U 18666A

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U 18666A

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

3039-71-2

包装与价格：

包装	价格(元)
10mg	电议
25mg	电议
50mg	电议

产品介绍

化学性质

Physical Appearance	A crystalline solid
Storage	Store at -20°C
M.Wt	424.07
Cas No.	3039-71-2
Formula	C₂₅H₄₁NO₂·HCl
Solubility	Soluble in H2O
Chemical Name	(3S,8R,9S,10R,13S,14S)-3-(2-(diethylamino)ethoxy)-10,13-dimethyl-3,4,7,8,9,10,11,12,13,14,15,16-dodecahydro-1H-cyclopenta[a]phenanthren-17(2H)-one hydrochloride
Canonical SMILES	O=C1[C@]2(C)[C@@H](CC1)[C@H]3[C@H](CC2)[C@](CC[C@@H]4OCCN(CC)CC)(C)C(C4)=CC3.Cl
运输条件	蓝冰运输或根据您的需求运输。
一般建议	为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

U 18666A is an inhibitor of cholesterol transport and synthesis [1] [2].

Cholesterol is a sterol that biosynthesized by all animal cells and is an essential component of all animal cell membranes that is required to maintain membrane fluidity and structural integrity.

U 18666A is an inhibitor of cholesterol transport and synthesis. In rat brain, U 18666A inhibited sterols production in a concentration-dependent way [1]. In cultured Chinese hamster ovary (CHO) cells, U18666A inhibited cholesterol esterification stimulated by low density lipoprotein (LDL)-derived cholesterol and also inhibited LDL receptor activities and 3-hydroxy-3-methylglutaryl-coenzyme A reductase. U18666A caused the accumulation of LDL-derived cholesterol in the lysosomes, suggesting the inhibition of LDL-derived cholesterol transport [2]. In cultured baby hamster kidney cells and human skin fibroblasts (HSF), U18666A reversibly and rapidly inhibited acyl-CoA cholesterol acyl transferase (ACAT) activated by sphingomyelinase in a dose dependent way. In sphingomyelinase-treated HSF cells, U18666A significantly and reversibly reduced the translocation of plasma membrane cholesterol. In mouse Leydig tumor cells, U18666A inhibited steroid hormones secretion stimulated by cyclic AMP in a dose dependent way [3]. In primary cortical neurons, U18666A caused cellular injury and caspase-3 activation. U18666A also caused the accumulation of cholesterol [4].

References:
[1]. Cenedella RJ. Concentration-dependent effects of AY-9944 and U18666A on sterol synthesis in brain. Variable sensitivities of metabolic steps. Biochem Pharmacol, 1980, 29(20): 2751-2754.
[2]. Liscum L, Faust JR. The intracellular transport of low density lipoprotein-derived cholesterol is inhibited in Chinese hamster ovary cells cultured with 3-beta-[2-(diethylamino)ethoxy]androst-5-en-17-one. J Biol Chem, 1989, 264(20): 11796-11806.
[3]. Harmala AS, Porn MI, Mattjus P, Slotte JP. Cholesterol transport from plasma membranes to intracellular membranes is inhibited by 3 beta-[2-(diethylamino)ethoxy]androst-5-en-17-one. Biochim Biophys Acta, 1994, 1211(3): 317-325.
[4]. Cheung NS, Koh CH, Bay BH, et al. Chronic exposure to U18666A induces apoptosis in cultured murine cortical neurons. Biochem Biophys Res Commun, 2004, 315(2): 408-417.

试验操作

细胞实验 [1]:
细胞系	原发性皮层神经元
溶解方法	该化合物在无菌水中的溶解度为100 mM。若获取更高浓度的溶液，可在37℃下孵育10分钟，随后在超声波浴中摇匀。-20℃以下可储存数月。
反应条件	0.1–2.5 μg/ml，37°C，72 h
应用	在原代培养的皮层神经元中，U18666A(2.5 μg/ml, 72 h)诱导细胞毒性。U18666A导致超过50％的细胞存活和主要形态学变化的损失，其特征在于皮质神经元中的细胞收缩和膜起泡。U18666A (0.1–2.5 μg/ml, 72 h)诱导原代培养的皮质神经元细胞损伤和细胞凋亡。
动物实验 [2]:
动物模型	Sprague-Dawley大鼠
给药剂量	皮下注射，10 mg/kg，每四或七天
应用	在新生大鼠中，每周注射U18666A(10 mg/kg, s.c.)，连续4周，导致雄性大鼠癫痫发作阈值降低至惊厥药物氟乙基的水平。
注意事项	由于实验环境的不同，实际溶解度可能与理论值略有不同，请测试室内所有化合物的溶解度。
References: [1]. Cheung N S, Koh C H V, Bay B H, et al. Chronic exposure to U18666A induces apoptosis in cultured murine cortical neurons[J]. Biochemical and biophysical research communications, 2004, 315(2): 408-417. [2]. Bierkamper G G, Cenedella R J. Induction of chronic epileptiform activity in the rat by an inhibitor of cholesterol synthesis, U18666A[J]. Brain research, 1978, 150(2): 343-351.