Crotedumab
Based on 1 Customer Validation
Crotedumab (REGN1193) is a fully human IgG4 monoclonal antibody that binds and inhibits glucagon receptor (GCGR), with a KD of 0.1 nM. Crotedumab can be used for the research of diabetes.
For research use only. We do not sell to patients.
- Purity : 99.22%
- CAS No.: 1452387-69-7
- Molecular Weight:146.82 kDa
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
Isotype
Human IgG4 kappa
Recommend Isotype Controls
Species Reactivity
Human
IC50 & Target
GCGR
In Vitro
Crotedumab binds to GCGR from multiple species (mouse, rat, monkey, and humans) with high affinity (KD=0.03 nM-0.39 nM)[2].
Crotedumab inhibits Glucagon-induced signaling through GCGR with IC50s of 0.65, 3.2, 0.94 and 1.0 nM in HEK293 cells transfected with GCGR from human, monkey, mouse, and rat, respectively[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Crotedumab (10 mg/kg; a single s.c.) markedly decreases blood glucose for 18 days in diabetic ob/ob mice[2].
REGN1193 (20 mg/kg; a single i.v.) produces a robust reduction in overnight-fasted blood glucose in both the conscious and anesthetized state of diabetic cynomolgus monkeys as well as in blood glucose measured 1 hour after feeding[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Diet-induced obese (DIO) male C57BL/6NTac mice were maintained on high-fat diet[2]
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Dosage:3, 10, 30 mg/kg
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Administration:S.c. injection once weekly for 4 weeks
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Result:Markedly reduced blood glucose throughout the dosing period.
Reversibly decreased body weight during the dosing period.
Dose- and time-dependently increased glucagon and GLP-1.
Reversibly increased α-cell area.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Gene ID
Accession
Conjugated
Unconjugated
Reconsititution
The product can be reconstituted/diluted with sterile PBS or saline.
Format
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Human IgG4 kappa
Application
ELISA, FACS, Functional assay
Verified Bioactivity
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Immobilized GCGR Protein, Human can bind Crotedumab. The EC50 for this effect is 32.62 ng/mL.
Chemical Information
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CAS No. 1452387-69-7
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Appearance Liquid
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Molecular Weight 146.82 kDa
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Color Colorless to light yellow
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SMILES
[Crotedumab]
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Synonyms
REGN1193; Anti-GCGR Reference Antibody (crotedumab)
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Shipping
Shipping with dry ice.
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Formulation
Please refer to the lot-specific COA for specific buffer information.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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Data Sheet (260 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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Inhibitory Antibodies User Guide (603 KB)
References
[1]. Kostic A, et, al. A first-in-human pharmacodynamic and pharmacokinetic study of a fully human anti-glucagon receptor monoclonal antibody in normal healthy volunteers. Diabetes Obes Metab. 2018 Feb;20(2):283-291. [Content Brief]
[2]. Okamot H, et, al. Glucagon Receptor Blockade With a Human Antibody Normalizes Blood Glucose in Diabetic Mice and Monkeys. Endocrinology. 2015 Aug;156(8):2781-94. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)