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1646682-14-5

中文名稱 FD-IN-1
英文名稱 FD-IN-1
CAS 1646682-14-5
分子式 C23H23NO4
分子量 377.43
MOL 文件 1646682-14-5.mol
1646682-14-5 結(jié)構(gòu)式 1646682-14-5 結(jié)構(gòu)式

基本信息

中文別名
化合物 T11269
英文別名
FD-IN-1
(S)-2-(2-((3'-(1-amino-2-hydroxyethyl)-[1,1'-biphenyl]-3-yl)methoxy)phenyl)acetic acid
Benzeneacetic acid, 2-[[3'-[(1S)-1-amino-2-hydroxyethyl][1,1'-biphenyl]-3-yl]methoxy]-

物理化學(xué)性質(zhì)

沸點(diǎn)629.4±55.0 °C(Predicted)
密度1.251±0.06 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)4.14±0.10(Predicted)
形態(tài)Solid
顏色White to off-white

常見問題列表

生物活性
FD-IN-1 (Compound 12) 是一種有效的,具有口服活性的補(bǔ)體因子 D (FD) 抑制劑,IC50 為 12 nM。補(bǔ)體因子 D 是一種高特異性的 S1 絲氨酸蛋白酶,在先天免疫系統(tǒng)的替代補(bǔ)體途徑中起著重要作用。FD-IN-1 還抑制因子 XIa (FXIa) 和類胰蛋白酶 β2,IC50 分別為 7.7 和 6.5 μM。
體外研究

FD-IN-1 (Compound 12) exhibits functional inhibition of AP activation (IC 50 =0.26 μM) in vitro in a membrane attack complex (MAC) deposition assay using 50% human whole blood (WB).

體內(nèi)研究

FD-IN-1 (Compound 12) demonstrates systemic suppression of AP activation in a lipopolysaccharide-induced alternative complement pathway (AP) activation model as well as local ocular suppression in intravitreal injection-induced AP activation model in mice expressing human FD.
FD-IN-1 (Compound 12) exhibits high oral bioavailability (C57BL6 mice 83%, Beagle dogs 70%) following oral administration (mice and dogs 10 mg/kg).
FD-IN-1 (Compound 12) exhibits terminal elimination half-lives (C57BL6 mice 1.6 h and Beagle dogs 3.8 h) following intravenous administration (mice and dogs 1 mg/kg).

Animal Model: Human FD knock-in mice
Dosage: 3 and 10 mg/kg
Administration: Oral gavage
Result: The AP pathway was fully inhibited for up to 10 h at the 10 mg/kg dose.
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