DN-1289,3026597-15-6

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DN-1289

CAS No. :

MCE 国际站：DN-1289

产品活性：DN-1289 是一种口服有效的、选择性的抑制剂，靶向双亮氨酸拉链激酶 (DLK; IC₅₀=17 nM) 和亮氨酸拉链轴承激酶 (LZK; IC₅₀=40 nM)。DN-1289 对小鼠模型中视神经挤压 (ONC) 诱导的 p-c-Jun 有显著的衰减作用。DN-1289 具有良好的体内血浆半衰期和血脑屏障渗透性。

研究领域：MAPK/ERK Pathway

作用靶点：JNK

In Vitro: DN-1289 (compound 14) (0.1, 0.3, and 1 μM; 0-20 h) can block axon degeneration in dorsal root ganglion (DRG) neurons induced by nerve growth factor (NGF) withdrawal.
DN-1289 (0.1, 0.3, and 1 μM; 0-20 h) inhibits the activation of caspases in DRG neurons over time induced by NGF withdrawal.

In Vivo: DN-1289 (compound 14) (100 mg/kg and 150 mg/kg; i.p.; once daily for 10-15 d) is well-tolerated in mice model.
DN-1289 (150 mg/kg; p.o.; b.i.d. for 10 d) inhibits phosphorylation of c-Jun in an acute injury model with optic nerve crush (ONC) application.

Pharmacokinetic Analysis

Species	Route	Dose (mg/kg)	plasma Cmax (μM)	plasma AUC0-24 h (μM·h)	CLp (mL/min/kg)	CLu (mL/min/kg)	Vd (L/kg)	t1/2 (h)	F (%)	Kpuu (AUC)	brain AUC0-2 h (μM·h)
rat	IV	1	1.09	2.42	14.7	150	6.7	6.5	/	0.6	4.05
	PO	3	0.58	3.9	/	/	/	4.6	52	/	/
mouse	IV	1	1.06	4.06	8.6	200	4.7	6.8	/	/	/
	PO	10	2.32	21.9	/	/	/	7.9	56	0.4	6.91
	PO	150	24.9	324	/	/	/	23.7	53	/	/
	IP	100	15.4	280	/	/	/	23.7	53	/	/
cyno	IV	0.5	0.746	2.79	6.1	64	3.4	7.9	/	/	/

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