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GSK2982772

Cat. No. M9625
GSK2982772 Structure
Synonym:

GSK772

Size Price Availability Quantity
5mg USD 176  USD176 In stock
10mg USD 264  USD264 In stock
100mg USD 1384  USD1384 In stock
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Quality Control & Documentation
Biological Activity

GSK2982772 is a potent inhibitor of selective receptor interaction protein kinase 1 (RIPK1), with IC50 values of 16 nM and 20 nM for human and monkey RIP1, respectively. GSK2982772 binds effectively to RIP1, has sensitive kinase specificity, and has excellent activity in blocking many TNF-dependent cellular responses. RIP1 is an important upstream kinase that has been shown to regulate inflammation through specific functions of scaffold and kinase. In vivo, GSK2982772 showed good free fractions in the blood of rats (4.2%), dogs (11%), cynomolgus monkeys (11%), and humans (7.4%).

Chemical Information
Molecular Weight 377.40
Formula C20H19N5O3
CAS Number 1622848-92-3
Solubility (25°C) DMSO ≥ 60 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] Philip A Harris, et al. J Med Chem. Discovery of a First-in-Class Receptor Interacting Protein 1 (RIP1) Kinase Specific Clinical Candidate (GSK2982772) for the Treatment of Inflammatory Diseases

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Keywords: GSK2982772, GSK772 supplier, Necroptosis, inhibitors, activators


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