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.
For research use only. We do not sell to patients.
- Purity : 95.48%
- CAS No.: 2887445-76-1
- Molecular Weight:153,514 (average)
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Storage:
-80°C, protect from light
Biological Activity
Description
IC50 & Target
[1]|
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) |
In Vitro
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. Further protocols information, click here.
Parmacokinetics
In Vivo
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.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2887445-76-1
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Appearance Liquid
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Molecular Weight 153,514 (average)
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Color Colorless to light yellow
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SMILES
[Maridebart cafraglutide]
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Synonyms
AMG 133
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Shipping
Shipping with dry ice.
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Storage
-80°C, protect from light
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Research Protocol for Metabolic Diseases
AMP-activated protein kinase, AMPK, is a conserved cellular energy sensor that responds to reduced cellular energy status and coordinates metabolism by increasing ATP-generating catabolic pathways while suppressing ATP-consuming anabolic processes. In metabolic disease research, the AMPK pathway is experimentally relevant because it regulates hepatic lipid synthesis, fatty acid oxidation, glucose production, skeletal-muscle glucose disposal, mTORC1-linked biosynthesis, autophagy, mitochondrial homeostasis, and whole-body energy balance. The central pathway logic is that energy stress, metformin, exercise-like stimulation, or direct AMPK activators increase AMPKα Thr172 phosphorylation and downstream substrate phosphorylation, including ACC and RAPTOR. Phosphorylation of ACC suppresses lipogenesis and supports fatty acid oxidation, whereas phosphorylation of RAPTOR suppresses mTORC1 signaling and links cellular energy status to growth and protein synthesis control. The pathway is linked
Purity & Documentation
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Data Sheet (275 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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Handling Instructions (2659 KB)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)