FAAH/MAGL-IN-2
FAAH/MAGL-IN-2 is a potent, reversible, orally active, and cross the blood-brain barrier FAAH and MAGL inhibitor with IC50s of 11 nM and 36 nM (Kis of 28 nM and 60 nM), respectively . FAAH/MAGL-IN-2 has the potential to research neuropathic pain without causing locomotion impairment.
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- CAS No.: 2765077-82-3
- Formule: C15H13Cl2N3O3S
- Masse moléculaire:386.25
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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: 11 nM (FAAH); 36 nM (MAGL)[1]
In Vitro
FAAH/MAGL-IN-2 (compound 14) (1, 3, 10, 30, 100 μM) shows potent neuroprotection effect[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
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Cell Line:SH-SY5Y cells
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Concentration:1, 3, 10, 30, 100 μM
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Incubation Time:24 h
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Result:Showed potent neuroprotection effect.
In Vivo
FAAH/MAGL-IN-2 (5, 10, 20 mg/kg) has the potential to treat neuropathic pain without causing locomotion impairment[1].
FAAH/MAGL-IN-2 (2000 mg/kg; p.o.; female rats) shows well tolerated and safe up to 2000 mg/kg in the oral dose and did not alter the liver enzymes activity[1].
FAAH/MAGL-IN-2 (20 mg/kg; p.o.) shows a good absorption behavior after oral administration[1].
Pharmacokinetic Parameters of JAK1/TYK2-IN-2 in 200–250 g, male Wistar rats[1].
| Pharmacokinetic parameters | Results (Plasma) |
| Cmax (μg/mL) | 22.04±2.5 |
| Tmax (h) | 0.5 |
| AUC(0-t) (μg min/mL) | 535±1.5 |
| t1/2 (h) | 20.58 |
| MRT 0-inf (h) | 0.5 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nerve-injured rats (CCI model)[1]
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Dosage:5, 10, 20 mg/kg
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Administration:
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Result:Significantly increased paw withdrawal threshold and attenuated tail flick latency in nerve injured rats.
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Animal Model:200–250 g, male Wistar rats[1]
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Dosage:20 mg/kg
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Administration:Oral administration
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Result:Showed a good absorption behavior after oral administration.
Chemical Information
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CAS No. 2765077-82-3
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Masse moléculaire 386.25
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Formule C15H13Cl2N3O3S
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SMILES
O=C(N/N=C\C1=C(Cl)C=CC=C1Cl)NC2=CC=C(S(=O)(C)=O)C=C2
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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)
FAAH/MAGL-IN-2 Related Classifications
HY-143264 Related Classifications
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