| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
In the Ramos cellular test and the human whole blood assay, BMS-986143 inhibits BTK with IC50s of 6.9±3.4 and 25±19 nM, respectively[1]. BMS-986143 inhibits Fcγ receptor signaling in peripheral blood mononuclear cells (PBMC) with a strong IC50 of 2 nM, which is obtained from an immune complex comprising IgG. In human whole blood, BMS-986143 suppresses CD63 expression on the surface of basophiles, which is mediated via FcεRI signaling (IC50 of 54 nM) [1]. With IC50 values of 7±3, 1±0.4, 1±0.5, and 2 nM, respectively, BMS-986143 suppresses calcium flux in Ramos B Cells, human peripheral B Cell proliferation, peripheral B Cell CD86 surface expression, and TNFα from human PBMC Cells[1].
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|---|---|
| ln Vivo |
In mice models of collagen-induced arthritis (CIA) and anticollagen antibody-induced arthritis (CAIA), BMS-986143 exhibits desirable efficacy[1]. After oral treatment (mouse 6, dog 2 mg/kg), BMS-986143 shows moderate Cmax (mouse 4.3, dog 1.2 μM) and good oral bioavailability (mouse 100%, dog 82%). Due to moderate plasma clearance (8.6, 4.4 mL/min/kg, respectively) and low volumes of distribution (1.8, 2.6 L/kg, respectively) after intravenous injection (mouse 3.0, dog 1.0 mg/kg), BMS-986143 demonstrates extended elimination half-lives (3.6, 7.9 h)[1].
|
| Animal Protocol |
Animal/Disease Models: DBA/1 male mice (8- 10wk of age) bearing CIA model[1]
Doses: 15 and 45 mg/kg Route of Administration: Oral gavage; BID Experimental Results: 15 and 45 mg/kg provided dose-dependent inhibition of observed clinical disease progression (63% and 80%, respectively ), representing 17 and 19 h coverage of the mouse whole blood IC50 (130 nM). |
| References |
| Molecular Formula |
C31H24CL2N4O4
|
|---|---|
| Molecular Weight |
587.45
|
| CAS # |
1643372-83-1
|
| Appearance |
Typically exists as solid 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 | 1.7023 mL | 8.5114 mL | 17.0227 mL | |
| 5 mM | 0.3405 mL | 1.7023 mL | 3.4045 mL | |
| 10 mM | 0.1702 mL | 0.8511 mL | 1.7023 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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