R 59-022
Chemical Name: 6-[2-[4-[(4-Fluorophenyl)phenylmethylene]-1-piperidinyl]ethyl]-7-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one
Purity: ≥98%
Biological Activity
R 59-022 is a diacylglycerol (DAG) kinase inhibitor (IC50 = 2.8 μM); increases protein kinase C activity. Potentiates thrombin-induced platelet aggregation and induces neutrophil chemotaxis. Inhibits U46619-induced contractions in mouse aorta and porcine coronary artery.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Evaluation of AaDOP2 receptor antagonists reveals antidepressants and antipsychotics as novel lead molecules for control of the yellow fever mosquito, Aedes aegypti.
Conley J, Meyer J, Nuss A, Doyle T, Savinov S, Hill C, Watts V
J Pharmacol Exp Ther, 2015;352(1):53-60. -
R 59 022, a diacylglycerol kinase inhibitor. Its effect on diacylglycerol and thrombin-induced C kinase activation in the intact platelet.
de Chaffoy de Courcelles et al.
J.Biol.Chem., 1985;260:15762 -
A diacylglyerol kinase inhibitor, R59022, potentiates secretion by and aggregation of thrombin-stimulated human platelets.
Nunn and Watson
Biochem.J., 1987;243:809 -
Neutrophil chemotaxis induced by the diacylglycerol kinase inhibitor R59022.
Boonen et al.
Biochim.Biophys.Acta, 1993;1178:97 -
Novel diacylglycerol kinase inhibitor selectively suppressed an U46619-induced enhancement of mouse portal vein contraction under high glucose conditions.
Nobe et al.
Br.J.Pharmacol., 2004;143:166
Product Datasheets
Citation for R 59-022
The citations listed below are publications that use Tocris products. Selected citations for R 59-022 include:
1 Citation: Showing 1 - 1
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Evaluation of AaDOP2 receptor antagonists reveals antidepressants and antipsychotics as novel lead molecules for control of the yellow fever mosquito, Aedes aegypti.
Authors: Conley Et al.
Nature 2015;352:53
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