| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Targets |
NB-360 targets BACE1 (beta-secretase 1), a membrane-bound aspartic protease that cleaves amyloid precursor protein (APP) at the beta-site to generate amyloid-β peptides. By inhibiting BACE1, NB-360 reduces the production of amyloid-β peptides, which are the primary components of amyloid plaques in Alzheimer's disease. The compound is brain-penetrant, enabling central nervous system target engagement. NB-360 shows selectivity for BACE1 over other aspartic proteases.
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| ln Vitro |
In vitro, NB-360 potently inhibits BACE1 enzymatic activity. It shows excellent selectivity for BACE1 over other aspartic proteases. The compound reduces amyloid-β production in cell-based assays. Its brain penetration enables target engagement in CNS models. Detailed in vitro data are available in the primary literature. NB-360 is a valuable tool for studying BACE1 function in Alzheimer's disease.
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| ln Vivo |
In vivo, NB-360 has been evaluated in animal models of Alzheimer's disease. The compound reduces amyloid-β levels in the brain and cerebrospinal fluid. It is brain-penetrant and shows efficacy in reducing amyloid pathology. NB-360 has been studied in transgenic mouse models of Alzheimer's disease. Further studies are needed to fully characterize its efficacy and safety profile.
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| Enzyme Assay |
In vitro BACE1 activity assays for NB-360 typically use recombinant BACE1 enzyme and a fluorogenic peptide substrate (e.g., APP beta-secretase cleavage site peptide). The compound is dissolved in DMSO and diluted in assay buffer (50 mM sodium acetate, pH 4.5, 0.1% CHAPS). Reactions are incubated at 37°C for 30-60 minutes. Fluorescence is measured at appropriate wavelengths. IC₅₀ values are calculated from dose-response curves. Selectivity is assessed against other aspartic proteases (e.g., cathepsin D, renin). Controls include DMSO vehicle and known BACE1 inhibitors.
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| Cell Assay |
For cell-based assays, cells expressing APP (e.g., CHO-APP or SH-SY5Y-APP) are cultured in appropriate medium. Cells are seeded in multi-well plates and treated with NB-360 at various concentrations (0.001-10 μM) for 24-48 hours. Amyloid-β levels in conditioned media are measured by ELISA or MSD assays. Cell viability is assessed by MTT or CellTiter-Glo. All treatments include vehicle controls and are performed in triplicate.
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| Animal Protocol |
In vivo, NB-360 is typically administered orally to rodents. For Alzheimer's disease models, transgenic mice (e.g., APP/PS1) are dosed at various regimens. Amyloid-β levels in brain and cerebrospinal fluid are measured by ELISA. Amyloid plaque burden is assessed by immunohistochemistry. Cognitive function may be assessed by behavioral tests. Blood and tissue samples are collected for pharmacokinetic analysis. All procedures follow institutional animal care guidelines.
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| ADME/Pharmacokinetics |
NB-360 is a brain-penetrant BACE1 inhibitor. Detailed pharmacokinetic parameters (bioavailability, half-life, brain penetration) are available from preclinical studies. The compound is typically stored at -20°C. It is for research purposes. The compound shows excellent selectivity for BACE1 over other aspartic proteases.
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| Toxicity/Toxicokinetics |
NB-360 is for research use only and not intended for human therapeutic applications. Standard safety pharmacology and toxicology studies would be required for therapeutic development. The compound should be handled with standard laboratory safety precautions. Toxicity data are limited in publicly available sources.
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| References | |
| Additional Infomation |
NB-360 is a research-grade BACE1 inhibitor for studying Alzheimer's disease and amyloid pathology. Its primary applications include neuroscience, Alzheimer's disease research, and drug discovery. The compound is not approved for clinical use. It is commercially available from various chemical suppliers for research purposes only. Its mechanism involves BACE1 inhibition and reduction of amyloid-β production.
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| Molecular Formula |
C21H19F4N5O2
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|---|---|
| Molecular Weight |
449.4015
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| Exact Mass |
449.147
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| Elemental Analysis |
C, 56.12; H, 4.26; F, 16.91; N, 15.58; O, 7.12
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| CAS # |
1262857-73-7
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| Related CAS # |
1262857-73-7;1262855-97-9 (HCl);1416433-41-4 (xHCl);
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| PubChem CID |
66665322
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| Appearance |
White to off-white solid powder
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| LogP |
2.2
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
32
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| Complexity |
812
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CC1=CC(=CN=C1C(=O)NC2=CC(=C(C=C2)F)[C@@]3(CO[C@@](C(=N3)N)(C)C(F)(F)F)C)C#N
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| InChi Key |
BQFHTVUWPJXLOW-VQTJNVASSA-N
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| InChi Code |
InChI=1S/C21H19F4N5O2/c1-11-6-12(8-26)9-28-16(11)17(31)29-13-4-5-15(22)14(7-13)19(2)10-32-20(3,18(27)30-19)21(23,24)25/h4-7,9H,10H2,1-3H3,(H2,27,30)(H,29,31)/t19-,20+/m0/s1
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| Chemical Name |
N-(3-((3R,6R)-5-amino-3,6-dimethyl-6-(trifluoromethyl)-3,6-dihydro-2H-1,4-oxazin-3-yl)-4-fluorophenyl)-5-cyano-3-methylpicolinamide
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| Synonyms |
NB360 NB 360 NB-360
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~556.30 mM)
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2252 mL | 11.1259 mL | 22.2519 mL | |
| 5 mM | 0.4450 mL | 2.2252 mL | 4.4504 mL | |
| 10 mM | 0.2225 mL | 1.1126 mL | 2.2252 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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