AZD9898

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AZD9898

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:

2042347-69-1

AZD9898 是一种口服有效的白三烯-C4 合成酶(LTC4S)抑制剂，IC₅₀值为 0.28 nM。AZD9898 减轻GABA 结合和肝毒性信号。AZD9898 可用于哮喘的研究。

生物活性

AZD9898 is an orally activeleukotriene-C4 synthetase (LTC4S, glutathione S-transferase II)inhibitor, with anIC₅₀of 0.28 nM. AZD9898 mitigates the GABA binding and hepatic toxicity signal. AZD9898 has the potential to treat asthma^[1].

IC₅₀& Target

IC50: 0.28 nM (LTC4S)^[1].

体内研究
(In Vivo)

AZD9898 with the single dose of 100 mg/kg is well tolerated and no safety concerns are raised^[1].

Animal Model:	Rat 6M/group^[1].
Dosage:	10 and 100 mg/kg (forToxicology Study).
Administration:	Sing oral dose.
Result:	Showed no signs of testicular toxicity, and only adaptive changes in the liver due to cytochrome P450 induction which were not judged adverse, providing a 200 fold margin between the no adverse effect level and the predicted human exposure at the predicted therapeutic dose.

Clinical Trial

分子量

457.83

性状

Solid

Formula

C₂₀H₁₉ClF₃N₃O₄

CAS 号

2042347-69-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : ≥ 250 mg/mL(546.05 mM)

*"≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	2.1842 mL	10.9211 mL	21.8422 mL
5 mM	0.4368 mL	2.1842 mL	4.3684 mL
10 mM	0.2184 mL	1.0921 mL	2.1842 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。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。