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Adomeglivant

Cat. No. M13966
Adomeglivant Structure
Synonym:

LY2409021

Size Price Availability
5mg USD 120  USD120 4-7 Days
10mg USD 180  USD180 4-7 Days
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Quality Control & Documentation
Biological Activity

Adomeglivant (LY2409021) is a potent, selective glucagon receptor (GluR) allosteric antagonist. Adomeglivant is widely used in the research for type 2 diabetes mellitus.

Chemical Information
Molecular Weight 555.63
CAS Number 1488363-78-5
Solubility (25°C) DMSO ≥ 90 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] Sofie Hdersdal, et al. The glucagon receptor antagonist LY2409021 has no effect on postprandial glucose in type 2 diabetes

[2] Sofie Hdersdal, et al. The Role of Glucagon in the Acute Therapeutic Effects of SGLT2 Inhibition

[3] Wyatt J Roth, et al. A Demonstration of Mixing Robustness in a Direct Compression Continuous Manufacturing Process

[4] Christof M Kazda, et al. Response to Comment on Kazda et al. Evaluation of Efficacy and Safety of the Glucagon Receptor Antagonist LY2409021 in Patients With Type 2 Diabetes: 12- and 24-Week Phase 2 Studies. Diabetes Care 2016;39:1241-1249

[5] Yong Li, et al. Efficient Synthesis of β-CF3/SCF3-Substituted Carbonyls via Copper-Catalyzed Electrophilic Ring-Opening Cross-Coupling of Cyclopropanols

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Keywords: Adomeglivant, LY2409021 supplier, Glucagon Receptor, inhibitors, activators


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