1188-38-1
1188-38-1 結(jié)構(gòu)式
基本信息
卡哥魯酸
氨甲酰谷氨酸
N-氨甲?；劝彼?BR>N-氨基甲酰谷氨酸
N-氨甲酰-L-谷氨酸
N-氨基甲酰-L-谷氨酸
N-氨基甲酰基-L-谷氨酸
N-氨基甲酰谷氨酸(NCG)
N-氨基甲酰-L-谷氨酸(N-氨甲酰-L-谷氨酸)
Carbaglu
N-Cbm-Glu-OH
carglumicaci
CargluMic Acid
ureidoglutaricacid
n-carbamylglutamate
carbamylglutamicacid
N-Carbamyl-L-glutamic
N-Carbamyl-L-glutamate
物理化學(xué)性質(zhì)
SKIN CONDITIONING - HUMECTANT
HAIR CONDITIONING
ANTIOXIDANT
SKIN PROTECTING
安全數(shù)據(jù)
制備方法
590-28-3
56-86-0
1188-38-1
以氰酸鉀和L-谷氨酸為原料合成N-氨基甲酰-L-谷氨酸的一般步驟如下：將4 mmol的L-谷氨酸溶解于20 mL水中，使用濃鹽酸（37 μL，體積分?jǐn)?shù)）酸化該溶液。隨后，向酸化后的溶液中加入12 mmol的硫氰酸鉀（KOCN）。在持續(xù)攪拌下，將反應(yīng)混合物加熱至333 K，維持此溫度反應(yīng)4小時。反應(yīng)完成后，將溶液冷卻至室溫，并轉(zhuǎn)移至用封口膜密封的玻璃小瓶中，封口膜上穿孔以促進(jìn)溶劑蒸發(fā)，直至觀察到白色固體析出。通過緩慢蒸發(fā)乙醇溶液的方法，在室溫下培養(yǎng)出適合X射線單晶衍射分析的（I）晶體（參見方案1）。該合成方法的產(chǎn)率為62%，所得產(chǎn)物的熔點(diǎn)為170°C至171°C。此實驗步驟是對先前報道方法的改進(jìn)和優(yōu)化。
參考文獻(xiàn)：
[1] Molecular Crystals and Liquid Crystals, 2016, vol. 625, # 1, p. 225 - 232
[2] Pharmaceutical Chemistry Journal, 1978, vol. 12, # 5, p. 601 - 606
[3] Khimiko-Farmatsevticheskii Zhurnal, 1978, vol. 12, # 5, p. 53 - 59
常見問題列表
卡谷氨酸兒童常用劑量為100～250 mg/（kg·d）。單次口服100 mg/kg后約3 h可達(dá)最大血藥濃度2.6 μg/mL。
CPS1
Carglumic acid suppresses cell viability in the pancreatic ductal adenocarcinoma cell lines, triple-negative breast cancer cell lines, hepatoma cell lines, and human non-small cell lung carcinoma cell lines in a dose-dependent manner. The 50% inhibitory concentration (IC 50 ) of Carglumic acid against those cell lines is between 5 and 7.5 mM. The results show that Carglumic acid does not induce complete cell cycle arrest. Instead, there are more sub-G1 cells among Carglumic acid-treated AsPC1 and MDA-MB-231 cells than among untreated cells. In AsPC1 and HPDE-E6E7 cells, the IC 50 s of Carglumic acid are 5 mM and over 10 mM, respectively . In MDA-MB-231 and MCF-12A cells, the IC 50 s of Carglumic acid are 5 mM and 6 mM, respectively.
The results show that Carglumic acid, but not the vehicle control, markedly inhibits tumor growth. In the orthotopic pancreatic cancer model, tumor growth inhibition by Carglumic acid on day 21 is 80% (P<0.01). In the orthotopic triple-negative breast cancer model, tumor growth inhibition by Carglumic acid on day 20 is 82% (P<0.01). These results indicate that Carglumic acid suppresses tumor growth in pancreatic cancer and triple-negative breast cancer. On day 20, mean tumor growth inhibition in orally and intravenously treated mice is 55% and 93%, respectively, relative to untreated mice (P<0.01).