| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
BIIB042 (compound 10a) showed very weak inhibitory effects on COX1 and COX2 (IC50 = 35 and 27 μM, respectively) and also showed weak inhibitory effects on hERG channels (IC50 = 15 μM)[1]. BIIB042 has good cell permeability and is not a substrate for efflux transport proteins[1]. BIIB042 exhibits good metabolic stability in liver microsomes and does not inhibit major cytochrome P450 enzymes[1]. BIIB042 (3-30 μM, 20 h) had no effect on HES-1 protein levels in MC-IXC cells, indicating that it selectively acts on the processing of amyloid precursor proteins without affecting the Notch signaling pathway[2]. BIIB042 (20 h) reduced the level of Aβ42 in H4-APP cells (IC50 = 64.3 nM) and increased the level of Aβ38 (EC50 = 146 nM), but had little effect on the level of Aβ40 [2].
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|---|---|
| ln Vivo |
BIIB042 (0-60 mg/kg, oral (mixed with feed), once daily for 65 days) significantly increased Aβ38 levels and decreased Aβ42 levels in the brains of Tg2576 mice[2]. BIIB042 (0.3-30 mg/kg, oral (mixed with feed), once daily for 6 months) significantly decreased Aβ42 levels in the brains of Tg2576 mice. BIIB042 (0-100 mg/kg, gavage, single dose) dose-dependently decreased Aβ42 levels in the brain, myocardium, and umbilicus of CF-1 mice and increased Aβ38 levels, indicating that it has a strong GSM property that impairs the blood-brain barrier[2].
|
| Cell Assay |
Western Blot Analysis[2]
Cell Types: MC-IXC cells Tested Concentrations: 3, 10 and 30 μM Incubation Duration: 20 h Experimental Results: Did not alter HES1 protein levels. |
| Animal Protocol |
Animal/Disease Models: Tg2576 mice (5 months old)[2]
Doses: 0, 3, 10, 30 and 60 mg/kg Route of Administration: p.o. (in diet), daily for 65 days Experimental Results: Significantly increased Aβ38 levels in brain in a dose-dependent manner. Significantly decreased Aβ42 levels in brain in a dose-dependent manner. Showed no significant changes in levels of Aβ40. Significantly reduced insoluble Aβ42 at 10, 30 and 60 mg/kg compared to vehicle. Showed no significant changes in insoluble Aβ38. Animal/Disease Models: Tg2576 mice (10 months old)[2] Doses: 0.3,1,10 and 30 mg/kg Route of Administration: p.o. (in diet), daily for 6 months Experimental Results: Significantly reduced soluble and insoluble Aβ42 levels in the brain and plasma at 30 mg/kg. Significantly reduced parenchymal amyloid plaque burden in both the cortex and hippocampus at 30 mg/kg. Showed a trend towards increased Aβ levels at 0.3 and 1 mg/kg. Animal/Disease Models: CF-1 mice[2] Doses: 0, 3, 10, 30 and 100 mg/kg Route of Administration: i.g., single dose Experimental Results: Induced significant and dose-dependent decreases in Aβ42 at all tested doses. Showed a dose-dependent increases in Aβ38 at 10, 30 and 100 mg/kg. Induced Aβ pharmacodynamic responses in plasma, with similar effects as in brain with decreases in Aβ42, increases in Aβ38 and small changes in Aβ40 at higher doses. Brain concentrations were approximately 80% of plasma concentrations at the 4 h time point across all doses. |
| References |
| Molecular Formula |
C29H29F4NO2
|
|---|---|
| Molecular Weight |
499.54
|
| CAS # |
1257396-73-8
|
| Related CAS # |
(Rac)-BIIB042; 1257395-14-4
|
| Appearance |
Typically exists as solids at room temperature
|
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.0018 mL | 10.0092 mL | 20.0184 mL | |
| 5 mM | 0.4004 mL | 2.0018 mL | 4.0037 mL | |
| 10 mM | 0.2002 mL | 1.0009 mL | 2.0018 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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