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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- CAS. Nr.: 1207745-58-1
- Formel: C22H17ClFN3O2S
- Molecular Weight:441.91
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
Beschreibung
In Vitro
MK-4409 showed a Kν of 1254 nM in the hERG K+ channel binding assay[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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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CAS. Nr. 1207745-58-1
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Molecular Weight 441.91
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Formel 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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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.
Protokoll
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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.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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