R59022
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    WARNING: This product is for research use only, not for human or veterinary use.

Hodoodo CAT#: H561705

CAS#: 93076-89-2

Description: R59022 is a DGKalpha inhibitor and serotonin receptor antagonist.


Chemical Structure

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R59022
CAS# 93076-89-2

Theoretical Analysis

Hodoodo Cat#: H561705
Name: R59022
CAS#: 93076-89-2
Chemical Formula: C27H26FN3OS
Exact Mass: 459.18
Molecular Weight: 459.580
Elemental Analysis: C, 70.56; H, 5.70; F, 4.13; N, 9.14; O, 3.48; S, 6.98

Price and Availability

Size Price Availability Quantity
5mg USD 285 2 weeks
10mg USD 500 2 weeks
50mg USD 1250 2 weeks
Bulk inquiry

Synonym: R59022; R-59022; R 59022;

IUPAC/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

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

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 459.58 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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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.

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3: 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.

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9: Sato M, Liu K, Sasaki S, Kunii N, Sakai H, Mizuno H, Saga H, Sakane F. Evaluations of the selectivities of the diacylglycerol kinase inhibitors R59022 and R59949 among diacylglycerol kinase isozymes using a new non-radioactive assay method. Pharmacology. 2013;92(1-2):99-107. doi: 10.1159/000351849. Epub 2013 Aug 16. PubMed PMID: 23949095.

10: Natalini PM, Zulian SE, Ilincheta de Boschero MG, Giusto NM. Diacylglycerol kinase epsilon in bovine and rat photoreceptor cells. Light-dependent distribution in photoreceptor cells. Exp Eye Res. 2013 Jul;112:139-50. doi: 10.1016/j.exer.2013.04.012. Epub 2013 Apr 19. PubMed PMID: 23608524.

11: Dominguez CL, Floyd DH, Xiao A, Mullins GR, Kefas BA, Xin W, Yacur MN, Abounader R, Lee JK, Wilson GM, Harris TE, Purow BW. Diacylglycerol kinase α is a critical signaling node and novel therapeutic target in glioblastoma and other cancers. Cancer Discov. 2013 Jul;3(7):782-97. doi: 10.1158/2159-8290.CD-12-0215. Epub 2013 Apr 4. PubMed PMID: 23558954; PubMed Central PMCID: PMC3710531.

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13: Martinez K, Shyamasundar S, Kennedy A, Chuang CC, Marsh A, Kincaid J, Reid T, McIntosh M. Diacylglycerol kinase inhibitor R59022 attenuates conjugated linoleic acid-mediated inflammation in human adipocytes. J Lipid Res. 2013 Mar;54(3):662-70. doi: 10.1194/jlr.M031211. Epub 2012 Dec 22. PubMed PMID: 23264678; PubMed Central PMCID: PMC3617941.

14: Nakano T, Hozumi Y, Goto K, Wakabayashi I. Involvement of diacylglycerol kinase γ in modulation of iNOS synthesis in Golgi apparatus of vascular endothelial cells. Naunyn Schmiedebergs Arch Pharmacol. 2012 Aug;385(8):787-95. doi: 10.1007/s00210-012-0760-0. Epub 2012 May 25. PubMed PMID: 22627682.

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20: Zulian SE, de Boschero MG, Giusto NM. Insulin action on polyunsaturated phosphatidic acid formation in rat brain: an "in vitro" model with synaptic endings from cerebral cortex and hippocampus. Neurochem Res. 2009 Jul;34(7):1236-48. doi: 10.1007/s11064-008-9901-8. Epub 2009 Jan 7. PubMed PMID: 19130221.