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).
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||73 mg/mL in DMSO|
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.
|Related ROCK Products|
BDP5290 is a potent inhibitor of both ROCK and MRCK with IC50s of 5 nM, 50 nM, 10 nM and 100 nM for ROCK1, ROCK2, MRCKα and MRCKβ, respectively.
SLx-2119, also known as KD-025, is an orally bioavailable inhibitor of ROCK-II with IC50 of 105 nM.
ZINC00881524 is a potent and selective ROCK inhibitor.
|HA 1100 hydrochloride
HA 1100 hydrochloride is a cell-permeable, selective Rho-kinase inhibitor.
|Ripasudil (K-115) dihydrate
Ripasudil (K-115) hydrochloride dihydrate is potent ROCK inhibitor with IC50 of 51 nM and 19 nM for ROCK1 and ROCK2, respectively, used for the treatment of glaucoma and ocular hypertension.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.