Maridebart cafraglutide
Based on 1 Customer Validation
Maridebart cafraglutide (AMG 133) is a long-acting peptide-antibody conjugate that combines GLP-1 receptor agonist with glucose-dependent insulinotropic polypeptide (GIP) receptor antagonism. Maridebart cafraglutide shows antagonist activity against human, cynomolgus monkey and rat GIPR with IC50 values of 46.4 nM, 26.5 nM, 822.3 nM, respectively. Maridebart cafraglutide shows agonist activity against human, cynomolgus monkey, rat and mouse GLP-1R with EC50 values of 24.4 pM, 5.7 pM, 2.4 pM and 123 pM, respectively. Maridebart cafraglutide can be used for the study of obesity and type 2 diabetes.
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: 95.48%
- CAS 番号: 2887445-76-1
- 分子量:153,514 (average)
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保管条件:
-80°C, protect from light
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生物活性
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化学情報
- 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
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GIPR 42.4 nM (IC50, Human) |
GIPR 26.5 nM (IC50, Cynomolgus monkey) |
GIPR 822.3 nM (IC50, Rat) |
GLP-1R 24.4 pM (EC50, Human) |
GLP-1R 5.7 pM (EC50, Cynomolgus monkey) |
GLP-1R 2.4 pM (EC50, Rat) |
GLP-1R 123 pM (EC50, Mice) |
Maridebart cafraglutide is an optimized GIPR/GLP-1R bispecific molecule engineered by conjugating a fully human monoclonal anti-human GIPR-Ab with two GLP-1 analogue agonist peptides using amino acid linkers[1][2].
Maridebart cafraglutide (AMG 133) functionally inhibits GIP signalling through human and cynomolgus monkey GIPR with similar potency, whereas it has more than 20-fold lower potency for inhibition of GIP signalling through rat GIPR and does not fully antagonize mouse GIPR with concentrations of up to 3 µM[1].
Maridebart cafraglutide, prolongs half-life by engaging neonatal Fc receptor (FcRn) recycling and reducing renal clearance, enabling sustained GLP-1 receptor activation with infrequent injections[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Cynomolgus Monkey (male, diet-induced obesity)[1]
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Dosage:0.25 mg/kg, 0.75 mg/kg
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Administration:s.c.; weekly; 6 weeks
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Result:Reduced body weight by 11% and 13% from baseline at the end of the treatment period, decreased total energy intake, fasting triglycerides, fasting insulin, total cholesterol, and low-density lipoprotein cholesterol.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 2887445-76-1
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性状 Liquid
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分子量 153,514 (average)
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Color Colorless to light yellow
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SMILES
[Maridebart cafraglutide]
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別名
AMG 133
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輸送条件
Shipping with dry ice.
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保管条件
-80°C, protect from light
純度とドキュメンテーション
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データシート (270 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
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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