Name | diacylglycerol kinase inhibitor ii |
Synonyms | DAG Kinase Inhibitor DAG Kinase Inhibitor II diacylglycerol kinase inhibitor ii DIACYLGLYCEROL KINASE INHIBITOR II DIACYLGLYCEROL KINASE INHIBITOR I (R59 949) 3-[2-[4-Bis(4-fluorophenyl)methylenepiperidino]ethyl]-2,3-dihydro-2-thioxoquinazolin-4(1H)-one 3-[2-(4-[BIS(4-FLUOROPHENYL)-METHYLENE)-1-PIPERIDINYL)ETHYL]-2,3-DIHYDRO-2-THIOXO-4[1H]-QUINAZOLINONE 3-[2-[4-(bis(4-Fluorophenyl)Methylene)-1-piperidinyl]ethyl]-2,3-dihydro-2-thioxo-4(1H)-quinazolinone, R59949 R59949, 3-[2-[4-(bis(4-Fluorophenyl)methylene)-1-piperidinyl]ethyl]-2,3-dihydro-2-thioxo-4(1H)-quinazolinone |
CAS | 120166-69-0 |
InChI | InChI=1/C28H25F2N3OS/c29-22-9-5-19(6-10-22)26(20-7-11-23(30)12-8-20)21-13-15-32(16-14-21)17-18-33-27(34)24-3-1-2-4-25(24)31-28(33)35/h1-12H,13-18H2,(H,31,35) |
Molecular Formula | C28H25F2N3OS |
Molar Mass | 489.58 |
Density | 1.36±0.1 g/cm3(Predicted) |
Melting Point | 228-230 °C |
Boling Point | 637.1±65.0 °C(Predicted) |
Flash Point | 339.1°C |
Solubility | 0.1 M HCl: slightly soluble |
Vapor Presure | 3.94E-16mmHg at 25°C |
Appearance | solid |
Color | pale yellow |
pKa | 11.24±0.20(Predicted) |
Storage Condition | -20°C |
Refractive Index | 1.688 |
In vitro study | In the presence of R59949, vasopressin- as well as collagen-induced release reaction and aggregation was strongly increased, independently of the formation of arachidonate metabolites. In THP‐1 monocytes, R59949 attenuates CCL2‐evoked Ca 2+ signalling with a half‐maximal concentration of 8.6 μM. R59949 inhibits inducible nitric oxide production through decreasing transplasmalemmal L-arginine uptake in vascular smooth muscle cells. |
Hazard Symbols | Xi - Irritant |
Risk Codes | 36/37/38 - Irritating to eyes, respiratory system and skin. |
Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S36 - Wear suitable protective clothing. |
WGK Germany | 3 |
Biological activity | R59949 is a pan-diacylglycerol kinase (DGK) inhibitor with IC50 of 300 nM. R59949 strongly inhibited the activity of type I DGKα and γ, and moderately weakened the activity of type II DGKθ and κ. R59949 activates protein kinase C (PKC) by increasing the level of endogenous ligand diacylglycerol. |