Size | Price | |
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100mg | ||
250mg | ||
500mg | ||
Other Sizes |
Targets |
BRD2 BD1 570 nM (IC50) BRD2 BD2 5.9 nM (IC50) BRD3 BD1 465 nM (IC50) BRD3 BD2 6.0 mM (IC50) BRD4 BD1 524 nM (IC50) BRD4 BD2 1.6 nM (IC50) BRDT BD1 527 nM (IC50)
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ln Vitro |
Compared to BD1, BET BD2-IN-1 (500 nM) exhibits superior selectivity for BD2 and can effectively block Th17 cell differentiation[1]. When bound to BRD4 BD2 in intact cells, BET BD2-IN-1 (4 nM) stabilizes BRD4 BD2 [1].
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ln Vivo |
BET BD2-IN-1 (20 mg/kg, intravenous injection; once daily, used for 7 days) substantially reduces psoriasis symptoms by inhibiting the production of p-STAT3 and p-NF-κB proteins in mouse skin tissue. alterations in pathology in mouse models [1]. The DSS-induced IBD mouse model's disease activity index (DAI) score was dramatically lowered by BET BD2-IN-1 (20 mg/kg, intravenous injection; once daily for 7 days) [1]. In Sprague Dawley Rat Model, Pharmacokinetic Analysis of BET BD2-IN-1[1]
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Cell Assay |
Cell Differentiation Assay[1]
Cell Types: Th17 cells Tested Concentrations: 500 nM Incubation Duration: Experimental Results: demonstrated the strongest inhibitory activity and decreased differentiation from 19.0 to 7.81%. Cell Migration Assay [1] Cell Types: HEK 293 T cells Tested Concentrations: 4, 20, 100, 500, 2500, 10000 nM Incubation Duration: 30 min Experimental Results: Stabilized BRD4 BD2 at 50.4 °C. |
Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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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) |
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.) |
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.