LRRK2-IN-14
LRRK2-IN-14 (Compound 8) is an orally active LRRK2 inhibitor. LRRK2-IN-14 has an IC50 of 6.3 nM for LRRK2(G2019S) cell activity.LRRK2-IN-14 has an inhibitory effect on hERG (IC50=22 μM). LRRK2-IN-14 has blood-brain barrier permeability.
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- CAS. Nr.: 2942328-06-3
- Formel: C17H18F3N5O2
- Molecular Weight:381.35
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
Pharmacokinetic Analysis in ICR mice[1]
| Route | Dose (mg/kg) | C0 (ng/mL) | Cmax (ng/mL) | Tmax (h) | t1/2 (h) | Vdss (mL/kg) | Clobs (mL/min/kg) | AUC0-last (ng·h/mL) | AUC0-INF (ng·h/mL) | MRT0-INF (h) | F (%) |
| i.v. | 5 | 4101 | / | / | 0.905 | 1233 | 16.3 | 5122 | 5181 | 1.27 | / |
| p.o. | 5 | / | 2803 | 0.083 | 0.709 | / | / | 3657 | 3672 | 1.22 | 70.9 |
| brain | 5 | / | 837 | 0.292 | 0.648 | / | / | 1230 | 1233 | 1.14 | / |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ICR mice[1]
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Dosage:30 mg/kg
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Administration:p.o.; single dose
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Result:Reduced phosphorylated LRRK2 levels to 34%.
Chemical Information
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CAS. Nr. 2942328-06-3
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Molecular Weight 381.35
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Formel C17H18F3N5O2
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SMILES
COC1=C2C=C(C(N(CCCNC3=NC(N2)=NC=C3C(F)(F)F)C)=O)C=C1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)