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AY 9944 dihydrochloride

现货
Catalog No.
A8658
Δ7固醇还原酶抑制剂
组合的产品项目
规格价格库存 数量
10mg
¥ 2,070.00
Ship with 10-15 days

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Background

AY 9944 dihydrochloride is a selective inhibitor of Δ7-sterol reductase with IC50 value of 13 nM [1].

Δ7-sterol reductase (Dhcr7) is an enzyme and plays an important role in catalyzing the production of cholesterol from 7-Dehydrocholesterol through using NADPH [2, 3].

AY 9944 dihydrochloride is a potentΔ7-sterol reductase inhibitor and has higher inhibition thanΔ7-sterol reductase inhibitor BM15766 and triparanol. When tested with Saccharomyces cerevisiae expressed cDNA without an N-terminal 9E10 c-myc epitope (mycD7-ORF) and 5’ noncoding region (D7-ORF), AY 9944 dihydrochloride exhibited highly inhibition on D7-ORF (recombinant humanΔ7-sterol reductase ) with IC50 value of 13 nM [1]. In PBMCs isolated from AIDS patients, AY 9944 treatment exhibited ability to restore the normal mitogenic responses and cytokine profiles [2].

In Sprague-Dawley rats model of Smith-Lemli-Opitz syndrome, administration of AY9944 elevated 7-DHC expression and reduced cholesterol in all biological tissues by inhibitingΔ7-sterol reductase [3].

References:
[1].  Moebius, F.F., et al., Molecular cloning and expression of the human delta7-sterol reductase. Proc Natl Acad Sci U S A, 1998. 95(4): p. 1899-902.
[2].  Achour, A., et al., Restoration of immune response by a cationic amphiphilic drug (AY 9944) in vitro: a new approach To chemotherapy against human immunodeficiency virus type 1. Antimicrob Agents Chemother, 1998. 42(10): p. 2482-91.
[3].   Xu, L., et al., Novel oxysterols observed in tissues and fluids of AY9944-treated rats: a model for Smith-Lemli-Opitz syndrome. J Lipid Res, 2011. 52(10): p. 1810-20.

Chemical Properties

Physical AppearanceA crystalline solid
StorageDesiccate at RT
M.Wt464.3
Cas No.366-93-8
FormulaC22H28Cl2N2.2HCl
SolubilitySoluble in H2O
Chemical NameN-[(2-chlorophenyl)methyl]-1-[4-[[(2-chlorophenyl)methylamino]methyl]cyclohexyl]methanamine;dihydrochloride
SDFDownload SDF
Canonical SMILESC1CC(CCC1CNCC2=CC=CC=C2Cl)CNCC3=CC=CC=C3Cl.Cl.Cl
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
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。

试验操作

细胞实验 [1]:

细胞系

PBMCs

制备方法

在无菌水中的溶解度为50 mM。若配制更高浓度的溶液,一般步骤如下:请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。

反应条件

3 × 10-6 M

实验结果

在感染了HIV-1的PBMCs中,AY 9944 Dihydrochloride恢复促分裂原诱导的以及记忆抗原和超抗原诱导的增殖。经过2周治疗后,HIV-1感染的培养物中死亡CD4 +细胞的百分比与未感染的培养物相当。同时,AY 9944 Dihydrochloride诱导IL-12和干扰素-γ合成(2 ~ 12倍)。

动物实验 [2]:

动物模型

SD大鼠

给药剂量

25 mg/kg;皮下注射

实验结果

接受AY 9944 Dihydrochloride治疗后,大鼠大脑脂筏的胆固醇相对值(平均7.85倍)与对照组数值接近(5.44倍)。上述结果表明7-脱氢胆固醇 (7DHC) 以类似于胆固醇作用的方式促进脂筏形成。 然而,在AY 9944 Dihydrochloride处理大鼠的大脑中,脂筏的蛋白质谱与对照组具有显著的差异。

注意事项

请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。

References:

[1]. Achour, A., et al., Restoration of immune response by a cationic amphiphilic drug (AY 9944) in vitro: a new approach To chemotherapy against human immunodeficiency virus type 1. Antimicrob Agents Chemother, 1998. 42(10): p. 2482-91.

[2]. Keller RK, Arnold TP, Fliesler SJ. Formation of 7-dehydrocholesterol-containing membrane rafts in vitro and in vivo, with relevance to the Smith-Lemli-Opitz syndrome. J Lipid Res. 2004 Feb;45(2):347-55.

质量控制

质量控制和MSDS

批次:

化学结构

AY 9944 dihydrochloride