[CAS NO. 817194-38-0] GSK180736A

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PRODUCTS SPECIFICATIONS [817194-38-0]

Catalog

HY-18990

Brand

MCE

CAS

817194-38-0

DESCRIPTION [817194-38-0]

Overview

MDL	MFCD30533616
Molecular Weight	365.36
Molecular Formula	C19H16FN5O2
SMILES	CC(N1)=C(C(NC2=CC=C(NN=C3)C3=C2)=O)C(C4=CC=C(F)C=C4)NC1=O

For research use only. We do not sell to patients.

4 Publications Citing Use of MCE

Summary

GSK180736A is potent Rho-associated coiled-coil kinase 1 (ROCK1) inhibitor with an IC ₅₀ of 100 nM. GSK180736A is also a selective and ATP-competitive G protein-coupled receptor kinase 2 (GRK2) inhibitor with an IC ₅₀ of 0.77 μM.

IC50 & Target

ROCK1

100 nM (IC ₅₀ )

GRK2

770 nM (IC ₅₀ )

In Vitro

GSK180736A is a compound structurally similar to paroxetine that is developed as a ROCK inhibitor, is shown to be an even more potent and selective inhibitor of GRK2 with an IC ₅₀ of 0.77 μM and more than 100-fold selectivity over other GRKs. ROCK1 is a potential therapeutic target in the treatment of cardiovascular diseases such as hypertension. GSK180736A is a weak inhibitor of PKA with an IC ₅₀ of 30 μM, but highly potent against ROCK1 (IC ₅₀ =100 nM) ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : ≥ 30 mg/mL ( 82.11 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.7370 mL	13.6851 mL	27.3703 mL
5 mM	0.5474 mL	2.7370 mL	5.4741 mL
10 mM	0.2737 mL	1.3685 mL	2.7370 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (6.84 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (6.84 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (6.84 mM); Clear solution

* All of the co-solvents are available by MCE.

References

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