LRRK2-IN-6
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.
- CAS No.: 2892451-17-9
- Formula: C23H24F2N4O2S
- Molecular Weight:458.52
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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. Further protocols information, click here.
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Cell Line:HEK293 cells
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Concentration:0, 30, 100, 300, 1000, 3000, and 10000 nM
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Incubation Time:24 hours
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Result:Reduced GS-LRRK2 pSer935 and GS-LRRK2 pSer1292 autophosphorylation levels over WT-LRRK2.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CD-1 mice[1]
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Dosage:0.5 mg/kg (i.v.) and 5 mg/kg (p.o.)
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Administration:Intravenous injection and oral administration
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Result:
1.19 Route of Administration IV PO Dose (mg/kg) 0.5 5 AUCinf (μM*h) 0.71 11.9 Cmax (μM) 0.53 1.86 Tmax (h) 0.08 1.33 T1/2 (h) 1.09 5.40 MRT (h) 1.17 6.40 CL (mL/min) 26.1 F (%) 174
Chemical Information
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CAS No. 2892451-17-9
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Molecular Weight 458.52
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Formula C23H24F2N4O2S
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SMILES
CC1=C(C(C2=CC=NC=C2)=NN1)C3=CC(F)=C(C(F)=C3)N4CCC5(C4)CCS(=O)(CC5)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
LRRK2-IN-6 Related Classifications
HY-151444 Related Classifications
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