Iclepertin

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Iclepertin

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:

1421936-85-7

BI-425809

Iclepertin (BI-425809) 是一种有效、选择性且具有口服活性的甘氨酸转运蛋白 1 (GlyT1) 抑制剂。Iclepertin 对 GlyT2 无活性。Iclepertin 可用于阿尔茨海默病和精神分裂症研究。

生物活性

Iclepertin (BI-425809) is a potent, selective and orally activeglycine transporter 1 (GlyT1)inhibitor. Iclepertin is inactive againstGlyT2. Iclepertin can be used for Alzheimer disease and schizophrenia research^[1].

IC₅₀& Target^[1]

GLT1

5.2 mM (IC₅₀, In rat primary neurons )

GLT1

5 nM (IC₅₀, In human SK-N-MC cells)

体外研究
(In Vitro)

Iclepertin inhibits GlyT1 with the IC₅₀values of 5.2 nM in rat primary neurons and 5.0 nM in human SK-N-MC cells^[1].

体内研究
(In Vivo)

Single oral administration of Iclepertin induced a dose-dependent increase of glycine cerebrospinal fluid (CSF) levels. Oral administration of Iclepertin in rats induced a dose‐dependent increase of glycine CSF levels from 30% (0.2 mg/kg, not significant) to 78% (2 mg/kg), relative to vehicle^[1].

Clinical Trial

分子量

512.42

性状

Solid

Formula

C₂₀H₁₈F₆N₂O₅S

CAS 号

1421936-85-7

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 : 11.36 mg/mL(22.17 mM;ultrasonic and warming and heat to 60℃)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	1.9515 mL	9.7576 mL	19.5152 mL
5 mM	0.3903 mL	1.9515 mL	3.9030 mL
10 mM	0.1952 mL	0.9758 mL	1.9515 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。