Product Name :
R59022
Description:
R59022 is a DGKalpha inhibitor and serotonin receptor antagonist.
CAS:
93076-89-2
Molecular Weight:
459.58
Formula:
C27H26FN3OS
Chemical Name:
6-[2-[4-[(4-Fluorophenyl)-phenylmethylidene]piperidin-1-yl]ethyl]-7-methyl-[1,3]thiazolo[3,2-a]pyrimidin-5-one
Smiles :
CC1N=C2SC=CN2C(=O)C=1CCN1CCC(CC1)=C(C1C=CC=CC=1)C1C=CC(F)=CC=1
InChiKey:
MFVJXLPANKSLLD-UHFFFAOYSA-N
InChi :
InChI=1S/C27H26FN3OS/c1-19-24(26(32)31-17-18-33-27(31)29-19)13-16-30-14-11-22(12-15-30)25(20-5-3-2-4-6-20)21-7-9-23(28)10-8-21/h2-10,17-18H,11-16H2,1H3
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.{{Elbasvir} MedChemExpress|{Elbasvir} HCV|{Elbasvir} Biological Activity|{Elbasvir} Formula|{Elbasvir} manufacturer|{Elbasvir} Autophagy}
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
R59022 is a DGKalpha inhibitor and serotonin receptor antagonist.|Product information|CAS Number: 93076-89-2|Molecular Weight: 459.58|Formula: C27H26FN3OS|Synonym:|R 59-022|R59022|Chemical Name: 6-[2-[4-[(4-Fluorophenyl)-phenylmethylidene]piperidin-1-yl]ethyl]-7-methyl-[1,3]thiazolo[3,2-a]pyrimidin-5-one|Smiles: CC1N=C2SC=CN2C(=O)C=1CCN1CCC(CC1)=C(C1C=CC=CC=1)C1C=CC(F)=CC=1|InChiKey: MFVJXLPANKSLLD-UHFFFAOYSA-N|InChi: InChI=1S/C27H26FN3OS/c1-19-24(26(32)31-17-18-33-27(31)29-19)13-16-30-14-11-22(12-15-30)25(20-5-3-2-4-6-20)21-7-9-23(28)10-8-21/h2-10,17-18H,11-16H2,1H3|Technical Data|Appearance: Solid Power.{{Esomeprazole} site|{Esomeprazole} Membrane Transporter/Ion Channel|{Esomeprazole} Purity & Documentation|{Esomeprazole} Data Sheet|{Esomeprazole} custom synthesis|{Esomeprazole} Autophagy} |Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: Soluble in DMSO|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.PMID:23991096 |Drug Formulation: To be determined.|HS Tariff Code: 382200|How to use|In Vitro:|In the intact platelet, R59022 is able to interrupts thrombin-induced inositol lipid cycling at the level of diacylglycerol and leads to an elevation of protein kinase C activity. R59022 (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+. R59022, an inhibitor of filovirus entry, prevents the macropinocytic uptake of filoviral particles, inhibits entry mediated by multiple filovirus GPs, and blocks replicative EBOV growth. R59022 blocks entry of EBOV pseudotypes in a concentration-dependent manner (IC50: ~5 µM). R59022 dose-dependent decreases in entry by the VLPs harboring the EBOV GP (IC50: ~2 µM). R59022 (2-12 μM; 1 hour) can inhibit EBOV GP-mediated entry in multiple cell types. R59022 (5 µM; 30 minutes) blocks macropinocytosis in vero cells.|References:|McCloud RL, Franks CE, Campbell ST, Purow BW, Harris TE, Hsu KL. Deconstructing Lipid Kinase Inhibitors by Chemical Proteomics. Biochemistry. 2017 Nov 22. doi: 10.1021/acs.biochem.7b00962. [Epub ahead of print] PubMed PMID: 29155586.Boroda S, Niccum M, Raje V, Purow BW, Harris TE. Dual activities of ritanserin and R59022 as DGKα inhibitors and serotonin receptor antagonists. Biochem Pharmacol. 2016 Oct 27. pii: S0006-2952(16)30380-X. doi: 10.1016/j.bcp.2016.10.011. [Epub ahead of print] PubMed PMID: 27989726.Products are for research use only. Not for human use.|
