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Art. -Nr.: HY-151441

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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.

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CAS. Nr.: 2892451-45-3
Formel: C₂₄H₂₆F₂N₄O₂S
Molecular Weight:472.55

Speicherung:

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

Data Sheet (275 KB)

LRRK2-IN-5 Chemical Structure

CAS. Nr.: 2892451-45-3

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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

Chemical Information

CAS. Nr. 2892451-45-3
Molecular Weight 472.55
Formel C₂₄H₂₆F₂N₄O₂S
SMILES

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

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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