AY 9944 dihydrochloride
目录号 : GC12429
A cholesterol synthesis inhibitor
Cas No.:366-93-8
Sample solution is provided at 25 µL, 10mM.
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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.
| Cell experiment [1]: | |
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Cell lines |
PBMCs |
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Preparation method |
The solubility of this compound in sterile water is 50 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
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Reacting condition |
3 × 10-6 M |
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Applications |
In HIV-1-infected PBMCs, AY 9944 Dihydrochloride restored mitogen-induced as well as recall antigen- and superantigen-induced proliferation. After 2-week treatment, the percentage of dead CD4+ cells in HIV-1-infected cultures was comparable that in uninfected culture. AY 9944 Dihydrochloride also stimulated IL-12 and interferon-γ production by 2 ~ 12 folds. |
| Animal experiment [2]: | |
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Animal models |
SD rats |
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Dosage form |
25 mg/kg; s.c. |
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Applications |
The relative enrichment of sterol in rafts from AY 9944 Dihydrochloride-treated rat brains (average 7.85 folds) was similar to that from the control group (5.44 folds), which implied that 7-dehydrocholesterol (7DHC) promoted raft formation in a similar way as cholesterol did. However, the protein profiles of rafts from AY 9944 Dihydrochloride-treated rat brains were markedly different from those from the control group. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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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. |
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| Cas No. | 366-93-8 | SDF | |
| 化学名 | N-[(2-chlorophenyl)methyl]-1-[4-[[(2-chlorophenyl)methylamino]methyl]cyclohexyl]methanamine;dihydrochloride | ||
| Canonical SMILES | C1CC(CCC1CNCC2=CC=CC=C2Cl)CNCC3=CC=CC=C3Cl.Cl.Cl | ||
| 分子式 | C22H28Cl2N2.2HCl | 分子量 | 464.3 |
| 溶解度 | DMSO : 5 mg/mL (10.77 mM; Need ultrasonic) ; Water : 5 mg/mL (10.77 mM; Need ultrasonic) | 储存条件 | 4°C, sealed storage, away from moisture |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1538 mL | 10.7689 mL | 21.5378 mL |
| 5 mM | 0.4308 mL | 2.1538 mL | 4.3076 mL |
| 10 mM | 0.2154 mL | 1.0769 mL | 2.1538 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet