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MK 0893

Cat. No. M13971
MK 0893 Structure
Size Price Availability Quantity
5mg USD 393  USD393 In stock
10mg USD 662  USD662 In stock
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Quality Control & Documentation
Biological Activity

MK 0893 is a potent and selective glucagon receptor antagonist with an IC50 of 6.6 nM.

Chemical Information
Molecular Weight 588.48
CAS Number 870823-12-4
Solubility (25°C) DMSO ≥ 33.33 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Fengbin Song, et al. Design, synthesis and structure activity relationships of indazole and indole derivatives as potent glucagon receptor antagonists

[2] Ali Jazayeri, et al. Extra-helical binding site of a glucagon receptor antagonist

[3] Hong-Ping Guan, et al. Glucagon receptor antagonism induces increased cholesterol absorption

[4] Songnian Lin, et al. A novel series of indazole-/indole-based glucagon receptor antagonists

[5] Yusheng Xiong, et al. Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes

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Keywords: MK 0893 supplier, Glucagon Receptor, inhibitors, activators

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