| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
With an IC50 of 3.7 nM, INCB 3284 dimesylate, an orally accessible, five-selective human CCR2 antagonist, prevents monocyte chemoattractant protein-1 from binding to hCCR2. Moreover, INCB 3284 demonstrated an IC50 of 84 μM when it came to suppressing hERG potassium currents and 4.7 nM when it came to opposing chemotactic activity. At a dose of 1 μM, INCB 3284 did not exhibit any effect on GPCRs, including CCR1, CCR3, CCR5, CXCR3, and CXCR5. Furthermore, with IC50 values of 6 and 2.6 nM, respectively, INCB 3284 can potently block CCR2-mediated signal transduction processes, such as intracellular calcium mobilization and ERK phosphorylation [1].
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|---|---|
| ln Vivo |
By blocking CCR2, INCB 3284 (1 mg/kg/day, i.p.) lessens microglial activation and liver damage in mice given AOM. INCB 3284 was also found to dramatically decrease proinflammatory cytokine production, G protein signaling pathway activity, and the ratio of pERK1/2 to tERK1/2 in cortical lysates of mice given azoxymethane [2].
|
| References |
|
| Molecular Formula |
C26H31N4O4F3.2[CH4O3S]
|
|---|---|
| Molecular Weight |
712.7532
|
| Exact Mass |
712.205
|
| CAS # |
887401-93-6
|
| Related CAS # |
INCB 3284;887401-92-5
|
| PubChem CID |
11679268
|
| Appearance |
Colorless to light yellow ointment
|
| LogP |
4.749
|
| Hydrogen Bond Donor Count |
5
|
| Hydrogen Bond Acceptor Count |
15
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
47
|
| Complexity |
883
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
O=C(NCC(N[C@H]1CN([C@H]2CC[C@](C3=CC=C(OC)N=C3)(O)CC2)CC1)=O)C4=CC=CC(C(F)(F)F)=C4.CS(=O)(O)=O.CS(=O)(O)=O
|
| InChi Key |
PNPNUHKICDECDH-SEBNIYPMSA-N
|
| InChi Code |
InChI=1S/C26H31F3N4O4.2CH4O3S/c1-37-23-6-5-19(14-30-23)25(36)10-7-21(8-11-25)33-12-9-20(16-33)32-22(34)15-31-24(35)17-3-2-4-18(13-17)26(27,28)29;2*1-5(2,3)4/h2-6,13-14,20-21,36H,7-12,15-16H2,1H3,(H,31,35)(H,32,34);2*1H3,(H,2,3,4)/t20-,21?,25?;;/m1../s1
|
| Chemical Name |
N-(2-(((R)-1-((1r,4R)-4-hydroxy-4-(6-methoxypyridin-3-yl)cyclohexyl)pyrrolidin-3-yl)amino)-2-oxoethyl)-3-(trifluoromethyl)benzamide dimethanesulfonate
|
| Synonyms |
INCB3284 mesylateINCB3284 INCB3284 dimesylate INCB 3284 INCB-3284
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 : ≥ 83.3 mg/mL (~116.87 mM)
|
|---|---|
| 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 | 1.4030 mL | 7.0151 mL | 14.0302 mL | |
| 5 mM | 0.2806 mL | 1.4030 mL | 2.8060 mL | |
| 10 mM | 0.1403 mL | 0.7015 mL | 1.4030 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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