AY 9944

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AY 9944

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

366-93-8

包装与价格：

包装	价格(元)
5mg	电议
10mg	电议
25mg	电议
50mg	电议
100mg	电议
200mg	电议
500mg	电议

产品介绍

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，其IC₅₀值为 13 nM。AY 9944 引起胆固醇不足和 7DHC 积累。在高剂量下，AY 9944 也可在培养的胚胎中抑制固醇 Δ7-Δ8 异构酶，这会导致胆固醇 8-en-3β-ol 的积累。

生物活性

AY 9944 is a specificcholesterolbiosynthesisinhibitor. AY 9944 inhibits the 7-dehydrocholesterolΔ7-reductase (DHCR7) enzyme with anIC₅₀of 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^[1]^[2]^[3].

IC₅₀& Target

IC50: 13 nM (DHCR7)¹

体外研究
(In Vitro)

AY 9944 (1 μg/mL; 15 h) affects types of free sterol in keratinocytes^[2].

Cell Viability Assay^[2]

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^[3].

Animal Model:	Long–Evans hooded rats^[3].
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.

分子量

464.30

性状

Solid

Formula

C₂₂H₃₀Cl₄N₂

CAS 号

366-93-8

运输条件

Room temperature in continental US; may vary elsewhere.

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)

溶解性数据

In Vitro:

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

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

配制储备液

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

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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。