LRRK2-IN-5

Cat. No.: HY-151441: FAQs
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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

CAS No. : 2892451-45-3

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Description

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
AUC_inf (μM*h)	0.51	1.44
C_max (μM)	0.61	0.60
T_max (h)	0.08	0.50
T_1/2 (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.

2892451-45-3

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

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-5 Related Classifications

Neurological Disease

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

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-52892451-45-3LRRK2Leucine-rich repeat kinase 2GS LRRK2WT LRRK2Ser1292Ser925autophosphorylationblood-brain barrierHEK293 cellsInhibitorinhibitorinhibit

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