R59022


Catalog No. size PriceQuantity
M6826-2 2mg solid $150
M6826-10 10mg solid $611

Description

Cas:93076-89-2

Product Information

R59022 is a DGKalpha inhibitor and serotonin receptor antagonist.

 

Chemical Formula: C27H26FN3OS

 

Exact Mass: 459.1781

 

Molecular Weight: 459.58

 

Elemental Analysis: C, 70.56; H, 5.70; F, 4.13; N, 9.14; O, 3.48; S, 6.98

 

Synonym:

 

R59022

 

Chemical Name: 6-[2-[4-[(4-Fluorophenyl)-phenylmethylidene]piperidin-1-yl]ethyl]-7-methyl-[1,3]thiazolo[3,2-a]pyrimidin-5-one

 

InChi Key: 

MFVJXLPANKSLLD-UHFFFAOYSA-N

 

InChi Code: 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

 

Smiles Code:

O=C1C(CCN2CC/C(CC2)=C(C3=CC=C(F)C=C3)\C4=CC=CC=C4)=C(C)N=C5N1C=CS5

 

 

Technical Data:

 

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

 

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.

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+.

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.

 

 

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.

 

  1. 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.

 

  1. 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. 2017 Jan 1;123:29-39. doi: 10.1016/j.bcp.2016.10.011. Epub 2016 Oct 28. PubMed PMID: 27974147; PubMed Central PMCID: PMC5164959.

 

  1. Ruffo E, Malacarne V, Larsen SE, Das R, Patrussi L, Wülfing C, Biskup C, Kapnick SM, Verbist K, Tedrick P, Schwartzberg PL, Baldari CT, Rubio I, Nichols KE, Snow AL, Baldanzi G, Graziani A. Inhibition of diacylglycerol kinase α restores restimulation-induced cell death and reduces immunopathology in XLP-1. Sci Transl Med. 2016 Jan 13;8(321):321ra7. doi: 10.1126/scitranslmed.aad1565. PubMed PMID: 26764158; PubMed Central PMCID: PMC4918505.

 

  1. Sovadinova I, Babica P, Böke H, Kumar E, Wilke A, Park JS, Trosko JE, Upham BL. Phosphatidylcholine Specific PLC-Induced Dysregulation of Gap Junctions, a Robust Cellular Response to Environmental Toxicants, and Prevention by Resveratrol in a Rat Liver Cell Model. PLoS One. 2015 May 29;10(5):e0124454. doi: 10.1371/journal.pone.0124454. eCollection 2015. Erratum in: PLoS One. 2015;10(9):e0137599. PubMed PMID: 26023933; PubMed Central PMCID: PMC4449167.

 

Products are for research use only. Not for human use.

 

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