2. Autophagy
  3. LRRK2
  4. LRRK2-IN-6

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。

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LRRK2-IN-6 Chemical Structure

LRRK2-IN-6 Chemical Structure

CAS No. : 2892451-17-9

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LRRK2-IN-6 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

LRRK2-IN-6 (compound 22) is a potent, orally active, selective leucine rich repeat protein kinase 2 gene (LRRK2) inhibitor with IC50 values of 4.6 and 49 μM for GS LRRK2 and WT LRRK2, respectively. LRRK2-IN-6 inhibits LRRK2 Ser1292 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].

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

LRRK2-IN-6 相关抗体:

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].

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

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
AUCinf (μM*h) 0.71 11.9
Cmax (μM) 0.53 1.86
Tmax (h) 0.08 1.33
T1/2 (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
CAS 号
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.
纯度 & 产品资料
参考文献

LRRK2-IN-6 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

LRRK2-IN-62892451-17-9LRRK2Leucine-rich repeat kinase 2GS LRRK2WT LRRK2Ser1292Ser925autophosphorylationblood-brain barrierHEK293 cellsInhibitorinhibitorinhibit

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