680C91|163239-22-3|-陌孚医药/Medlife

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680C91

目录号: PC15082 纯度: ≥98%

CAS No. :163239-22-3

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PC15082-10mg	10mg	¥2222.50	请登录
PC15082-50mg	50mg	¥8715.00	请登录

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中文名称

680C91

中文别名

6-氟-3-[(1E)-2-(3-吡啶基)乙烯基]-1H-吲哚

英文名称

680C91

英文别名

1H-Indole,6-fluoro-3-[(1E)-2-(3-pyridinyl)ethenyl]-;680C91;6-Fluoro-3-[(E)-2-(3-pyridinyl)vinyl]-1H-indole;MC 1443;1H-Indole,6-fluoro-3-[2-(3-pyridinyl)ethenyl]-, (E)-

Cas No.

163239-22-3

分子式

C₁₅H₁₁N₂F

分子量

238.26

包装储存

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

生物活性

680C91 is an orally active, selective tryptophan 2,3-dioxygenase (TDO) inhibitor with a K_i 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.

性状

Solid

体外研究(In Vitro)

680C91 is a potent (K_i=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.

Medlife 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

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.

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

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

运输条件

Room temperature or refrigerated transportation.

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

[1]. M Salter, et al. The effects of an inhibitor of tryptophan 2,3-dioxygenase and a combined inhibitor of tryptophan 2,3-dioxygenase and 5-HT reuptake in the rat. Neuropharmacology. 1995 Feb;34(2):217-27. [Information]

[2]. M Salter, et al. The effects of a novel and selective inhibitor of tryptophan 2,3-dioxygenase on tryptophan and serotonin metabolism in the rat. Biochem Pharmacol. 1995 May 17;49(10):1435-42. [Information]

[3]. Dang-Dang Li, et al. Differential expression and regulation of Tdo2 during mouse decidualization. J Endocrinol. 2013 Dec 2;220(1):73-83.

[4]. Tsai-Der Chuang, et al. Tryptophan catabolism is dysregulated in leiomyomas. Fertil Steril. 2021 Oct;116(4):1160-1171. [Information]

[5]. Sophie Imbeault, et al. Effects of IDO1 and TDO2 inhibition on cognitive deficits and anxiety following LPS-induced neuroinflammation. Acta Neuropsychiatr. 2020 Feb;32(1):43-53. [Information]

溶解度数据

体外研究:

DMSO : 125 mg/mL (524.64 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	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

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。-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。

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Data Sheet

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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