solid , 120166-69-0
Synonym(s):
3-[2-[4-(bis(4-Fluorophenyl)methylene)-1-piperidinyl]ethyl]-2,3-dihydro-2-thioxo-4(1H)-quinazolinone;Diacylglycerol Kinase Inhibitor II - CAS 120166-69-0 - Calbiochem;R59949;R59949, 3-{2-[4-[ bis-(4-Fluorophenyl)methylene]-1-piperidinyl]ethyl}-2,3-dihydro-2-thioxo-4(1H)quinazolinone, DGK Inhibitor II;R59949, 3-{2-[4-[bis-(4-Fluorophenyl)methylene]-1-piperidinyl]ethyl}-2,3-dihydro-2-thioxo-4(1H)quinazolinone, DGK Inhibitor II
CAS NO.:120166-69-0
Empirical Formula: C28H25F2N3OS
Molecular Weight: 489.58
MDL number: MFCD00069258
Pack Size | Price | Stock | Quantity |
1mg | RMB554.41 | In Stock |
|
5mg | RMB1508.82 | In Stock |
|
others | Enquire |
PRODUCT Properties
Melting point: | 228-230 °C |
Boiling point: | 637.1±65.0 °C(Predicted) |
Density | 1.36±0.1 g/cm3(Predicted) |
storage temp. | -20°C |
solubility | 0.1 M HCl: slightly soluble |
form | solid |
pka | 11.24±0.20(Predicted) |
color | pale yellow |
Description and Uses
R-59-949 is an inhibitor of diacylglycerol kinase α (DGK-α) with an IC50 value of 300 nM in isolated platelet plasma membranes using exogenous diacylglycerol as a substrate. DGK-α inhibition with R-59-949 increases diacylglycerol-dependent PKC activity, serotonin secretion, and aggregation of thrombin-stimulated platelets. R-59-949 inhibits DGK-α activity induced by platelet-derived growth factor (PDGF) in intact vascular smooth muscle cells (VSMCs). It inhibits high K+- and glucose-induced insulin secretion in MIN6 pancreatic β-cells in a dose-dependent manner. In vivo, administration of R-59-949 prevents retinal neovascularization in a mouse model of oxygen-induced retinopathy.
Diacylglycerol Kinase Inhibitor II has been used to determine tumor-induced inhibition with genetically modified cytotoxic T cells expressing chimeric antigen receptors (CAR). It has also been used to induce pAkt and PKR-like extracellular signal-regulated kinase (pErk) signals in T-cell acute lymphoblastic leukemia (T-ALL) cells.
Safety
Symbol(GHS) | GHS07 |
Signal word | Warning |
Hazard statements | H335-H315-H319 |
Precautionary statements | P264-P280-P302+P352-P321-P332+P313-P362-P264-P280-P305+P351+P338-P337+P313P |
Hazard Codes | Xi |
Risk Statements | 36/37/38 |
Safety Statements | 26-36 |
WGK Germany | 3 |