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GSK180736A

Cat. No. M5269
GSK180736A Structure
Synonym:

GSK180736

Size Price Availability Quantity
5mg USD 85  USD85 In stock
10mg USD 115  USD115 In stock
50mg USD 400  USD400 In stock
100mg USD 750  USD750 In stock
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Quality Control & Documentation
Biological Activity

GSK180736A exhibits a 770 nM IC50 value against GRK2 and 300-fold less potency against GRK5. It is a weak inhibitor of PKA with an IC50 of 30 μM, but highly potent against ROCK1 (IC50 = 100 nM).

Chemical Information
Molecular Weight 365.36
Formula C19H16FN5O2
CAS Number 817194-38-0
Solubility (25°C) 73 mg/mL in DMSO
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] Waldschmidt HV, et al. J Med Chem. Structure-Based Design, Synthesis, and Biological Evaluation of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors.

[2] Homan KT, et al. J Biol Chem. Crystal Structure of G Protein-coupled Receptor Kinase 5 in Complex with a Rationally Designed Inhibitor.

[3] Homan KT, et al. ACS Chem Biol. Identification and structure-function analysis of subfamily selective G protein-coupled receptor kinase inhibitors.

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Keywords: GSK180736A, GSK180736 supplier, ROCK, inhibitors, activators


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