MK-4409
MK-4409 is an orally active and blood-brain barrier-penetrant fatty acid amide hydrolase (FAAH) inhibitor (human IC50 = 11 nM; rat IC50 = 11 nM) that reversibly and non-covalently inhibits this serine hydrolase, elevating endogenous fatty acid ethanolamides. MK-4409 alleviates inflammatory and neuropathic pain, with a long duration of action, and reduces edema. MK-4409 can be used for research on inflammatory and neuropathic pain.
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- No. CAS: 1207745-58-1
- Fòrmula: C22H17ClFN3O2S
- Peso molecular:441.91
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | T1/2 | CL | Vd | F |
|---|---|---|---|---|---|---|
| Rat[3] | 1 mg/kg | i.v. | 4.3 h | 20 mL/min/kg | 6.2 L/kg | 120 % |
In Vivo
MK-4409 (3 mg/kg; oral) alleviates neuropathic pain in the rat spinal nerve ligation (SNL) model, with a duration of action lasting up to 24 h[2].
MK-4409 (30 mg/kg; oral; single administration) demonstrated excellent efficacy in the rat CFA inflammatory pain model, reversing 70-71% of tactile allodynia at 30 mg/kg and maintaining efficacy for more than 10 days without tachyphylaxis[3].
MK-4409 (3-100 mg/kg) produced approximately 50% analgesic effects at doses of 3, 30, and 100 mg/kg in the rat SNL neuropathic pain model, and did not cause motor skill impairment at doses up to 100 mg/kg[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rat[2]
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Dosage:10 mg/kg
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Administration:p.o.
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Result:Reduced inflammatory pain in the CFA model at a 10 mg/kg oral dose with a long duration of action until 24 h post-dose.
No apparent side effects were observed up to a dose of 100 mg/kg.
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Animal Model:Rat[2]
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Dosage:3 mg/kg
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Administration:p.o.
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Result:Attenuated neuropathic pain in the SNL model at a 3 mg/kg oral dose with a long duration of action until 24 h post-dose.
No apparent side effects were observed up to a dose of 100 mg/kg.
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Animal Model:Rats[3]
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Dosage:30 mg/kg (acute model); 10 mg/kg (acute model); 30 mg/kg (chronic model)
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Administration:p.o.; single dose (acute model); p.o.; daily; 10 days (chronic model)
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Result:Showed 70% and 71% reversal of allodynia at 1 h and 3 h time points, respectively, at 30 mg/kg.
Showed 49% and 51% reversal at 1 h and 3 h, respectively, at 10 mg/kg.
Showed excellent efficacy out to 10 days with no tachyphylaxis apparent at 30 mg/kg.
Reduced edema observed in the animals over several days.
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Animal Model:Rats[3]
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Dosage:3, 30, 100 mg/kg
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Administration:single dose
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Result:Provided roughly 50% analgesia at all three doses (3, 30, and 100 mg/kg).
Did not show any effect in the concomitant rota-rod assay at doses as high as 100 mg/kg.
Chemical Information
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No. CAS 1207745-58-1
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Peso molecular 441.91
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Fòrmula C22H17ClFN3O2S
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SMILES
CC(C)(O)C(C=C1)=NC=C1C2=C(SC3=NC=C(Cl)C=C3)OC(C4=CC=C(F)C=C4)=N2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MK-4409 Related Classifications
HY-12909 Related Classifications
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