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87233-62-3

中文名稱 富馬酸依美斯汀
英文名稱 EMEDASTINE FUMARATE
CAS 87233-62-3
分子式 C25H34N4O9
分子量 534.56
MOL 文件 87233-62-3.mol
更新日期 2024/10/28 17:14:46
87233-62-3 結(jié)構(gòu)式 87233-62-3 結(jié)構(gòu)式

基本信息

中文別名
富馬酸依美司汀
富馬酸依美達(dá)斯汀
依美斯汀二富馬酸鹽
富馬酸依美斯汀 EP標(biāo)準(zhǔn)品
富馬酸依美斯汀 USP標(biāo)準(zhǔn)品
1-(2-乙氧基乙基)-2-(4-甲基-1,4-二氮雜環(huán)庚-1-基)-1H-苯并[D]咪唑 二富馬酸鹽
1-(2-乙氧基乙基)-2-(六氫-4-甲基-1H-1,4-二氮雜卓-1-基)-1H-苯并咪唑二富馬酸鹽
英文別名
Daren
kb2413
Remicut
Emadine
kb-2413
kg-2413
Rapimine
AL 3432A
ly188695
arate(1:2)
所屬類別
原料藥

物理化學(xué)性質(zhì)

熔點(diǎn)148-151°
儲(chǔ)存條件2-8°C
溶解度Soluble in water, sparingly soluble in anhydrous ethanol, very slightly soluble in acetone.
形態(tài)neat
Merck14,3557

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
RTECS號(hào)DD8870000
海關(guān)編碼2933992600
毒性LD50 orally in guinea pigs: 744 mg/kg (Fukuda)
富馬酸依美斯汀價(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
2024/08/19S5647富馬酸依美斯汀
Emedastine Difumarate
87233-62-35mg795.16元
2024/08/19S5647富馬酸依美斯汀
Emedastine Difumarate
87233-62-325mg2375.53元
2022/07/01E0936富馬酸依美斯汀
Emedastine Difumarate
87233-62-31g2655元

常見(jiàn)問(wèn)題列表

生物活性
Emedastine difumarate 是一種具有口服活性,選擇性和高親和力的組胺 H1 受體拮抗劑,Ki 值為 1.3 nM。Emedastine difumarate 是一種苯并咪唑衍生物,具有強(qiáng)大的抗過(guò)敏特性,可用于過(guò)敏性鼻炎,過(guò)敏性皮膚疾病和過(guò)敏性結(jié)膜炎。
靶點(diǎn)
TargetValue
Histamine H1 receptor
()
體外研究

Emedastine difumarate inhibits histamine H 2 receptor (K i =49067 nM) and histamine H 3 receptor (K i =12430 nM).
High concentrations of Emedastine difumarate (1 and 10 ng/ml) significantly inhibits type 1 collagen production in normal human dermal fibroblasts.
Emedastine difumarate (1, 10, 100, 1000 nM) at concentrations of ≥ 10 nM inhibits CC chemokine-elicited eosinophil migration.

體內(nèi)研究

Emedastine difumarate (0.03, 0.1, 0.3 mg/kg; orally; pretreatment of 30 min) significantly suppresses histamine-induced scratching with 0.1 and 0.3 mg/kg but not 0.03 mg/kg.
Pretreatment with Emedastine difumarate (0.03, 0.1, 0.3 mg/kg; orally) significantly inhibits the scratching induced by substance P and leukotriene B.
Emedastine difumarate (0.3 mg/kg, p.o.) produces significant inhibition of passive peritoneal anaphylaxis in guinea-pigs.
Emedastine difumarate inhibits histamine-induced contractions of isolated ileum (IC 50 =6.1 nM).

Animal Model: Male ICR mice 5-6 weeks of age
Dosage: 0.03, 0.1, 0.3 mg/kg
Administration: Orally; 30 min before pruritogen injection
Result: Significantly suppressed histamine-induced scratching with pretreatment of 0.1 and 0.3 mg/kg.
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