LRRK2-IN-6

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LRRK2-IN-6

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

LRRK2-IN-6 (compound 22) 是一种口服有效的选择性富含亮氨酸重复蛋白激酶 2 基因 (LRRK2) 抑制剂，抑制 GS LRRK2 和 WT LRRK2 的IC₅₀值分别为 4.6 和 49 μM。LRRK2-IN-6 抑制 LRRK2 Ser1292 和 Ser925 的自磷酸化。LRRK2-IN-6 可以通过血脑屏障。

生物活性

LRRK2-IN-6 (compound 22) is a potent, orally active, selectiveleucine rich repeat protein kinase 2 gene (LRRK2)inhibitor withIC₅₀values of 4.6 and 49 μM for GSLRRK2and WTLRRK2, respectively. LRRK2-IN-6 inhibitsLRRK2Ser1292 and Ser925 autophosphorylation. LRRK2-IN-6 can cross the blood-brain barrier^[1].

IC₅₀& Target

IC50: 4.6 (GS LRRK2) and 49 μM (GS LRRK2)^[1]

体外研究
(In Vitro)

LRRK2-IN-6 (compound 22; 0-10000 nM; 24 h; HEK293 cells) has excellent potency and GS-LRRK2 selectivity^[1].

Western Blot Analysis^[1]

Cell Line:	HEK293 cells
Concentration:	0, 30, 100, 300, 1000, 3000, and 10000 nM
Incubation Time:	24 hours
Result:	Reduced GS-LRRK2 pSer935 and GS-LRRK2 pSer1292 autophosphorylation levels over WT-LRRK2.

体内研究
(In Vivo)

LRRK2-IN-6 (compound 22; 0.5 mg/kg (i.v.) and 5 mg/kg (p.o.); CD-1 mice) has good pharmacokinetic parametershigh and high bioavailability^[1].

Animal Model:

CD-1 mice^[1]

Dosage:

0.5 mg/kg (i.v.) and 5 mg/kg (p.o.)

Administration:

Intravenous injection and oral administration

Result:

1.19

Route of Administration	IV	PO
Dose (mg/kg)	0.5	5
AUC_inf(μM*h)	0.71	11.9
C_max(μM)	0.53	1.86
T_max(h)	0.08	1.33
T_1/2(h)	1.09	5.40
MRT (h)	1.17	6.40
CL (mL/min)	26.1
F (%)		174

分子量

458.52

Formula

C₂₃H₂₄F₂N₄O₂S

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.