GSK2578215A 1285515-21-0

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Molecular Weight:

399.42 GSK2578215A is a potent and Selective LRRK2 Kinase Inhibitor with IC50 of 8.9 nM and 10.9 nM for LRRK2 (G2019S) and LRRK2 (WT), respectively.


Biological Activity


GSK2578215A induces a dose-dependent inhibition of Ser910 and Ser935
phosphorylation in both wild-type LRRK2 and LRRK2[G2019S] stably
transfected into HEK293 cells, and induces similar dose-dependent Ser910
and Ser935 dephosphorylation of endogenous LRRK2 in mouse Swiss 3T3
cells. In SH-SY5Y cells, GSK2578215A impairs the Autophagy flux by
altering autophagosome–lysosome fusion, and induces mitophagy though
induction of Drp-1-mediated mitochondrial fission and
mitochondrial-derived ROS signaling.


In vivo, GSK2578215A (100 mg/kg i.p.) inhibits Ser910 and Ser935 phosphorylation in mouse spleen and kidney, but not in brain.


Protocol(Only for Reference)


Animal Study: [1]

Animal Models	Normal mice
Formulation
Dosages	100 mg/kg
Administration	i.p.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species	Baboon	Dog	Monkey	Rabbit	Guinea pig	Rat	Hamster	Mouse
Weight (kg)	12	10	3	1.8	0.4	0.15	0.08	0.02
Body Surface Area (m2)	0.6	0.5	0.24	0.15	0.05	0.025	0.02	0.007
Km factor	20	20	12	12	8	6	5	3

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B Km
	Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×	mouse Km(3)	= 11.2 mg/kg
	rat Km(6)

Chemical Information

Molecular Weight (MW)	399.42
Formula	C24H18FN3O2
CAS No.	1285515-21-0

Storage	3 years -20℃Powder
	6 months-80℃in solvent (DMSO, water, etc.)
Synonyms	N/A

Chemical Name	2-(benzyloxy)-5-(2-fluoropyridin-4-yl)-N-(pyridin-3-yl)benzamide

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Product Categories : Autophagy > LRRK2 Inhibitor