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210755-45-6

中文名稱 2-[[[4-(4-氟苯氧基)苯基]磺酰基]氨基] -N-羥基-2-甲基丙酰胺
英文名稱 CP 471,474
CAS 210755-45-6
分子式 C16H17FN2O5S
分子量 368.38
MOL 文件 210755-45-6.mol
210755-45-6 結(jié)構(gòu)式 210755-45-6 結(jié)構(gòu)式

基本信息

中文別名
2-[[[4-(4-氟苯氧基)苯基]磺?;鵠氨基] -N-羥基-2-甲基丙酰胺
英文別名
CP 471,474
PF-1626077
2-(4-(4-Fluorophenoxy)phenylsulfonamido)-N-hydroxy-2-methylpropanamide
2-[[[4-(4-Fluorophenoxy)phenyl]sulfonyl]amino]-N-hydroxy-2-methylpropanamide
Propanamide, 2-[[[4-(4-fluorophenoxy)phenyl]sulfonyl]amino]-N-hydroxy-2-methyl-

物理化學(xué)性質(zhì)

熔點(diǎn)135-137°C (dec.)
密度1.375±0.06 g/cm3(Predicted)
儲(chǔ)存條件room temp
溶解度二甲基亞砜:≥20mg/mL
酸度系數(shù)(pKa)9.33±0.50(Predicted)
形態(tài)粉末
顏色白色至灰白色

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險(xiǎn)性描述H302
防范說(shuō)明P280-P305+P351+P338
危險(xiǎn)品標(biāo)志Xn
危險(xiǎn)類別碼22
WGK Germany1

常見(jiàn)問(wèn)題列表

生物活性
CP-471474 是一個(gè)口服有效的、廣泛的 MMP 抑制劑,IC50 值分別為1170 nM (MMP-1)、0.7 nM (MMP-2)、16 nM (MMP-3)、13 nM (MMP-9) 和 0.9 nM (MMP-13)。
靶點(diǎn)

MMP-2

0.7 nM (IC 50 )

MMP-13

0.9 nM (IC 50 )

MMP-9

13 nM (IC 50 )

MMP-3

16 nM (IC 50 )

MMP-1

1170 nM (IC 50 )

體內(nèi)研究

CP-471474 plasma levels following subcutaneous injection are 2,020 ng/mL (1 h postdose) to 160 ng/mL (6 h postdose).
CP-471,474 significantly reduces both the extent and severity of inflammation at 2 months. At 4 months, a spontaneous reduction of the inflammatory response is observed in both treated and untreated animals, and consequently no difference is observed between both.
CP-471474 significantly decreases the destructive lesions mainly at 2 months and also at 4 months.

Animal Model: Guinea pigs weighing 400 to 450 g (COPD).
Dosage: 20 mg/kg (also supplemented daily by the diet (200 mg/200 g powdered chow)).
Administration: Subcutaneously (in 20% ethanol/80% polyethylene glycol), once a day during the entire course.
Result: Lungs derived from smoking animals treated with the compound demonstrated a statistically significant reduction in the destructive lesions.
Showed an increase of both pro–MMP-9 and its active form (lanes 5 to 8) as compared with control animals.
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