1. Autophagy
  2. LRRK2
  3. LRRK2-IN-5

LRRK2-IN-5 (compound 25) is a potent, orally active, selective leucine rich repeat protein kinase 2 gene (LRRK2) inhibitor with IC50 values of 1.2 and 16 μM for GS LRRK2 and WT LRRK2, respectively. LRRK2-IN-5 inhibits LRRK2 Ser1292 and Ser925 autophosphorylation. LRRK2-IN-5 can cross the blood-brain barrier.

For research use only. We do not sell to patients.

LRRK2-IN-5 Chemical Structure

LRRK2-IN-5 Chemical Structure

CAS No. : 2892451-45-3

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Description

LRRK2-IN-5 (compound 25) is a potent, orally active, selective leucine rich repeat protein kinase 2 gene (LRRK2) inhibitor with IC50 values of 1.2 and 16 μM for GS LRRK2 and WT LRRK2, respectively. LRRK2-IN-5 inhibits LRRK2 Ser1292 and Ser925 autophosphorylation. LRRK2-IN-5 can cross the blood-brain barrier[1].

IC50 & Target

IC50: 1.2 (GS LRRK2) and 16 μM (GS LRRK2)[1]

In Vitro

LRRK2-IN-5 (compound 25; 0-10000 nM; 24 h; HEK293 cells) has excellent potency and GS-LRRK2 selectivity[1].

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

Cell Viability Assay[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.
In Vivo

LRRK2-IN-5 (compound 25; 0.5 mg/kg (i.v.) and 5 mg/kg (p.o.); CD-1 mice) has good pharmacokinetic parametershigh and high bioavailability[1].

MedChemExpress (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) 0.51 1.44
Cmax (μM) 0.61 0.60
Tmax (h) 0.08 0.50
T1/2 (h) 0.45 1.46
MRT (h) 0.65 2.35
CL (mL/min) 34.3
F (%) 28
Molecular Weight

472.55

Formula

C24H26F2N4O2S

CAS No.
SMILES

CC1=NC=CC(C2=NNC(C)=C2C3=CC(F)=C(C(F)=C3)N4CCC5(C4)CCS(=O)(CC5)=O)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
References
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LRRK2-IN-5 Related Classifications

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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.

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LRRK2-IN-5
Cat. No.:
HY-151441
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