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15307-86-5

中文名稱 雙氯芬酸
英文名稱 1-(2,6-Dichlorophenyl)-2-indolinone
CAS 15307-86-5
EINECS 編號(hào) 239-348-5
分子式 C14H9Cl2NO
MDL 編號(hào) MFCD00451393
分子量 278.13
MOL 文件 15307-86-5.mol
更新日期 2024/12/20 18:42:51
15307-86-5 結(jié)構(gòu)式 15307-86-5 結(jié)構(gòu)式

基本信息

中文別名
雙氯芬酸
奧爾芬
2-[(2,6-二氯苯基)氨基]-苯乙酸
英文別名
1-(2,6-DICHLOROPHENYL)-1,3-DIHYDRO-INDOLE-2-ONE
(N-1-(2,6-DICHLOROPHENYL) -2-INDOLIN-2-ONE
Diciofenac
2-[[2,6-Dichlorophenyl] amino] benzeneacetic acid
1-(2,6-DICHLOROPHENYL)-2-INDOLINONE /MEQUITAZINE
1-(2,6-DICHLOROPHENYL)-2-INDOLINONE/INDOLINONE
DICLOFENAC ACID/[2-(2,6-DICHLORO-PHENYLAMINO)-PHENY]-ACETIC ACID
(o-(2,6-dichloroanilino)phenyl)-acetic acid
dichlofenac
[2-(2,6-Dichloroanilino)phenyl]-acetic acid
2-[2-(2,6-Dichlorophenyl)aminophenyl]ethanoic acid
Diclofenac
DICLOFENAC FREE ACID
Rhumalgan
2-(2-(2,6-dichlorophenylamino)phenyl)acetic acid
所屬類別
原料藥:非甾抗炎藥

物理化學(xué)性質(zhì)

熔點(diǎn)156-158°
沸點(diǎn)412.0±45.0 °C(Predicted)
密度1.431±0.06 g/cm3(Predicted)
儲(chǔ)存條件Sealed in dry,Room Temperature
溶解度溶于甲醇
酸度系數(shù)(pKa)pKa 4 (Uncertain)
形態(tài)粉末晶體
顏色白色到近乎白色
水溶解性1.278mg/L(30 ºC)
Merck14,3081
InChIKeyDCOPUUMXTXDBNB-UHFFFAOYSA-N
CAS 數(shù)據(jù)庫(kù)15307-86-5(CAS DataBase Reference)

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictogramsGHS hazard pictogramsGHS hazard pictograms
GHS06,GHS08,GHS09
警示詞危險(xiǎn)
危險(xiǎn)性描述H301-H361d-H372-H411
危險(xiǎn)品運(yùn)輸編號(hào)3249
RTECS號(hào)AG6310000
海關(guān)編碼2922.49.2600
危險(xiǎn)等級(jí)6.1(b)
包裝類別III
毒害物質(zhì)數(shù)據(jù)15307-86-5(Hazardous Substances Data)

應(yīng)用領(lǐng)域

用途一
用作消炎鎮(zhèn)痛藥

常見(jiàn)問(wèn)題列表

簡(jiǎn)介
雙氯芬酸商品名有扶他林、待克菲那、服他靈等,是一種衍生于苯乙酸類的非甾體抗炎藥(NSAID),主要用于治療骨關(guān)節(jié)炎、類風(fēng)濕關(guān)節(jié)炎、多發(fā)性肌炎、皮肌炎、脊柱關(guān)節(jié)病、強(qiáng)直性脊柱炎、痛風(fēng),以及偏頭痛、牙痛、膽結(jié)石和腎結(jié)石等需要急性止痛的情況。藥用雙氯芬酸常使用鈉鹽或鉀鹽,在中國(guó)主要以鈉鹽為主,即雙氯芬酸鈉,各個(gè)國(guó)家的情況各有不同。
?作用機(jī)理

雙氯芬酸的作用機(jī)理為抑制環(huán)氧化酶活性,從而阻斷花生四烯酸向前列腺素的轉(zhuǎn)化生成,因前列腺素為引起疼痛、發(fā)燒及發(fā)炎等之現(xiàn)象的主要因子。

性質(zhì)
雙氯芬酸為白色結(jié)晶性粉末,無(wú)臭,易溶于丙酮,溶于甲,乙醇,微溶于水。
藥理作用
雙氯芬酸具有顯著的抗風(fēng)濕,消炎,止痛和解熱作用,其抗炎作用比阿司匹林強(qiáng)26—50倍,能很好的解除關(guān)節(jié)疼能,消腫,改善其活動(dòng),同時(shí)具有良好的耐受性。
生物活性
Diclofenac acid是一種非類固醇的消炎藥,具有止痛、消炎和退熱活性,在治療多種急性和慢性疼痛、炎癥反應(yīng)中有效。它能抑制cyclooxygenase-1 (COX-1)和cyclooxygenase-2 (COX-2),具有相近的效力。
靶點(diǎn)

Human COX-2

1.3 nM (IC 50 , in CHO cells)

Human COX-1

4 nM (IC 50 , in CHO cells)

Ovine COX-2

0.84 μM (IC 50 )

Ovine COX-1

5.1 μM (IC 50 )

體外研究

Diclofenac effectively blocks COX-1 mediated prostanoid production from U937 cell microsomes, with an IC 50 of 7±3 nM.
Diclofenac (1-60 μM; 1 day) induces neural stem cells (NSCs)death in a concentration-dependent manner.
Diclofenac (10-60 μM; 6 hours) increases the expression of cleaved (activated) caspase-3.

Cell Viability Assay

Cell Line: Neural stem cells (NSCs)
Concentration: 1, 3, 10, 30, 60 μM
Incubation Time: 1 day
Result: Induction of cell death was concentration-dependent and the effect was not saturated at a concentration of up to 60 μM.

Western Blot Analysis

Cell Line: Neural stem cells (NSCs)
Concentration: 10, 30 or 60 μM
Incubation Time: 6 hours
Result: The activation of caspase-3 was increased in a concentration-dependent manner.
體內(nèi)研究

Diclofenac (3 mg/kg, b.i.d., for 5 days) significantly increases faecal 51 Cr excretion in rats, and such effect is also observed in squirrel monkeys after administrated of 1 mg/kg twice daily for 4 days.
Diclofenac (10 mg/kg; administered via oral route just prior to induction of inflammation) shows in vivo anti-inflammatory activity in Wistar rats.

Animal Model: Male Sprague-Dawley rats (150±200 g)
Dosage: 3 mg/kg
Administration: Oral administration, b.i.d., for 5 days
Result: Resulted in a significant increase in faecal 51 Cr excretion.
Animal Model: Wistar rats (150-175 g) bearing Formalin-induced rat foot paw edema model
Dosage: 10 mg/kg
Administration: Administered via oral route just prior to induction of inflammation
Result: Showed in vivo anti-inflammatory activity (% edema inhibition=29.2, 1 h; 22.2, 3 h; 20, 6 h).
雙氯芬酸價(jià)格(試劑級(jí))
報(bào)價(jià)日期產(chǎn)品編號(hào)產(chǎn)品名稱CAS號(hào)包裝價(jià)格
2024/11/11XW153078652雙氯芬酸15307-86-55G49元
2024/11/08HY-15036雙氯芬酸
Diclofenac
15307-86-5500mg350元
2024/11/08HY-15036雙氯芬酸
Diclofenac
15307-86-55G484元
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