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AY 9944 dihydrochloride

Katalog-Nr.GC12429

AY 9944 Dihydrochlorid ist ein spezifischer Hemmer der Cholesterinbiosynthese.

Products are for research use only. Not for human use. We do not sell to patients.

AY 9944 dihydrochloride Chemische Struktur

Cas No.: 366-93-8

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5mg
90,00 $
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10mg
153,00 $
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25mg
315,00 $
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50mg
495,00 $
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100mg
792,00 $
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

View current batch:

Protocol

Cell experiment [1]:

Cell lines

PBMCs

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.

Reacting condition

3 × 10-6 M

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]:

Animal models

SD rats

Dosage form

25 mg/kg; s.c.

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.

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.

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.

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

Cas No. 366-93-8 SDF
Chemical Name 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
Formula C22H28Cl2N2.2HCl M.Wt 464.3
Löslichkeit DMSO : 5 mg/mL (10.77 mM; Need ultrasonic) ; Water : 5 mg/mL (10.77 mM; Need ultrasonic) Storage 4°C, sealed storage, away from moisture
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
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
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Gewicht
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Konzentration
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Inhalt
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**Bei der Herstellung von Stammlösungen ist immer das chargenspezifische Molekulargewicht von

Berechnen

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 25 reference(s) in Google Scholar.)

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