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130464-84-5

中文名稱 (2S,3R)-N-羥基-N'-[(2S)-1-甲基氨基-1-氧代-3-苯基丙-2-基]-3-異丁基-2-(噻吩-2-基硫甲基)丁二酰胺單鈉鹽
英文名稱 (2S,3R)-N-Hydroxy-N'-[(2S)-1-methylamino-1-oxo-3-phenylpropan-2-yl]-3-(2-methylpropyl)-2-(thiophen-2-ylsulfanylmethyl)butanediamide sodium salt
CAS 130464-84-5
分子式 C23H30N3NaO4S2
分子量 499.62
MOL 文件 130464-84-5.mol
130464-84-5 結(jié)構(gòu)式 130464-84-5 結(jié)構(gòu)式

基本信息

中文別名
巴馬司他納鹽
巴馬司他單鈉鹽
(2S,3R)-N-羥基-N'-[(2S)-1-甲基氨基-1-氧代-3-苯基丙-2-基]-3-異丁基-2-(噻吩-2-基硫甲基)丁二酰胺單鈉鹽
英文別名
BB94 sodiuM salt
BB-94 sodiuM salt
BB 94 sodiuM salt
Batimastat sodium salt
BB-94 SODIUM SALT
BB 94 SODIUM SALT
BB94 SODIUM SALT
(2S,3R)-N-Hydroxy-N'-[(2S)-1-methylamino-1-oxo-3-phenylpropan-2-yl]-3-(2-methylpropyl)-2-(thiophen-2-ylsulfanylmethyl)butanediamide sodium salt
所屬類別
生物化工:激動劑抑制劑

物理化學性質(zhì)

儲存條件Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
溶解度溶于二甲基亞砜

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險性描述H302-H315-H319-H335

常見問題列表

生物活性
Batimastat(BB-94)鈉是廣譜的基質(zhì)金屬蛋白酶(MMPs)抑制劑,對MMP-1/2/3/7/9的IC50分別為3/4/20/6/4 nM。
靶點

IC50: 3 nM (MMP-1), 4 nM (MMP-2), 4 nM (MMP-9), 6 nM (MMP-7), 20 nM (MMP-3)

體外研究

Batimastat (BB-94) is a potent matrix metalloproteinase inhibitor, exhibits an unexpected mode of binding. Batimastat inhibits gelatinases A and B with IC 50 values of 4 nM and 10 nM, respectively. The IC 50 with the structurally similar collagenase Ht-d is 6 nM, which is comparable with values for MMP-1 (3 nM), MMP-8 (10 nM), and MMP-3 (20 nM). CD30 shedding from the cell line Karpas299 can effectively be blocked by the hydroxamic acidbased metalloproteinase inhibitor Batimastat (BB-94, IC 50 =230 nM).

體內(nèi)研究

Intraperitoneal administration of Batimastat (BB-94) effectively blocks growth of human ovarian carcinoma xenografts and murine melanoma metastasis and delays the growth of primary tumors in an orthotopic model of human breast cancer without cytotoxicity and without affecting mRNA levels. Batimastat (BB-94) is a synthetic matrix metalloproteinase inhibitor that has shown antineoplastic and antiangiogenic activity in various tumor models. Treatment with Batimastat (60 mg/kg i.p. every other day, for a total of eight injections) concomitantly with Cisplatin (4 mg/kg i.v., every 7 days for a total of three injections) completely prevents growth and spread of both xenografts, and all animals are alive and healthy on day 200. Kaplan-Meier analysis of survival (at 48 h) shows that animals treated with Batimastat (BB-94) have increased survival (95.2%) in comparison with controls (75%), and differences are almost statistically significant (p=0.064). Matrix density is analyzed in saline- or Batimastat (40 mg/kg)-pretreated animals 4 h after E 2 administration, the time point at which collagen density is observed to be at its lowest after hormone treatment.

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