AY 9944 dihydrochloride
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
AY 9944 dihydrochloride是Δ7固醇还原酶的选择性抑制剂,IC50值为13 nM [1].
Δ7固醇还原酶(Dhcr7)是一种酶类,在利用NADPH催化7-脱氢胆甾醇生成胆固醇中发挥重要作用[2, 3].
AY 9944 dihydrochloride是Δ7固醇还原酶的高效抑制剂,比Δ7固醇还原酶抑制剂BM15766和曲帕拉醇具有更高的抑制活性.在表达无N-末端9E10 c-myc表位(mycD7-ORF)和5’端非编码区(D7-ORF)的cDNA的啤酒酵母细胞实验中,AY 9944 dihydrochloride高效抑制D7-ORF(重组人Δ7固醇还原酶)活性,IC50值为13 nM [1].在AIDS病人分离出的PBMCs中,AY 9944处理具有恢复正常促有丝分裂反应和细胞因子的能力[2].
在SD大鼠Smith-Lemli-Opitz综合征模型中,给予AY 9944能通过抑制Δ7固醇还原酶,从而在所有生物组织中提高7-DHC表达并降低胆固醇[3].
参考文献:
[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.
Physical Appearance | A crystalline solid |
Storage | Desiccate at -20°C |
M.Wt | 464.3 |
Cas No. | 366-93-8 |
Formula | C22H28Cl2N2·2HCl |
Solubility | Soluble in H2O |
Chemical Name | N,N'-(((1r,4r)-cyclohexane-1,4-diyl)bis(ethane-2,1-diyl))bis(2-chloroaniline) dihydrochloride |
SDF | Download SDF |
Canonical SMILES | C1CC(CCC1CNCC2=CC=CC=C2Cl)CNCC3=CC=CC=C3Cl.Cl.Cl |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 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。 |
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. |
质量控制和MSDS
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