DDR-TRK-1 - CAS:1934246-19-1 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	DDR-TRK-1
英文名称:	DDR-TRK-1
别名:	DDR-TRK-1 (R)-4-Methyl-N-(3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl)-2-(pyrimidin-5-yl)-1,2,3,4-tetrahydroisoquinoline-7-carboxamide
CAS No:	1934246-19-1	分子式:	C₂₆H₂₃F₃N₆O	分子量:	492.5
CAS No:	1934246-19-1
分子式:	C₂₆H₂₃F₃N₆O
分子量:	492.5

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D11299 DDR-TRK-1 (psaitong)

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包装规格：

100mg 250mg 1g in glass bottle

产品描述：

基本信息

产品编号：D11299
产品名称：DDR-TRK-1
CAS:	1934246-19-1	储存条件	粉末	-20℃	四年
分子式：	C26H23F3N6O		溶于液体	-80℃	两年
分子量	492.50
化学名：
Solubility (25°C)	体外	DMSO
		Ethanol
		Water
	体内（现配现用）
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
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。

生物活性

产品描述	一种选择性的圆盘状受体 1 (DDR1) 抑制剂，其 IC50 值为 9.4nM。DDR-TRK-1 也抑制 TRK 激酶家族。
靶点/IC₅₀	IC50: 9.4nM (DDR1)
体外研究	DDR-TRK-1 is a promising candidate, with an IC50 value of 9.4nM against DDR1. DDR-TRK-1 also exhibits reasonable pharmacokinetic (PK) properties, with an oral bioavailability of 66.8% and a T1/2 value of 1.25h at an oral dose of 20mg/kg in rats. However, the area under concentration−time curve (AUC) value of DDR-TRK-1 in mice is obviously higher than that in rats, suggesting its good absorption property in mice. The DDR1 inhibition of DDR1-IN-3 is further validated by determining its binding affinity with the DDR1 protein. It is shown that DDR-TRK-1 bounds tightly to DDR1, with a binding constant (Kd) value of 4.7nM.
体内研究	DDR-TRK-1 prevents these BLM-induced pathological changes in a dose-dependent manner. These results agree with the expression levels of fibrotic markers in lung tissue lysates, including fibronectin and α-smooth muscle actin (SMA). Further analyses also reveal that the administration of DDR-TRK-1 cause a dose-dependent suppression in the content of hydroxyproline, a unique amino acid found in collagen. The above data collectively indicate the promising therapeutic potential of DDR-TRK-1 against the BLM-induced pulmonary fibrosis.

推荐实验方法(仅供参考)

细胞实验:

Panc-1 cells are plated at low density in media in the presence or absence of controls or the indicated concentration of DDRTRK-1 (0.016, 0.0625, 0.25, 1μM). Colony formation is evaluated after 1.5-2 weeks by fixing and staining with crystal violet.The effect of DDR1-IN-3 on cell migration is determined through a‘scratch’assay. Panc-1 cells are grown to confluence in a 6 well dish. A scratch is made using a p20 pipette tip and cell migration into the wound is determined at 12, 24, 48, 60, and 72 hrs. The effect of control compounds or DDR-TRK-1 at the indicated concentrations is determined at each time point.

动物实验:

Mice

To induce pulmonary damage, 6- to 8-week-old sex- and age-matched wild type or slie mice (at least five animals per group)are intranasally dropped with bleomycin at 5mg/kg BW. The inhibitors (e.g., DDR-TRK-1) are dissolved in water at a concentration of 5 mg/mL and given to the mice orally by gavage twice a day. Hydroxyproline accounts for 13.4% of the total amino acids of collagen; thus its content can be used to reflect the severity of fibrosis. A commercial hydroxyproline kit is used. Briefly, fresh lung tissues are weighted and hydrolyzed to release hydroxyproline. After a series of chemical reactions, a pink color solution is formed and then subjected to measurement of absorbance at 560nm. The hydroxyproline content of each sample is calculated by comparing with the standards.

保存条件：

-20℃

UN码：

HazardClass：

危害声明：

安全说明：

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