- NB-598
- NB-598 Maleate
- NB-598 Maleate salt
- Terbinafine HCl
| NB-598 hydrochlorideSE inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
- View current batch:
- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
Chemical structure
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| Cas No. | 136719-25-0 | SDF | Download SDF |
| Synonyms | NB 598 hydrochloride;NB598 hydrochloride | ||
| 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;hydrochloride | ||
| Canonical SMILES | CCN(CC=CC#CC(C)(C)C)CC1=CC(=CC=C1)OCC2=CC(=CS2)C3=CSC=C3.Cl | ||
| Formula | C27H32ClNOS2 | M.Wt | 486.13 |
| Solubility | ≥54 mg/mL in DMSO with gentle warming, ≥49.3 mg/mL in EtOH with gentle warming, <2.58 mg/ml="" in="" h2o=""> | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
NB-598 is a competitive inhibitor of squalene epoxidase with IC50 value of 4.4 nM [1].Low-density lipoprotein (LDL) is a lipoprotein that transfers cholesterol from the liver to all tissues of the body. Increasing concentrations of LDL particles are strongly associated with increasing amounts of atherosclerosis. Therefore the inhibition of cholesterol synthesis is thought to have hypolipidemic effect. In the complex process of cholesterol synthesis, squalene epoxidase is located in the middle of the pathway and plays an important regulatory role. It is a good target for hypocholesterolemic drugs discovered. As an inhibitor of squalene epoxidase, NB-598 was a benzylamine derivative that screened out from synthetic compounds. It competitively inhibited squalene epoxidase with respect to squalene. The Ki value for it was 0.68 nM. NB-598 inhibited cholesterol synthesis both in vitro and in vivo [1].NB-598 is a selective inhibitor of squalene epoxidase. It had no inhibition on 2, 3-oxido-squalene cyclase. Unlike those compounds used as antifungal drugs, NB-598 showed no inhibitory effect against Trichophyton mentagrophytes or Candida albicans. In the in vitro assay using microsomes from HepG2 cells, NB-598 inhibited squalene epoxidase with IC50 value of 0.75 nM. In HepG2 cells, NB-598 prevented cells from incorporating acetate into cholesterol with IC50 value of 3.4 nM. It did not affect the synthesis of other lipids such as free fatty acid, triacylglycerol and phospholipids [1]. In rats, oral administration of NB-598 dose-dependently increased serum squalene levels and decreased serum cholesterol levels with ED50 value of 5.1 mg/kg. In beagle dogs, oral administration of NB-598 at dose of 10 mg/kg/day for 28 days significantly lowered cholesterol levels in serum. Besides that, it caused reduction of all classes of lipoprotein cholesterol. It was found that NB-598 reduced LDL cholesterol levels through inducing the activities of LDL receptors [1]. Reference:[1] Horie M, Tsuchiya Y, Hayashi M, et al. NB-598: a potent competitive inhibitor of squalene epoxidase. Journal of Biological Chemistry, 1990, 265(30): 18075-18078.
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