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GSK180736A

Cat. No. M5269
GSK180736A Structure
Synonym:

GSK180736

Size Price Availability Quantity
5mg USD 80 In stock
10mg USD 115 In stock
50mg USD 400 In stock
100mg USD 750 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
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).

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 365.36
Formula C19H16FN5O2
CAS Number 817194-38-0
Purity >98%
Solubility 73 mg/mL in DMSO
Storage at -20°C
References

Structure-Based Design, Synthesis, and Biological Evaluation of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors.
Waldschmidt HV, et al. J Med Chem. 2016 Apr 28;59(8):3793-807. PMID: 27050625.

Crystal Structure of G Protein-coupled Receptor Kinase 5 in Complex with a Rationally Designed Inhibitor.
Homan KT, et al. J Biol Chem. 2015 Aug 21;290(34):20649-59. PMID: 26032411.

Identification and structure-function analysis of subfamily selective G protein-coupled receptor kinase inhibitors.
Homan KT, et al. ACS Chem Biol. 2015 Jan 16;10(1):310-9. PMID: 25238254.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: GSK180736A, GSK180736 supplier, ROCK, inhibitors

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