CAY10594

CAY10594 is a potent phospholipase D2 inhibitor. CAY10594 ameliorates acetaminophen-induced acute liver injury by regulating the phosphorylated-GSK-3β/JNK axis. CAY10594 administration markedly blocked the acute liver injury in a dose-dependent manner, showing almost complete inhibition with 8 mg/kg of CAY10594. CAY10594 administration strongly blocked GSK-3β (Serine 9)/JNK phosphorylation in the APAP-induced acute liver injury model. Consistently, sustained JNK activation in the cytosol and mitochondria from hepatocytes were also decreased in CAY10594-treated mice.

Product information

CAS Number: 1130067-34-3

Molecular Weight: 428.53

Formula: C26H28N4O2

Chemical Name: N-[2-(4-oxo-1-phenyl-1, 3, 8-triazaspiro[4, 5]dec-8-yl)ethyl]-2-naphthalenecarboxamide

Smiles: O=C(NCCN1CCC2(CC1)C(=O)NCN2C1C=CC=CC=1)C1C=C2C=CC=CC2=CC=1

InChiKey: FAIFAFUXFFWVNQ-UHFFFAOYSA-N

InChi: InChI=1S/C26H28N4O2/c31-24(22-11-10-20-6-4-5-7-21(20)18-22)27-14-17-29-15-12-26(13-16-29)25(32)28-19-30(26)23-8-2-1-3-9-23/h1-11,18H,12-17,19H2,(H,27,31)(H,28,32)

Technical Data

Appearance: Solid Power

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

Solubility: To be determined

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

References:

1. Lingelem ABD, Kavaliauskiene S, Halsne R, Klokk TI, Surma MA, Klose C, Skotland T, Sandvig K. Diacylglycerol kinase and phospholipase D inhibitors alter the cellular lipidome and endosomal sorting towards the Golgi apparatus. Cell Mol Life Sci. 2021 Feb;78(3):985-1009. doi: 10.1007/s00018-020-03551-6. Epub 2020 May 23. PMID: 32447426; PMCID: PMC7897626.
2. Lee SK, Bae GH, Kim YS, Kim HS, Lee M, Ghim J, Zabel BA, Ryu SH, Bae YS. A phospholipase D2 inhibitor, CAY10594, ameliorates acetaminophen-induced acute liver injury by regulating the phosphorylated-GSK-3β/JNK axis. Sci Rep. 2019 May 10;9(1):7242. doi: 10.1038/s41598-019-43673-x. PMID: 31076618; PMCID: PMC6510900.
3. Zhou G, Yu L, Yang W, Wu W, Fang L, Liu Z. Blockade of PLD2 Ameliorates Intestinal Mucosal Inflammation of Inflammatory Bowel Disease. Mediators Inflamm. 2016;2016:2543070. doi: 10.1155/2016/2543070. Epub 2016 Sep 18. PMID: 27721573; PMCID: PMC5046040.
4. Choudhary V, Olala LO, Qin H, Helwa I, Pan ZQ, Tsai YY, Frohman MA, Kaddour- Djebbar I, Bollag WB. Aquaporin-3 re-expression induces differentiation in a phospholipase D2-dependent manner in aquaporin-3-knockout mouse keratinocytes. J Invest Dermatol. 2015 Feb;135(2):499-507. doi: 10.1038/jid.2014.412. Epub 2014 Sep 18. PMID: 25233074; PMCID: PMC7278525.

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