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142557-61-7

中文名稱 A 484954
英文名稱 7-AMino-1-cyclopropyl-3-ethyl-1,2,3,4-tetrahydro-2,4-dioxopyrido[2,3-d]pyriMidine-6-carboxaMide
CAS 142557-61-7
分子式 C13H15N5O3
分子量 289.29
MOL 文件 142557-61-7.mol
更新日期 2024/12/20 09:35:52
142557-61-7 結(jié)構(gòu)式 142557-61-7 結(jié)構(gòu)式

基本信息

中文別名
7-氨基-1-環(huán)丙基-3-乙基-1,2,3,4-四氫-2,4-二氧代-吡啶并[2,3-D]嘧啶-6-甲酰胺
英文別名
A 484954
A-484954(A 484954)
eEF2K Inhibitor, A-484954
eEF2K Inhibitor, A-484954 - CAS 142557-61-7 - Calbiochem
7-AMino-1-cyclopropyl-3-ethyl-2,4-dioxopyrido[2,3-d]pyriMidine-6-carboxaMide
7-amino-1-cyclopropyl-3-ethyl-2,4-dioxo-1H,2H,3H,4H-pyrido[2,3-d]pyrimidine-6-carboxamide
7-Amino-1-cyclopropyl-3-ethyl-2,4-dioxo-1,2,3,4-tetrahydropyrido[2,3-d]pyrimidine-6-carboxamid
7-AMino-1-cyclopropyl-3-ethyl-1,2,3,4-tetrahydro-2,4-dioxopyrido[2,3-d]pyriMidine-6-carboxaMide
7-Amino-1-cyclopropyl-3-ethyl-2,4-dioxo-1,2,3,4-tetrahydropyrido[2,3-d]pyrimidine-6-carboxamide
Pyrido[2,3-d]pyrimidine-6-carboxamide, 7-amino-1-cyclopropyl-3-ethyl-1,2,3,4-tetrahydro-2,4-dioxo-
所屬類別
生物化工:抑制劑

物理化學性質(zhì)

沸點522.9±60.0 °C(Predicted)
密度1.522±0.06 g/cm3 (20 ºC 760 Torr)
儲存條件2-8°C
溶解度DMSO:可溶,3mg/mL,澄清(加熱)
酸度系數(shù)(pKa)14.26±0.20(Predicted)
形態(tài)粉末
顏色白色至米色

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS06
警示詞危險
危險性描述H301-H315-H319-H335
危險品標志T
危險類別碼25-36/37/38
安全說明26-45
危險品運輸編號UN 2811 6.1 / PGIII
WGK Germany3

常見問題列表

簡介
A-484954 是一種 ATP 競爭性的真核延伸因子 2 激酶 (eEF-2K;IC50 = 420 nM) 抑制劑。當以 75 μM 的濃度使用時,它可降低 PC3、HeLa、H460、H1299 和 MDA-MB-231癌細胞中的 eEF-2K自磷酸化。
生物活性
A-484954 是真核延長因子 2 (eEF2) 的高度選擇性抑制劑,其 IC50 值為 280 nM。
靶點

IC50: 280 nM (eEF2).

體外研究

A-484954 is a highly selective eEF2K inhibitor with an IC 50 value of 280 nM against eEF2K in the enzymatic assay and little activity against a wide panel of serine/threonine and tyrosine kinases. In enzymatic assay, the IC 50 value of A-484954 is increased as the concentration of ATP increased but unaffected by increasing concentrations of calmodulin.

體內(nèi)研究

A484954 causes relaxation in E (+) and E (-) aorta or mesenteric artery precontracted with NA. Pretreatment with L-NAME but not indomethacin or cimetidine partially inhibits the A484954-induced relaxation in mesenteric artery. Long-term A-484954 treatment inhibits MCT-induced increases PA pressure. It is revealed that A-484954 inhibits MCT-induced PA hypertrophy and fibrosis but not impairment of endothelium-dependent and -independent relaxation. Furthermore, A-484954 inhibits MCT-induced NADPH oxidase-1 expression and ROS generation as well as matrix metalloproteinase-2 activation.

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