R59022

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.

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.

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:

1. 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.
2. 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.