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AY 9944 dihydrochloride
Δ7固醇还原酶抑制剂,AY 9944 是一种特异的胆固醇生物合成 (cholesterol biosynthesis) 抑制剂。AY 9944 抑制 7- 脱氢胆固醇 Δ7- 还原酶 (DHCR7) 酶 (IC50=13 nM)。
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
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。

搜索质检报告(COA)

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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