GSK180736A | CAS 817194-38-0

GSK180736A

This product is for research use only, not for human use. We do not sell to patients.

For small sizes, please check our retail website as below: www.invivochem.com

Size	Price	Stock
250mg	$750	Check With Us
500mg	$1280	Check With Us
1g	$1920	Check With Us

: [email protected] [email protected]

Cat #: V2730 CAS #: 817194-38-0 Purity ≥ 98%

Description: GSK180736A (GSK-180736A) is a GRK2 inhibitor that was developed as a novel and potent Rho-associated, coiled-coil-containing protein kinase (ROCK) inhibitor which binds to GRK2 (G protein-coupled receptor kinase 2) with IC50 of 0.77 μM; G protein-coupled receptors (GPCRs) are central to many physiological processes.

References: 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.

Top Publications Citing Invivochem Products

Product Catalog 2022

Guide to Product Handling

Publications Citing InvivoChem Products

Product Promise

Physicochemical and Storage Information
Protocol
Related Biological Data
Stock Solution Preparation
Quality Control Documentation

Molecular Weight (MW)	365.36
Molecular Formula	C19H16FN5O2
CAS No.	817194-38-0
Storage	-20℃ for 3 years in powder formr
Storage	-80℃ for 2 years in solvent
Solubility In Vitro	DMSO: 73 mg/mL (199.8 mM)r
	Water:<1 mg/mLr
	Ethanol: 3 mg/mL (8.2 mM)
SMILES Code	CC(N1)=C(C(NC2=CC=C(NN=C3)C3=C2)=O)C(C4=CC=C(F)C=C4)NC1=O
Synonyms	GSK-180736A; GSK180736A; GSK 180736A

Protocol	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 IC50 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 IC50 of 30 μM, but highly potent against ROCK1 (IC50=100 nM)

These protocols are for reference only. InvivoChem does not independently validate these methods.

Preparing Stock Solutions

Solvent volume to be added	Mass (the weight of a compound)
Mother liquor concentration	1mg	5mg	10mg	20mg
1mM	2.7370 mL	13.6851 mL	27.3703 mL	54.7405 mL
5mM	0.5474 mL	2.7370 mL	5.4741 mL	10.9481 mL
10mM	0.2737 mL	1.3685 mL	2.7370 mL	5.4741 mL
20mM	0.1369 mL	0.6843 mL	1.3685 mL	2.7370 mL

Quality Control Documentation	Select Batch Purity ≥ 98% COA MSDS NMR HPLC

The molarity calculator equation

Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)

Mass

Concentration

Volume

Molecular Weight*

The dilution calculator equation

Concentration_(start) × Volume_(start) = Concentration_(final) × Volume_(final)

This equation is commonly abbreviated as: C₁ V₁ = C₂ V₂

Concentration_(start)

Volume_(start)

Concentration_(final)

Volume_(final)

Step One: Enter information below

Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals

Step Two: Enter the in vivo formulation

%DMSO + % + %Tween 80 + %ddH₂O

Calculation Results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH₂O,mix and clarify.

Note:

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.