GNE-3511,1496581-76-0

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GNE-3511

CAS No. : 1496581-76-0

MCE 国际站：GNE-3511

产品活性：GNE-3511 是一种生物可利用性和脑渗透 dual leucine zipper kinase (DLK) 抑制剂，具有口服活性，其 K_i 值为 0.5 nM。GNE-3511 可穿过血脑屏障，被用于神经退行性疾病的研究。

研究领域：MAPK/ERK Pathway

作用靶点：MAP3K

In Vitro: GNE-3511 has inhibitory activity for p-JNK and DRG with IC₅₀ values of 30 nM and 107 nM, respectively.
GNE-3511 has kinase selectivity for MKK4, MKK7, JNK1, JNK2, JNK3, MLK1, MLK2 and MLK3 with IC₅₀ values of ＞5000 nM, ＞5000 nM, 129 nM, 514 nM, 364 nM, 67.8 nM, 767 nM and 602 nM, respectively.
GNE-3511 displays concentration-dependent protection of neurons from degeneration in vitro.

In Vivo: GNE-3511 (oral gavage; 75 mg/kg; single) suppresses CYP-induced nociceptive behavior by inhibiting DLK in mice.
GNE-3511 (oral gavage; 75 mg/kg; single) suppresses CYP-induced edema and hemorrhage in mouse bladder.
GNE-3511 (iv.; 1 mg/kg or po.; 5 mg/kg) exhibits moderate in vivo plasma clearances, moderate volumes of distribution, short half-lives, and brain penetration.
Pharmacokinetic Parameters of GNE-3511 (iv.; 1 mg/kg or po.; 5 mg/kg).

species	CLp (mL/min/kg	Vdss (L/kg	t1/2 (h)	F (%)	Bu/Pu	CSF/Pu
mouse	56	2.5	0.6	45	0.24 at 6 h
rat	30	3.7	1.8	63	0.7	0.4
dog	41	6.5	4	32		0.4
cynomolgous	16	3.1	2.4	19		0.6

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