2. Antibody-drug Conjugate/ADC Related GPCR/G Protein Protein Tyrosine Kinase/RTK
  3. Antibody-Drug Conjugates (ADCs) GLP Receptor Insulin Receptor
  4. Maridebart cafraglutide

Maridebart cafraglutide  (Synonyms: AMG 133)

Cat. No.: HY-164535 Pureza: 95.48%
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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.

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Maridebart cafraglutide

Maridebart cafraglutide Estructura química

No. CAS : 2887445-76-1

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Maridebart cafraglutide Related Antibodies

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Descripciòn

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[1][2].

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.

Maridebart cafraglutide Related Antibodies
Parmacokinetics
Species Dose Route T1/2 Tmax Cmax AUClast CL/F C0 AUCinf CL
Mice[1] 5 mg/kg i.v. 206 h / / / / 109 μg/mL 13700 μg·h/mL 0.367 mL/h/kg
Cynomolgus Monkey[1] 3 mg/kg s.c. 292 h 48 h 30.4 μg/mL 13200 μg·h/mL 0.198 mL/h/kg / / /
In Vivo

Maridebart cafraglutide (0.25-0.75 mg/kg; s.c.; weekly; 6 weeks) reduces body weight and improves metabolic parameters in male cynomolgus monkeys with obesity[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Cynomolgus Monkey (male, diet-induced obesity)[1]
Dosage: 0.25 mg/kg, 0.75 mg/kg
Administration: s.c.; weekly; 6 weeks
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.
Ensayo clínico
Peso molecular

153,514 (average)

No. CAS
Appearance

Liquid

Color

Colorless to light yellow

SMILES

[Maridebart cafraglutide]
Envío

Shipping with dry ice.
Almacenamiento

-80°C, protect from light
Pureza y Documentación
Referencias
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Maridebart cafraglutide Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Maridebart cafraglutide2887445-76-1AMG 133AMG133AMG-133Antibody-Drug Conjugates (ADCs)GLP ReceptorInsulin ReceptorAntibody-Drug ConjugatesGIPRGLP-1RFc-containing scaffoldratmale obese miceHEK 293T cellsCHO-AM1D cellshumancynomolgus monkeytype 2 diabetesInhibitorinhibitorinhibit

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Nombre del producto:
Maridebart cafraglutide
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HY-164535
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