| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
None (excipient). NT1-014B functions as a BBB-penetrating lipidoid, likely due to its tryptamine headgroup mimicking neurotransmitters, facilitating transport across the BBB. It also encapsulates AmB for antifungal therapy.
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|---|---|
| ln Vitro |
NT1-014B effectively encapsulates AmB (∼100 nm LNPs). In vitro, NT1-014B LNPs cross a BBB model (e.g., bEnd.3 cell monolayer) with significantly higher efficiency (2-4-fold increase) than non-NT LNPs. The encapsulated AmB retains its antifungal activity against C. neoformans and C. albicans. Cellular uptake in brain endothelial cells is enhanced due to the NT-lipidoid.
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| ln Vivo |
In vivo, intravenous administration of NT1-014B LNPs encapsulating AmB to mice results in enhanced brain delivery of AmB compared to free AmB or non-targeted LNPs. In a mouse model of fungal meningitis, NT1-014B/AmB LNPs reduce brain fungal burden and increase survival. The NT-lipidoid enables BBB penetration, allowing therapeutic concentrations of AmB to reach the brain with reduced systemic toxicity.
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| Enzyme Assay |
NT1-014B (C40H₆₈N2O4S4, MW 769.24) is a colorless to light yellow viscous liquid. For LNP preparation, NT1-014B is dissolved in ethanol (∼10-50 mg/mL) and mixed with helper lipids (e.g., DSPC, cholesterol, DOPC, and ionizable lipid) at optimized ratios (NT1-014B typically 10-30 mol%). The lipid mixture is combined with an aqueous solution containing AmB (amphotericin B, dissolved in DMSO or acidic buffer) via microfluidic mixing or ethanol injection, forming LNPs of ∼100 nm. Ethanol is removed by dialysis, and the pH is adjusted to 7.4. Characterization includes DLS (size, PDI, ∼0.1-0.2), zeta potential (∼0 to +10 mV), encapsulation efficiency (>90%), and AmB concentration measured by UV-Vis absorbance (λ=405 nm).
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| Cell Assay |
For in vitro BBB permeability, brain endothelial cells (e.g., bEnd.3, hCMEC/D3) are cultured on Transwell inserts (0.4 um pore, polycarbonate membrane) to form a tight BBB monolayer (TEER >200 omega·cm2). NT1-014B LNPs containing a fluorescent marker (e.g., DiD, FITC) or fluorescently labeled AmB (AmB-BODIPY) are added to the apical chamber. Permeability is measured by sampling the basolateral chamber at 0.5, 1, 2, 4, 6, 12, and 24 h, and quantifying fluorescence. Papp (apparent permeability coefficient) is calculated. Cellular uptake is assessed by flow cytometry. Antifungal activity is evaluated by broth microdilution: C. neoformans or C. albicans is incubated with AmB LNPs (0.1-10 ug/mL AmB equivalent) for 24-48 h, and MIC (minimum inhibitory concentration) is determined.
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| Animal Protocol |
For in vivo studies, NT1-014B LNPs (AmB dose: 1-5 mg/kg, lipid dose: 10-50 mg/kg) are administered intravenously via the tail vein to 6-8 week old female BALB/c or C57BL/6 mice. For fungal meningitis models: mice are infected intracranially or intravenously with C. neoformans or C. albicans (1-5×10⁵ CFU/mouse). After 3-7 days, treatment begins (q.d. or q.o.d. × 5-10 doses). Brain fungal burden is determined by homogenizing brain tissue and plating serial dilutions on Sabouraud agar, with CFU/g brain measured. Survival is monitored daily. For biodistribution: fluorescent LNPs are administered, mice are perfused transcardially, and brain AmB concentration is quantified by LC-MS/MS.
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| References |
| Molecular Formula |
C40H68N2O4S4
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|---|---|
| Molecular Weight |
769.24
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| Exact Mass |
768.406
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| CAS # |
2739805-64-0
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| PubChem CID |
162478212
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| Appearance |
Colorless to light yellow viscous liquid
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| LogP |
12.4
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
37
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| Heavy Atom Count |
50
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| Complexity |
765
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCCCCCCCCCSSCCOC(=O)CCN(CCC1=CNC2=CC=CC=C21)CCC(=O)OCCSSCCCCCCCCCC
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| InChi Key |
LBQUNMQRWYTNHB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C40H68N2O4S4/c1-3-5-7-9-11-13-15-19-31-47-49-33-29-45-39(43)24-27-42(26-23-36-35-41-38-22-18-17-21-37(36)38)28-25-40(44)46-30-34-50-48-32-20-16-14-12-10-8-6-4-2/h17-18,21-22,35,41H,3-16,19-20,23-34H2,1-2H3
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| Chemical Name |
2-(decyldisulfanyl)ethyl 3-[[3-[2-(decyldisulfanyl)ethoxy]-3-oxopropyl]-[2-(1H-indol-3-yl)ethyl]amino]propanoate
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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: 150 mg/mL (195.00 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 | 1.3000 mL | 6.4999 mL | 12.9998 mL | |
| 5 mM | 0.2600 mL | 1.3000 mL | 2.6000 mL | |
| 10 mM | 0.1300 mL | 0.6500 mL | 1.3000 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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