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AY 9944 dihydrochloride

Catalog No.
A8658
Hedgehog Inhibitor
Grouped product items
SizePriceStock Qty
5mg
$100.00
In stock
10mg
$160.00
In stock
25mg
$320.00
In stock
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

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Background

AY 9944 dihydrochloride (CAS 366-93-8) is a selective inhibitor of Δ7-sterol reductase (Dhcr7), an enzyme involved in cholesterol biosynthesis through NADPH-dependent conversion of 7-dehydrocholesterol to cholesterol. AY 9944 dihydrochloride inhibits recombinant human Δ7-sterol reductase expressed in yeast cells with an IC50 of 13 nM. In an SD rat model of Smith-Lemli-Opitz syndrome, AY 9944 treatment leads to increased accumulation of 7-dehydrocholesterol and decreased cholesterol levels across various tissues. Additionally, in PBMCs isolated from AIDS patients, AY 9944 intervention restored mitogenic responses and cytokine production, suggesting research applications in immunological studies and cholesterol metabolism disorders.

Product Citation

Chemical Properties

Physical AppearanceA crystalline solid
StorageDesiccate at -20°C
M.Wt464.3
Cas No.366-93-8
FormulaC22H28Cl2N2·2HCl
SolubilitySoluble in H2O
Chemical NameN,N'-(((1r,4r)-cyclohexane-1,4-diyl)bis(ethane-2,1-diyl))bis(2-chloroaniline) dihydrochloride
SDFDownload SDF
Canonical SMILESC1CC(CCC1CNCC2=CC=CC=C2Cl)CNCC3=CC=CC=C3Cl.Cl.Cl
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

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.

Quality Control

Chemical structure

AY 9944 dihydrochloride

Related Biological Data

AY 9944 dihydrochloride