271576-80-8
中文名稱
3-[N-(2-羥基乙?；?-4-哌啶基]-4-(4-嘧啶基)-5-(4-氯苯基)吡唑
英文名稱
3-[N-(2-Hydroxyacetyl)-4-piperidyl]-4-(4-pyrimidinyl)-5-(4-chlorophenyl)pyrazole
CAS
271576-80-8
分子式
C20H20ClN5O2
分子量
397.86
MOL 文件
271576-80-8.mol
更新日期
2023/07/03 08:45:42
271576-80-8 結(jié)構(gòu)式
基本信息
中文別名
ATG-0103-[N-(2-羥基乙?；?-4-哌啶基]-4-(4-嘧啶基)-5-(4-氯苯基)吡唑
英文別名
SD-06SD 0006
SD-06-1
CS-2591
SD 0006(SD-06)
SD-06
SD 06
SD06
3-[N-(2-Hydroxyacetyl)-4-piperidyl]-4-(4-pyrimidinyl)-5-(4-chlorophenyl)pyrazole
1-(4-(5-(4-Chlorophenyl)-4-(pyrimidin-4-yl)-1H-pyrazol-3-yl)piperidin-1-yl)-2-hydroxyethanone
Ethanone, 1-[4-[5-(4-chlorophenyl)-4-(4-pyrimidinyl)-1H-pyrazol-3-yl]-1-piperidinyl]-2-hydroxy-
所屬類別
生物化工：激動(dòng)劑抑制劑物理化學(xué)性質(zhì)
沸點(diǎn)652.6±55.0 °C(Predicted)
密度1.367
儲(chǔ)存條件Sealed in dry,2-8°C
溶解度DMSO : 50 mg/mL (125.67 mM; Need ultrasonic)
酸度系數(shù)(pKa)9.39±0.50(Predicted)
形態(tài)粉末
顏色White to off-white
常見(jiàn)問(wèn)題列表
生物活性
SD 0006 (SD-06) 是口服有效的、選擇性的、ATP競(jìng)爭(zhēng)性的、有效的 p38α MAPK 的二芳基吡唑抑制劑，其IC50 值為 110 nM。靶點(diǎn)
IC50: 110 nM (p38 MAPK).
體外研究
SD 0006 clearly inhibits p38α as shown by the dose-dependent inhibition of phosphorylation of its endogenous Hsp27 substrate.
體內(nèi)研究
SD 0006 (0-30 mg/kg) may be an effective alternative to steroids and biologics for RA therapy.
SD0006 (3.75, 7.5 and 15 mg/kg; p.o.; b.i.d.) is highly effective in attenuating SCW-induced inflammation as shown by the dose-dependent inhibition of paw swelling.
| Animal Model: | 8- to 12-week-old DBA/1 mice. |
| Dosage: | 3.75, 7.5 and 15 mg/kg. |
| Administration: | Orally twice daily. |
| Result: | Inhibited the transcription of several inflammatory mediators to prevent joint swelling and bone destruction and to preserve bone density. |