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215303-72-3

215303-72-3 structure
215303-72-3 structure
  • Name: RWJ 67657
  • Chemical Name: 4-[4-(4-fluorophenyl)-1-(3-phenylpropyl)-5-pyridin-4-ylimidazol-2-yl]but-3-yn-1-ol
  • CAS Number: 215303-72-3
  • Molecular Formula: C27H24FN3O
  • Molecular Weight: 425.497
  • Catalog: Pharmaceutical intermediate Heterocyclic compound Pyridine compound Hydroxypyridine
  • Create Date: 2016-12-04 05:12:42
  • Modify Date: 2025-08-21 11:35:16
  • RWJ 67657 (JNJ 3026582) is an orally active and selective p38α and p38β MAPK inhibitor with IC50s of 1 and 11 μM, respectively. RWJ 67657 displays no activity at p38γ and p38δ, and exhibits cardio protective. Anti-inflammatory and anti-tumor activity[1].

Name 4-[4-(4-fluorophenyl)-1-(3-phenylpropyl)-5-pyridin-4-ylimidazol-2-yl]but-3-yn-1-ol
Synonyms 4-(4-(4-Fluorophenyl)-1-(3-phenylpropyl)-5-(4-pyridinyl)-1H-imidazol-2-yl)-3-butyn-1-ol
4-[4-(4-Fluorophenyl)-1-(3-phenylpropyl)-5-(pyridin-4-yl)-1H-imidazol-2-yl]but-3-yn-1-ol
3-Butyn-1-ol, 4-(4-(4-fluorophenyl)-1-(3-phenylpropyl)-5-(4-pyridinyl)-1H-imidazol-2-yl)-
3-Butyn-1-ol, 4-[4-(4-fluorophenyl)-1-(3-phenylpropyl)-5-(4-pyridinyl)-1H-imidazol-2-yl]-
4-[4-(4-Fluorophenyl)-1-(3-phenylpropyl)-5-(4-pyridinyl)-1H-imidazol-2-yl]-3-butyn-1-ol
4-(4-Fluorophenyl)-2-(4-hydroxy-1-butynyl)-1-(3-Phenylpropyl)-5-(4-Pyridyl)imidazole
RWJ-67657
Description RWJ 67657 (JNJ 3026582) is an orally active and selective p38α and p38β MAPK inhibitor with IC50s of 1 and 11 μM, respectively. RWJ 67657 displays no activity at p38γ and p38δ, and exhibits cardio protective. Anti-inflammatory and anti-tumor activity[1].
Related Catalog
Target

p38α:1 μM (IC50)

p38β:11 μM (IC50)

In Vitro RWJ 67657 inhibits the release of TNF-α by lipopolysaccharide (LPS)-treated human peripheral blood mononuclear cells with an IC50 of 3 nM, as well as the release of TNF-α from peripheral blood mononuclear cells treated with the superantigen staphylococcal enterotoxin B, with an IC50 value of 13 nM[2]. RWJ67657 (10 μM; 24 hours) decreases colony formation in MCF-7 cells[3]. Cell Proliferation Assay[3] Cell Line: MCF-7 breast carcinoma cells Concentration: 10 μM Incubation Time: 24 hours Result: Did decrease colony formation.
In Vivo RWJ 67657 inhibits 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[2]. RWJ-67657 (50 mg/kg; administered orally; once per day for 7 consecutive days) displays a potent anti-inflammatory effect. By both improving the functioning of endothelial progenitor cells (EPCs) and reducing inflammation, EPC transplantation plus RWJ-67657 administration synergistically promotes angiogenesis and neurogenesis after diabetic stroke[4]. Animal Model: db/db mice (male, 8 weeks old) with EPCs[4] Dosage: 50 mg/kg Administration: Administered orally; once per day for 7 consecutive days Result: Increased angiogenesis and neurogenesis of diabetic mice after cotreatment with EPCs transplantation.
References

[1]. Shahin R, et al. Research advances in kinase enzymes and inhibitors for cardiovascular disease treatment. Future Sci OA. 2017 Aug 8;3(4):FSO204.

[2]. Wadsworth SA, et al. RWJ 67657, a potent, orally active inhibitor of p38 mitogen-activated protein kinase. J Pharmacol Exp Ther. 1999 Nov;291(2):680-7.

[3]. Frigo DE, et al. p38 mitogen-activated protein kinase stimulates estrogen-mediated transcription and proliferation through the phosphorylation and potentiation of the p160 coactivator glucocorticoid receptor-interacting protein 1. Mol Endocrinol. 2006 May;20(5):971-83.

[4]. Bai YY, et al. Synergistic Effects of Transplanted Endothelial Progenitor Cells and RWJ 67657 in Diabetic Ischemic Stroke Models. Stroke. 2015 Jul;46(7):1938-46.

Density 1.1±0.1 g/cm3
Boiling Point 611.8±65.0 °C at 760 mmHg
Melting Point 124℃
Molecular Formula C27H24FN3O
Molecular Weight 425.497
Flash Point 323.8±34.3 °C
Exact Mass 425.190338
PSA 50.94000
LogP 5.18
Vapour Pressure 0.0±1.8 mmHg at 25°C
Index of Refraction 1.599
Storage condition Store at RT
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