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R59949

Name: R59949
Brand: Selleck Chemicals
SKU: E0082
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.E0082

R59949, a diacylglycerol kinase (DGK) inhibitor with an IC50 of 300 nM, inhibits inducible nitric oxide production through decreasing transplasmalemmal L-arginine uptake in vascular smooth muscle cells. This compound strongly inhibits type I DGK a and γ, and moderately attenuates type II DGK θ and κ.

Chemical Structure

Molecular Weight: 489.58

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability

Quality Control

Batch: E008201 DMSO]98 mg/mL]false]Ethanol]2 mg/mL]false]Water]Insoluble]false Purity: 99.24%

99.24

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Chemical Information, Storage & Stability

Molecular Weight	489.58	Formula	C₂₈H₂₅F₂N₃OS	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	120166-69-0	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	FC1=CC=C(C=C1)C(=C2CCN(CCN3C(=S)NC4=CC=CC=C4C3=O)CC2)C5=CC=C(F)C=C5

Solubility

In vitro
Batch:

DMSO : 98 mg/mL (200.17 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (10.21mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

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 addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	DKG ^[1] 0.3 μM
In vitro	R59949 is a pan diacylglycerol kinase (DGK) inhibitor, which inhibits inducible NO production through decreasing transplasmalemmal L-arginine uptake in rat aortic smooth muscle cells (RASMCs).^[1]
In vivo	R59949 upregulates the expression of PHD-2, also downregulates HIF-1α and vascular endothelial growth factor (VEGF) in the retina of oxygen-induced retinopathy (OIR) mice, suggesting a potential possibility that this compound suppresses retinal neovascular pathophysiology via PHD2/HIF-1α/VEGF pathway.^[2]
References	[1] https://pubmed.ncbi.nlm.nih.gov/27909743/ [2] https://pubmed.ncbi.nlm.nih.gov/25451596/

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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