GSK180736A

Name: GSK180736A
Brand: MedChemExpress
SKU: HY-18990
Rating: 5.0 (5 reviews)

Cat. No.: HY-18990 Purity: 98.01%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

GSK180736A is potent Rho-associated coiled-coil kinase 1 (ROCK1) inhibitor with an IC₅₀ of 100 nM. GSK180736A is also a selective and ATP-competitive G protein-coupled receptor kinase 2 (GRK2) inhibitor with an IC₅₀ of 0.77 μM.

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

GSK180736A Chemical Structure

CAS No. : 817194-38-0

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 72	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 72	In-stock	Estimated Time of Arrival: December 31
Solid
2 mg	USD 60	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 90	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 120	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 400	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 750	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 5 publication(s) in Google Scholar

5 Publications Citing Use of MCE GSK180736A

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View All ROCK Isoform Specific Products:

View All Isoforms

ROCK ROCK1 ROCK2

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

ROCK1

100 nM (IC₅₀)

GRK2

770 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
BTI-TN-5B1-4	IC₅₀	0.77 μM Compound: 2	Inhibition of full length C-terminal hexahistidine tagged GRK2 (unknown origin) S670A mutant expressed in High Five cells using Bac to Bac insect cell expression system using tubulin as substrate by SDS-PAGE method Inhibition of full length C-terminal hexahistidine tagged GRK2 (unknown origin) S670A mutant expressed in High Five cells using Bac to Bac insect cell expression system using tubulin as substrate by SDS-PAGE method	[PMID: 27050625]
Sf9	IC₅₀	14 nM Compound: 1	Inhibition of human recombinant ROCK1 kinase expressed in insect Sf9 cells by SPA Inhibition of human recombinant ROCK1 kinase expressed in insect Sf9 cells by SPA	[PMID: 18842034]

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)^[1].

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

Molecular Weight

365.36

Formula

C₁₉H₁₆FN₅O₂

CAS No.

817194-38-0

Appearance

Solid

Color

Light yellow to khaki

SMILES

CC(N1)=C(C(NC2=CC=C(NN=C3)C3=C2)=O)C(C4=CC=C(F)C=C4)NC1=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : ≥ 30 mg/mL (82.11 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" 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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.84 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.01%

Select Batch:

Data Sheet (278 KB) SDS (251 KB)

COA (251 KB) RP-HPLC (260 KB)

Handling Instructions (2659 KB)

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. [Content Brief]

Cell Assay
^[1]

Cardiac myocytes are isolated from LV free wall and septum of C57/Bl6 mice. Cells are treated with isoproterenol (0.5 μM) for 2 min for the recording of contraction, with pretreatment of either PBS as vehicle or paroxetine (10 μM), 215022 (0.1, 0.5, 1, 10 μM), 215023 (0.1, 0.5, 1, 10 μM), 224064 (0.1, 0.5, 1, 10 μM), and GSK180736A ( 0.5, 1 μM), for 10 min^[1].

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

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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.7370 mL	13.6851 mL	27.3703 mL	68.4257 mL
	5 mM	0.5474 mL	2.7370 mL	5.4741 mL	13.6851 mL
	10 mM	0.2737 mL	1.3685 mL	2.7370 mL	6.8426 mL
	15 mM	0.1825 mL	0.9123 mL	1.8247 mL	4.5617 mL
	20 mM	0.1369 mL	0.6843 mL	1.3685 mL	3.4213 mL
	25 mM	0.1095 mL	0.5474 mL	1.0948 mL	2.7370 mL
	30 mM	0.0912 mL	0.4562 mL	0.9123 mL	2.2809 mL
	40 mM	0.0684 mL	0.3421 mL	0.6843 mL	1.7106 mL
	50 mM	0.0547 mL	0.2737 mL	0.5474 mL	1.3685 mL
	60 mM	0.0456 mL	0.2281 mL	0.4562 mL	1.1404 mL
	80 mM	0.0342 mL	0.1711 mL	0.3421 mL	0.8553 mL

GSK180736A Related Classifications

Cardiovascular Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GSK180736A817194-38-0ROCKRho-associated protein kinaseRho-associated kinaseRho-kinaseROKInhibitorinhibitorinhibit

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GSK180736A

Customer Review

GSK180736A Related Antibodies

5 Publications Citing Use of MCE GSK180736A

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All ROCK Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

GSK180736A Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

GSK180736A Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

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