RWJ 67657 (Synonyms: JNJ-3026582) |
Catalog No.GC13142
One-Click Copy Product Info
|
orally active inhibitor of the MAP kinases p38α and p38β
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 215303-72-3
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
IC50: 1 and 11 μM for p38α and p38β, respectively
RWJ 67657 is an orally active inhibitor of the MAP kinases p38α and p38β.
Tumor necrosis factor-alpha (TNF-alpha), a cytokine secreted by activated monocytes/macrophages and T lymphocytes, is implicated in several disease states, such as inflammatory bowel disease, rheumatoid arthritis, septic shock, as well as osteoporosis. The monocyte/macrophage production of TNF-alpha is dependent on the mitogen-activated protein kinase p38.
In vitro: RWJ 67657 could inhibit the release of TNF-alpha by lipopolysaccharide-treated human peripheral blood mononuclear cells, as well as the release of TNF-alpha from peripheral blood mononuclear cells treated with the superantigen staphylococcal enterotoxin B. RWJ 67657 was about 10-fold more potent than the literature standard p38 kinase inhibitor SB 203580 in all tested p38 dependent in-vitro systems tested. Moreover, RWJ 67657 was able to inhibit the enzymatic activity of recombinant p38alpha and beta, but not gamma or delta, and showed no significant activity against various other enzymes. In contrast, SB 203580 could significantly inhibit the tyrosine kinases p56 lck and c-src. In addition, RWJ 67657 did not inhibit T cell production of interleukin-2 or interferon-gamma and did not inhibit T cell proliferation in response to mitogens [1].
In vivo: Animal study found that RWJ 67657 could inhibit TNF-alpha production in lipopolysaccharide-injected mice (87% inhibition at 50 mg/kg) and in rats (91% inhibition at 25 mg/kg) after oral administration [1].
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] Wadsworth, S. A.,Cavender, D.E.,Beers, S.A., et al. RWJ 67657, a potent, orally active inhibitor of p38 mitogen-activated protein kinase. Journal of Pharmacology and Experimental Therapeutics 291(2), 680-687 (1999).
| Cas No. | 215303-72-3 | SDF | |
| Synonyms | JNJ-3026582 | ||
| Chemical Name | 4-[4-(4-fluorophenyl)-1-(3-phenylpropyl)-5-(4-pyridinyl)-1H-imidazol-2-yl]-3-butyn-1-ol | ||
| Canonical SMILES | FC(C=C1)=CC=C1C2=C(C3=CC=NC=C3)N(CCCC4=CC=CC=C4)C(C#CCCO)=N2 | ||
| Formula | C27H24FN3O | M.Wt | 425.5 |
| Solubility | ≤10mg/ml in ethanol;5mg/ml in DMSO;2mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.3502 mL | 11.7509 mL | 23.5018 mL |
| 5 mM | 470 μL | 2.3502 mL | 4.7004 mL |
| 10 mM | 235 μL | 1.1751 mL | 2.3502 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 15 reference(s) in Google Scholar.)