SB 220025
SB 220025 Basic information
- Product Name:
- SB 220025
- Synonyms:
-
- 5-(2-AMINO-4-PYRIMIDINYL)-4-(4-FLUOROPHENYL)-1-(4-PIPERIDINLYL)IMIDAZOLE
- 5-(2-AMINO-4-PYRIMIDINYL)-4-(4-FLUOROPHENYL)-1-(4-PIPERIDINYL)IMIDAZOLE
- SB 220025
- 4-[4-(4-fluorophenyl)-1-(piperidin-4-yl)-1H-imidazol-5-yl]pyrimidin-2-amine
- 2-Pyrimidinamine, 4-[4-(4-fluorophenyl)-1-(4-piperidinyl)-1H-imidazol-5-yl]-
- 4-[4-(4-Fluorophenyl)-1-(4-piperidinyl)-1H-imidazol-5-yl]-2-pyrimidinamine
- CAS:
- 165806-53-1
- MF:
- C18H19FN6
- MW:
- 338.38
- Mol File:
- 165806-53-1.mol
SB 220025 Chemical Properties
- Boiling point:
- 611.9±65.0 °C(Predicted)
- Density
- 1.42±0.1 g/cm3(Predicted)
- storage temp.
- -20°C
- solubility
- DMSO: 22mg/mL
- pka
- 9.92±0.10(Predicted)
- form
- White to pale amber solid.
- color
- white to pale yellow
SB 220025 Usage And Synthesis
Uses
SB 220025 is a reversible, orally active, cell-permeable, ATP-competitive and selective human p38 MAPK inhibitor (IC50 = 60 nM). SB 220025 also inhibits p56Lck and PKC with IC50 values of 3.5 and 2.89 μM, respectively. SB 220025 inhibits the expression of IL-8 gene in response to globular adiponectin (gAd), reduces inflammatory cytokine production and inhibits angiogenesis. SB 220025 effectively prevents the progression of arthritis in a chronic inflammatory disease model and can be used in the study of inflammation[1][2].
Definition
ChEBI: SB220025 is am member of the class of imidazoles carrying piperidin-4-yl, 4-fluophenyl and 2-aminopyrimidin-4-yl substituents at posiitons 1, 4 and 5 respectively. It has a role as an EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor, an angiogenesis inhibitor and an anti-inflammatory agent. It is a member of piperidines, an organofluorine compound, an aminopyrimidine and a member of imidazoles.
Biological Activity
Primary Target
P38MAPK
in vivo
SB 220025 (3-50 mg/kg; p.o.; single) inhibits inflammatory cytokine production in vivo[2].
SB 220025 (5, 30, 50 mg/kg; i.p.; b.i.d.) inhibits angiogenesis in the murine air pouch granuloma model[2].
SB 220025 (30 mg/kg; p.o.; twice a day for 3, 5, 7 or 14 days) prevents the increase in angiogenesis that occurs after day 3 in murine air pouch angiogenesis model[2].
SB 220025 (50 mg/kg; p.o.; b.i.d.; 10 days) effectively blocks the progression of arthritis in a chronic inflammatory disease model[2].
| Animal Model: | Acute model of LPS-induced TNF-a expression[2]. |
| Dosage: | 3-50 mg/kg |
| Administration: | Oral administration; single; 30 min before challenge with LPS. |
| Result: | Dosedependently inhibited TNF-a production with an ED50 value of 7.5 mg/kg, and showed more than 80% inhibition when at 50 mg/kg. |
| Animal Model: | Murine air pouch granuloma model[2]. |
| Dosage: | 5, 30, 50 mg/kg |
| Administration: | Intraperitoneal injection; bisindie (bid, twice a day). |
| Result: | Caused a dose-dependent reduction in angiogenesis. |
| Animal Model: | Murine air pouch granuloma model[2]. |
| Dosage: | 30 mg/kg |
| Administration: | Oral administration; twice a day from day 0 until removal of granuloma tissue at days 3, 5, 7 or 14. |
| Result: | Did not affect the initial burst of angiogenesis but did prevent the increase in angiogenesis that occurs after day 3. |
IC 50
p38: 60 nM (IC50); p56-Lck: 3.5 μM (IC50); PKC: 2.89 μM (IC50)
References
[1] Tomizawa A, et al. Induction of gene expression in response to globular adiponectin in vascular endothelial cells. Life Sci. 2009 Sep 9;85(11-12):457-61. DOI:10.1016/j.lfs.2009.07.012
[2] Jackson JR, et al. Pharmacological effects of SB 220025, a selective inhibitor of P38 mitogen-activated protein kinase, in angiogenesis and chronic inflammatory disease models. J Pharmacol Exp Ther. 1998 Feb;284(2):687-92. PMID:9454815
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