, respectively) than semaglutide.
Decreased hepatic triglyceride (TG) and total cholesterol (TC) levels with low and high doses; reduced hepatic TG levels only with medium dose.
Reduced steatosis scores to 1.4 (low dose), 1.6 (medium dose), 1.3 (high dose).
Lowered NAFLD Activity Score (NAS) to 3.3 (low dose) and 3.0 (high dose) versus MASH controls' 4.5.
Reduced perisinusoidal collagen content (%PS) to 0.30% (low dose), 0.27% (medium dose), 0.30% (high dose) versus MASH controls' 0.40%.
Reduced the number of thin perisinusoidal collagen fibre bundles (ThinStrPS) to 8.99 (low dose), 7.99 (medium dose), 8.25 (high dose).
Reduced hepatic α-SMA expression with high dose.
Reduced serum alanine aminotransferase (ALT) levels to 54.4 U/L (low dose), 67.5 U/L (medium dose), 55.9 U/L (high dose).
Reduced serum aspartate aminotransferase (AST) levels to 101.0 U/L (low dose), 121.2 U/L (medium dose), 104.9 U/L (high dose).
Reduced fasting blood glucose to 6.19 mmol/L (low dose), 5.02 mmol/L (medium dose), 5.28 mmol/L (high dose); medium and high doses produced greater reductions than semaglutide.
Reduced serum insulin levels to 1.35 ng/mL (high dose).
Reduced serum TC, low-density lipoprotein cholesterol (LDL-c), and high-density lipoprotein cholesterol (HDL-c) levels across all doses; reduced serum TG levels with low and high doses.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
遺伝子ID
アクセッション番号
Target
GLP1R
Conjugated
Unconjugated
Reconsititution
The product can be reconstituted/diluted with sterile PBS or saline.
Format
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[PEPTIDE]2-FC
アプリケーション
ELISA, FACS, Functional assay
Verified Bioactivity
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Immobilized GLP1R Protein, Human (HEK293, N-His, C-Myc, HY-P700468) can bind Efsubaglutide alfa. The EC50 for this effect is 56.05 ng/mL.
化学情報
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CAS 番号 2803875-75-2
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性状 Liquid
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分子量 59.695 kDa
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Color Colorless to light yellow
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SMILES
[Efsubaglutide alfa]
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別名
YN011; YN012; YN015
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輸送条件
Shipping with dry ice.
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Formulation
Please refer to the lot-specific COA for specific buffer information.
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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
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データシート (263 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Inhibitory Antibodies User Guide (603 KB)
参考文献
[1]. Jia W, Gao F, Lu J, Cheng Z, Dong X, Shi X, Su X, Li L, Zhang W, Wang Y, Ma J. Efsubaglutide alfa added to metformin improves glycaemia with β-cell functional responses in type 2 diabetes: a randomised, double-blind, placebo-controlled, two-stage adaptive phase 2b/3 trial (SUPER 2). Nature Communications. 2026 May 8. [Content Brief]
[2]. Wang Y, et al. Efsubaglutide Alfa attenuates metabolic dysfunction-associated steatohepatitis in mice with improvements in second harmonic generation-derived fibrosis features. Diabetes, obesity & metabolism. 2026 Apr;28(4):3070-3081. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)