680C91,98.16%

产品编号:Bellancom-108681| CAS NO:163239-22-3| 分子式:C15H11FN2| 分子量:238.26

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用,

货号 包装 价格 库存与货期 购买量 操作
Bellancom-108681
900.00 杭州 北京(现货)
Bellancom-108681
1400.00 杭州 北京(现货)
Bellancom-108681
3200.00 杭州 北京(现货)
Bellancom-108681
4800.00 杭州 北京(现货)

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680C91

产品介绍 680C91 是一种口服有效的,选择性色氨酸 2,3-双加氧酶 (TDO) 抑制剂,Ki 为 51 nM。TDO 是色氨酸分解代谢的关键酶。680C91 可用于肿瘤免疫和阿尔茨海默症的研究。
生物活性

680C91 is an orally active, selective tryptophan 2,3-dioxygenase (TDO) inhibitor with a Ki of 51 nM. TDO is the key enzyme of tryptophan catabolism. 680C91 can be used for the research of cancer immunotherapy and Alzheimer’s Disease[4].

体外研究

680C91 is a potent (Ki=51 nM) and selective TDO inhibitor with no inhibitory activity against indoleamine 2,3-dioxygenase, monoamine oxidase A and B, 5-HT uptake and 5-HT1A,1D,2A and 2C receptors at a concentration of 10 μM.
680C91 inhibits the catabolism of tryptophan by rat liver cells and rat liver perfused in situ.
Tdo2 could regulate cell proliferation and stimulate the expression of decidual marker Dtprp in the uterine stromal cells and decidual cells. Tdo2 inhibitor 680C91 also inhibits the prolifer ation activity of uterine decidual cells at 24 h.
Treatment of leiomyoma smooth muscle cell (LSMC) and myometrial smooth muscle cell (MSMC) spheroids with 680C91 (25 and 50 μM) significantly represses the expression of collagen type I (COL1A1) and type III (COL3A1) in a dose-dependent manner[4].

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

Cell Proliferation Assay

Cell Line: Uterine stromal cells
Concentration: 0.01, 0.05, 0.1, 0.5, 1, 5, and 10 μM
Incubation Time: 24 hours
Result: The proliferation activity of stromal cells was significantly decreased at 5 and 10 μM.

Western Blot Analysis[4]

Cell Line: MSMC and LSMC
Concentration: 25 and 50 μM
Incubation Time: 48 hours
Result: Significantly reduced the expression of COL1A1 and COL3A1 in LSMC spheroids with no significant effect on expression of these proteins in MSMC spheroids.
体内研究
(In Vivo)

680C91 (a dose of 15 mg/kg for acute treatment ) elevates tryptophan in brain[5].

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

Animal Model: Male C57Bl6/NCrl mice aged 13-18 weeks[5]
Dosage: 15 mg/kg
Administration: Administered per os
Result: Caused a significant increase in brain tryptophan.
体内研究

680C91 (a dose of 15 mg/kg for acute treatment ) elevates tryptophan in brain[5].

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

Animal Model: Male C57Bl6/NCrl mice aged 13-18 weeks[5]
Dosage: 15 mg/kg
Administration: Administered per os
Result: Caused a significant increase in brain tryptophan.
体内研究

680C91 (a dose of 15 mg/kg for acute treatment ) elevates tryptophan in brain[5].

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

Animal Model: Male C57Bl6/NCrl mice aged 13-18 weeks[5]
Dosage: 15 mg/kg
Administration: Administered per os
Result: Caused a significant increase in brain tryptophan.
性状Solid
溶解性数据
In Vitro: 

DMSO : 125 mg/mL (524.64 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.1971 mL 20.9855 mL 41.9710 mL
5 mM 0.8394 mL 4.1971 mL 8.3942 mL
10 mM 0.4197 mL 2.0985 mL 4.1971 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°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

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
参考文献

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