NB-598 hydrochloride (Synonyms: NB 598 hydrochloride;NB598 hydrochloride) |
| Catalog No.GC15686 |
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 136719-25-0
Sample solution is provided at 25 µL, 10mM.
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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.
Kinase experiment: | Caco-2 cells are grown in a 58 cm2 plastic dish with medium A for 13 days. The cells are washed with medium B, and then cultured with medium B including cholesterol-micelle and each compound. The compound is dissolved in Me2SO, and the final concentration of Me2SO is 0.1%(v/v). After 18 hr of incubation, the cells are washed extensively with phosphate-buffered saline (PBS) to remove the compound. Microsomes are prepared as described above. The reaction mixture (0.2 mL) consisted of 0.1 mg microsomes, 0.25% BSA and 40 PM [14C]oleoyl CoA in buffer A. To avoid the effects of endogenous cholesterol, liposome (2 mol of cholesterol: 1 mol of phosphatidylcholine) [15] is added to the reaction mixture. The microsomes are preincubated for 1 hr with or without exogenous cholesterol, and ACAT activity is determined as described above. |
References: [1]. Xia F, et al. Inhibition of cholesterol biosynthesis impairs insulin secretion and voltage-gated calcium channel function in pancreatic beta-cells. Endocrinology. 2008 Oct;149(10):5136-45. | |
| Cas No. | 136719-25-0 | 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 | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0571 mL | 10.2853 mL | 20.5706 mL |
| 5 mM | 0.4114 mL | 2.0571 mL | 4.1141 mL |
| 10 mM | 0.2057 mL | 1.0285 mL | 2.0571 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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