AY 9944 dihydrochloride|366-93-8|-陌孚医药/Medlife

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AY 9944 dihydrochloride

目录号: PC15846 纯度: ≥98%

CAS No. :366-93-8

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中文名称	AY 9944 dihydrochloride
中文别名	N-1-,N-3-二甲基-β-丙氨
英文名称	AY 9944 dihydrochloride
英文别名	1,4-Cyclohexanedimethanamine,N1,N4-bis[(2-chlorophenyl)methyl]-, hydrochloride (1:2), trans-;AY 9944;AY 9944 dihydrochloride;AY-9944;trans-1,4-bis(chlorobenzylaminomethyl)-cyclohexane dihydrochloride;1,4-BIS(2-CHLOROBENZYLAMINOMETHYL)CYCLOHEXANE DIHYDROCHLORIDE;trans-N,N-bis[2-ChlorophenylMethyl]-1,4-cyclohexanediMethanaMinedihydrochloride
Cas No.	366-93-8
分子式	C₂₂H₂₈N₂Cl₂^.HCl
分子量	427.84
包装储存	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

生物活性

AY 9944 is a specific cholesterol biosynthesis inhibitor. AY 9944 inhibits the 7-dehydro cholesterol Δ7-reductase (DHCR7) enzyme with an IC₅₀ of 13 nM. AY 9944 causes hypocholesterolemia and accumulation of 7DHC. At high doses, AY 9944 inhibits also in cultured embryos sterol Δ7-Δ8 isomerase, which causes the accumulation of cholest-8-en-3β-ol.

性状

Solid

IC50 & Target[1][2]

IC50: 13 nM (DHCR7)

体外研究(In Vitro)

AY 9944 (1 μg/mL; 15 h) affects types of free sterol in keratinocytes.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

Cell Line:	Human foreskin keratinocytes
Concentration:	1 μg/mL
Incubation Time:	15 hours
Result:	Inhibited the synthesis of cholesterol and desmosterol, but increased 7-dehydrocholesterol and zymosterol synthesis.

体内研究(In Vivo)

AY 9944 (7.5 mg/kg; i.h. every 6 days once from postnatal day 2 to postnatal day 20) reduces brain cholesterol until 400 days after stop treatment.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Long–Evans hooded rats.
Dosage:	7.5 mg/kg
Administration:	Subcutaneous injection; 7.5 mg/kg every 6 days once; from postnatal day 2 to postnatal day 20
Result:	Reduced brain cholesterol and increased 7-dehydrocholesterol in all brain regions of rats till the treatment stopped for 400 days and showed a more severe effect on the change of sterols in plasma and liver of female rats.

运输条件

Room temperature or refrigerated transportation.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

参考文献

[1]. Moebius FF, et al. Molecular cloning and expression of the human delta7-sterol reductase. Proc Natl Acad Sci U S A. 1998 Feb 17;95(4):1899-902. [Information]

[2]. Nemanic MK, et al. 体外研究 synthesis of vitamin D-3 by cultured human keratinocytes and fibroblasts: action spectrum and effect of AY-9944. Biochim Biophys Acta. 1985 Sep 6;841(3):267-77. [Information]

[3]. Cortez MA, et al. Brain sterols in the AY-9944 rat model of atypical absence seizures. Epilepsia. 2002 Jan;43(1):3-8. [Information]

溶解度数据

体外研究:

DMSO : 5 mg/mL (10.77 mM; Need ultrasonic)

H₂O : 5 mg/mL (10.77 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	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

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。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。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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