Name | 6-[2-[4-[(4-fluorophenyl)-phenylmethylidene]piperidin-1-yl]ethyl]-7-methyl-[1,3]thiazolo[3,2-a]pyrimidin-5-one |
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Synonyms | R 59022 |
Description | R 59-022 (DKGI-I) is a diacylglycerol kinase inhibitor (IC50=2.8 μM). R 59-022 is a 5-HTR antagonist, and activates protein kinase C (PKC). R 59-022 potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils[1][2][3][4]. |
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Related Catalog | |
In Vitro | In the intact platelet, R 59-022 is able to interrupts thrombin-induced inositol lipid cycling at the level of diacylglycerol and leads to an elevation of protein kinase C activity[1]. R 59-022 (10 μM) potentiates aggregation, but not shape change induced by sub-maximal concentrations of thrombin. R59022 (10 μM) had no significant effect on the dose-response curve for the mobilization of intracellular Ca2+ by thrombin in either the presence or the absence of extracellular Ca2+[2]. R 59-022, an inhibitor of filovirus entry, prevents the macropinocytic uptake of filoviral particles, inhibits entry mediated by multiple filovirus GPs, and blocks replicative EBOV growth. R 59-022 blocks entry of EBOV pseudotypes in a concentration-dependent manner (IC50: ~5 µM). R 59-022 dose-dependent decreases in entry by the VLPs harboring the EBOV GP (IC50: ~2 µM). R 59-022 (2-12 μM; 1 hour) can inhibit EBOV GP-mediated entry in multiple cell types. R 59-022 (5 µM; 30 minutes) blocks macropinocytosis in vero cells[5]. |
References |
Density | 1.26g/cm3 |
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Boiling Point | 619.8ºC at 760mmHg |
Molecular Formula | C27H26FN3OS |
Molecular Weight | 459.57800 |
Flash Point | 328.6ºC |
Exact Mass | 459.17800 |
PSA | 65.85000 |
LogP | 5.28180 |
Index of Refraction | 1.654 |
Personal Protective Equipment | Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter |
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Hazard Codes | Xi |
Safety Phrases | S23-S24/25 |
RIDADR | NONH for all modes of transport |