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 No.: 2892451-45-3
- Formule: C24H26F2N4O2S
- Masse moléculaire:472.55
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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.
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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) 0.51 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
Chemical Information
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CAS No. 2892451-45-3
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Masse moléculaire 472.55
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Formule C24H26F2N4O2S
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SMILES
CC1=NC=CC(C2=NNC(C)=C2C3=CC(F)=C(C(F)=C3)N4CCC5(C4)CCS(=O)(CC5)=O)=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
LRRK2-IN-5 Related Classifications
HY-151441 Related Classifications
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