131179-95-8
中文名稱
乙丙昔羅
英文名稱
Efaproxiral
CAS
131179-95-8
分子式
C20H23NO4
分子量
341.4
MOL 文件
131179-95-8.mol
更新日期
2024/12/23 10:29:51
131179-95-8 結(jié)構(gòu)式
基本信息
中文別名
乙丙昔羅2-[4-(3,5-二甲基苯基氨基甲酰甲基)苯氧基]-2-甲基丙酸
2-(4-(((3,5-二甲基苯胺)羰基)甲基)苯氧基)-2-甲基丙酸
2-[4-(3,5-二甲基苯基氨基甲酰甲基)苯氧基]-2-甲基丙酸,乙丙昔羅自由酸
英文別名
faproxiralEfaproxiral
EFAPROXIRALUM
Efaproxiral free acid
EFAPROXIRAL
EFAPROXIRAL FREE ACID
FAPROXIRAL
2-[4-(3,5-Dimethylphenylcarbamoylmethyl)phenoxy]-2-methylpropionic acid
2-(4-(((3,5-dimethylanilino)carbonyl)methyl)phenoxy)-2-methylpropionic acid
Propanoic acid, 2-[4-[2-[(3,5-dimethylphenyl)amino]-2-oxoethyl]phenoxy]-2-methyl-
所屬類別
生物化工:激動劑抑制劑物理化學性質(zhì)
熔點48-50°C
沸點554.5±50.0 °C(Predicted)
密度1.202±0.06 g/cm3(Predicted)
儲存條件Refrigerator
溶解度可溶于DMSO(少許)、甲醇(少許)
酸度系數(shù)(pKa)3.26±0.10(Predicted)
形態(tài)固體
顏色灰白色到棕褐色
乙丙昔羅價格(試劑級)
報價日期 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS號 | 包裝 | 價格 |
2024/11/08 | HY-13619 | 乙丙昔羅 Efaproxiral | 131179-95-8 | 50mg | 700元 |
2024/11/08 | HY-13619 | 乙丙昔羅 Efaproxiral | 131179-95-8 | 10mM * 1mLin DMSO | 770元 |
2024/11/08 | HY-13619 | 乙丙昔羅 Efaproxiral | 131179-95-8 | 1g | 6000元 |
常見問題列表
生物活性
Efaproxiral (RSR13) 是一種血紅蛋白 (Hb) 合成變構(gòu)調(diào)節(jié)劑, 能降低血紅蛋白氧 (O2) 的結(jié)合親和力,增強放射處理中缺氧腫瘤的氧合作用。靶點
haemoglobin (Hb)
體外研究
Efaproxiral binds to only one pair of symmetry-related sites in the Hb central water cavity.
Efaproxiral readily crosses the red cell membrane in the presence of serum albumin solutions.
Efaproxiral is not inhibited from entering erythrocytes in the presence of an anion-channel blocking agent (DIDS).
體內(nèi)研究
Efaproxiral (150 mg/kg, i.p.) increase tumor oxygenation,and increase the tumor growth inhibition of radiotherapy over 5 days of treatment.
Efaproxiral reduces hemoglobin-oxygen binding affinity, which facilitates oxygen release from hemoglobin into surrounding tissues and potentially increases the pO(2) of the tumors
Animal Model: | Female C3H/HEJ mice (18–20 g), with radiation-induced fibrosarcoma tumor (RIF-1) cells xenograft |
Dosage: | 150 mg/kg |
Administration: | Intraperitoneal injection; prior to X Irradiation (4 Gy/day), for 5 days |
Result: | Significantly increased tumor oxygenation by 8.4 to 43.4 mmHg within 5 days, with maximum increases at 22–31 minutes after treatment. |