Cas：131060-14-5 (free base)
NB-598 is a potent competitive inhibitor of squalene epoxidase (SE). NB-598 suppresses triglyceride biosynthesis through the farnesol pathway. NB-598 suppresses the secretion of cholesterol and triacylglycerol and simultaneously reduces apolipoprotein B in HepG2 cells. NB-598 reduced basolaterally secreted radioactivity in cholesterol, cholesterol ester, PL and TG. Furthermore, NB-598 suppressed the basolateral secretion of apolipoprotein (apo) B. When microsomes prepared from control Caco-2 cells were incubated with 10 microM NB-598, acyl CoA:cholesterol acyltransferase (ACAT) activity was inhibited slightly.
Chemical Formula: C27H31NOS2
Exact Mass: 449.1847
Molecular Weight: 449.671
Elemental Analysis: C, 72.12; H, 6.95; N, 3.11; O, 3.56; S, 14.26
NB-598 free base
Chemical Name: (E)-N-ethyl-6,6-dimethyl-N-[[3-[(4-thiophen-3-ylthiophen-2-yl)methoxy]phenyl]methyl]hept-2-en-4-yn-1-amine
InChi Code: InChI=1S/C27H31NOS2/c1-5-28(14-8-6-7-13-27(2,3)4)18-22-10-9-11-25(16-22)29-19-26-17-24(21-31-26)23-12-15-30-20-23/h6,8-12,15-17,20-21H,5,14,18-19H2,1-4H3/b8-6+
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: >3 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
NB598 (10 μM) causes a 36±7% reduction in total cholesterol level of MIN6 cells. NB598 causes a significant decrease in cholesterol by 49±2%, 46±7%, and 48±2% from PM, ER, and SG, respectively. NB598 dose-dependently inhibits insulin secretion under both basal (1 mM glucose) and glucose-stimulated (16.7 mM glucose) conditions. NB598 at concentrations up to 10 μM does not affect peak outward KV currents or the voltage dependence of activation but increases current inactivation. NB-598 (10 μM) inhibits the synthesis of sterol and sterol ester from [14C]acetate without affecting the synthesis of other lipids such as phospholipids (PL), free fatty acids (FFA) and triacylglycerol (TG). In the absence of exogenous liposomal cholesterol, NB-598 reduces ACAT activity by 31%. NB-598 reduces ACAT activity by 22% even in the presence of a 600 PM concentration of liposomal cholesterol. NB-598 suppresses the secretion of cholesterol and triacylglycerol from HepG2 cells into the medium.
Horie M, Iwasawa Y, Satoh T, Shimizu A, Nagata Y, Kamei T. Effects of NB-598, a potent squalene epoxidase inhibitor, on the apical membrane uptake of cholesterol and basolateral membrane secretion of lipids in Caco-2 cells. Biochem Pharmacol. 1993 Jul 20;46(2):297-305. doi: 10.1016/0006-2952(93)90418-v. PMID: 8347152.
Horie M, Hayashi M, Satoh T, Hotta H, Nagata Y, Ishida F, Kamei T. An inhibitor of squalene epoxidase, NB-598, suppresses the secretion of cholesterol and triacylglycerol and simultaneously reduces apolipoprotein B in HepG2 cells. Biochim Biophys Acta. 1993 May 20;1168(1):45-51. PMID: 8504141.
Nagata Y, Horie M, Hidaka Y, Yonemoto M, Hayashi M, Watanabe H, Ishida F, Kamei T. Effect of an inhibitor of squalene epoxidase, NB-598, on lipid metabolism in Hep G2 cells. Chem Pharm Bull (Tokyo). 1992 Feb;40(2):436-40. doi: 10.1248/cpb.40.436. PMID: 1606641.
Hidaka Y, Hotta H, Nagata Y, Iwasawa Y, Horie M, Kamei T. Effect of a novel squalene epoxidase inhibitor, NB-598, on the regulation of cholesterol metabolism in Hep G2 cells. J Biol Chem. 1991 Jul 15;266(20):13171-7. PMID: 1649182.
Horie M, Sawasaki Y, Fukuzumi H, Watanabe K, Iizuka Y, Tsuchiya Y, Kamei T. Hypolipidemic effects of NB-598 in dogs. Atherosclerosis. 1991 Jun;88(2-3):183-92. doi: 10.1016/0021-9150(91)90080-m. PMID: 1892485.
Products are for research use only. Not for human use.
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