LRRK2-IN-6

Cat. No.: HY-151444: FAQs
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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.

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

LRRK2-IN-6 Chemical Structure

CAS No. : 2892451-17-9

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Description

IC₅₀ & Target

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

In Vitro

LRRK2-IN-6 (compound 22; 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.

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.

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].

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
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

Molecular Weight

458.52

Formula

C₂₃H₂₄F₂N₄O₂S

CAS No.

2892451-17-9

SMILES

CC1=C(C(C2=CC=NC=C2)=NN1)C3=CC(F)=C(C(F)=C3)N4CCC5(C4)CCS(=O)(CC5)=O

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

Handling Instructions (2659 KB)

References

[1]. Leśniak RK, et, al. Discovery of azaspirocyclic 1H-3,4,5-Trisubstitued pyrazoles as novel G2019S-LRRK2 selective kinase inhibitors. Eur J Med Chem. 2022 Nov 15;242:114693. [Content Brief]

LRRK2-IN-6 Related Classifications

Neurological Disease

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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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