Description
R59949 is a pan diacylglycerol kinase (DGK) inhibitor with an IC50 of 300 nM. R59949 strongly inhibits the activity of type I DGK α and γ and moderately attenuates the activity of type II DGK θ and κ. R59949 activates protein kinase C (PKC) by enhancing the levels of the endogenous ligand diacyl glycerol.
Product information
CAS Number: 120166-69-0
Molecular Weight: 489.58
Formula: C28H25F2N3OS
Chemical Name: 3-(2-{4-[bis(4-fluorophenyl)methylidene]piperidin-1-yl}ethyl)-2-sulfanylidene-1,2,3,4-tetrahydroquinazolin-4-one
Smiles: O=C1C2=CC=CC=C2NC(=S)N1CCN1CCC(CC1)=C(C1C=CC(F)=CC=1)C1C=CC(F)=CC=1
InChiKey: ZCNBZFRECRPCKU-UHFFFAOYSA-N
InChi: InChI=1S/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)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
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 Ca2+ 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.
Products are for research use only. Not for human use.
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