| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| Other Sizes |
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| ln Vitro |
ELN318463 is a conventional gamma-secretase inhibitor that displaces active site-directed inhibitors only in the presence of substrate at very high concentrations and suppresses Aβ synthesis in cells 75–120 times more specifically than Notch signaling [2].
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|---|---|
| ln Vivo |
ELN318463 (30 mg/kg or 100 mg/kg; oral) generates a substantial reduction in brain Aβ in a PDAPP transgenic model of Alzheimer's disease (AD) as well as in wild-type FVB strain mice [2].
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| Animal Protocol |
Animal/Disease Models: Female, two to three months old, FVB/N mice and PDAPP transgenic model of Alzheimer's disease (AD) [2]
Doses: 30 mg/kg or 100 mg/kg Route of Administration: Oral Experimental Results: Brain levels at 30 mg/kg were 0.754 μM in FVB brains and 0.69 μM in PDAPP brains, and at the 100 mg/kg dose, levels in FVB brains were 2.7 μM and 1.87 μM in PDAPP brains. |
| References |
| Molecular Formula |
C19H20BRCLN2O3S
|
|---|---|
| Molecular Weight |
471.795701980591
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| Exact Mass |
470.006
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| CAS # |
851600-86-7
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| Related CAS # |
ELN318463 racemate;851599-82-1
|
| PubChem CID |
46883899
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| Appearance |
Off-white to light yellow solid powder
|
| LogP |
4.1
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
27
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| Complexity |
597
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| Defined Atom Stereocenter Count |
1
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| SMILES |
N([C@@H]1CCCCNC1=O)(CC1C=CC(Br)=CC=1)S(C1C=CC(Cl)=CC=1)(=O)=O
|
| InChi Key |
KTCJYACFOQWRDO-GOSISDBHSA-N
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| InChi Code |
InChI=1S/C19H20BrClN2O3S/c20-15-6-4-14(5-7-15)13-23(18-3-1-2-12-22-19(18)24)27(25,26)17-10-8-16(21)9-11-17/h4-11,18H,1-3,12-13H2,(H,22,24)/t18-/m1/s1
|
| Chemical Name |
N-[(4-bromophenyl)methyl]-4-chloro-N-[(3R)-2-oxoazepan-3-yl]benzenesulfonamide
|
| Synonyms |
ELN318463; ELN-318463
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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)
|
| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~264.94 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.41 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.41 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1195 mL | 10.5977 mL | 21.1954 mL | |
| 5 mM | 0.4239 mL | 2.1195 mL | 4.2391 mL | |
| 10 mM | 0.2120 mL | 1.0598 mL | 2.1195 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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