3-[N-(2-Hydroxyacetyl)-4-piperidyl]-4-(4-pyrimidinyl)-5-(4-chlorophenyl)pyrazole
3-[N-(2-Hydroxyacetyl)-4-piperidyl]-4-(4-pyrimidinyl)-5-(4-chlorophenyl)pyrazole Basic information
- Product Name:
- 3-[N-(2-Hydroxyacetyl)-4-piperidyl]-4-(4-pyrimidinyl)-5-(4-chlorophenyl)pyrazole
- Synonyms:
-
- 3-[N-(2-Hydroxyacetyl)-4-piperidyl]-4-(4-pyrimidinyl)-5-(4-chlorophenyl)pyrazole
- SD-06
- SD-06-1
- 1-(4-(5-(4-Chlorophenyl)-4-(pyrimidin-4-yl)-1H-pyrazol-3-yl)piperidin-1-yl)-2-hydroxyethanone
- SD 0006
- SD-06;SD 06;SD06
- SD 0006(SD-06)
- CS-2591
- CAS:
- 271576-80-8
- MF:
- C20H20ClN5O2
- MW:
- 397.86
- Product Categories:
-
- MAPK
- Mol File:
- 271576-80-8.mol
3-[N-(2-Hydroxyacetyl)-4-piperidyl]-4-(4-pyrimidinyl)-5-(4-chlorophenyl)pyrazole Chemical Properties
- Boiling point:
- 652.6±55.0 °C(Predicted)
- Density
- 1.367
- storage temp.
- 2-8°C
- solubility
- DMSO : 50 mg/mL (125.67 mM; Need ultrasonic)
- form
- Powder
- pka
- 9.39±0.50(Predicted)
- color
- White to off-white
3-[N-(2-Hydroxyacetyl)-4-piperidyl]-4-(4-pyrimidinyl)-5-(4-chlorophenyl)pyrazole Usage And Synthesis
Definition
ChEBI: SD-06 is a member of the class of pyrazoles that is 1H-pyrazole in which the hydrogens at positions 3, 4, and 5 are replaced by N-(hydroxyacetyl)piperidin-4-yl, pyrimidin-4-yl and p-chlorophenyl groups, respectively. It is a member of pyrazoles, a member of pyrimidines, a N-acylpiperidine, a member of monochlorobenzenes and a primary alcohol.
Biological Activity
SD 0006 (SD-06) is an orally potent, selective, ATP-competitive, and potent diarylpyrazole inhibitor of p38α MAPK with IC50 of 110 nM.
in vitro
SD 0006 clearly inhibits p38α as shown by the dose-dependent inhibition of phosphorylation of its endogenous Hsp27 substrate.
in vivo
SD 0006 (0-30 mg/kg) may be an effective alternative to steroids and biologics for RA therapy.It(3.75, 7.5 and 15 mg/kg; po; bid) is highly effective in attenuating SCW-induced inflammation as shown by the dose-dependent inhibition of paw swelling.
target
IC50: 110 nM (p38 MAPK).
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