MK-5661
MK-5661 is an orally potent NaV1.8 voltage-gated sodium channel inhibitor with an EC50 of 4.3 nM. MK-5661 selectively inhibits peripheral nociceptive signaling mediators. MK-5661 reduces capsaicin-induced spontaneous nociceptive behaviors in humanized rats and attenuates capsaicin-induced skin flushing responses in rhesus monkeys. MK-5661 is applicable for pain-related research.
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- No. CAS: 2417328-24-4
- Fòrmula: C18H18F5N5O3S
- Peso molecular:479.42
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Descripciòn
IC50 & Target
[1]|
Nav1.8 4.3 nM (EC50) |
In Vitro
MK-5661 potently modulates human NaV1.8 channels stably expressed in HEK 293 cells with an EC50 of 4.3 nM and a VLE of 6.5[1].
MK-5661 is highly selective for human NaV1.8 channels, with IC50 values greater than 30 μM against human NaV1.2, NaV1.4, NaV1.5, NaV1.6, and NaV1.7 channels stably expressed in HEK-293 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | CL | Vss | T1/2 | F |
|---|---|---|---|---|---|---|
| Rat[1] | 2 mg/kg | i.v. | 19 mL/min/kg | 7.1 L/kg | 4.4 h | / |
| Rat[1] | 10 mg/kg | p.o. | 317 mL/min/kg | 118 L/kg | 4.4 h | ~100 % |
| Dog[1] | 1 mg/kg | i.v. | 0.23 mL/min/kg | 0.63 L/kg | 35 h | / |
| Dog[1] | 2 mg/kg | p.o. | 14 mL/min/kg | 37 L/kg | 35 h | 78 % |
| Rhesus monkey[1] | 1 mg/kg | i.v. | 1.5 mL/min/kg | 1.8 L/kg | 16 h | / |
| Rhesus monkey[1] | 2 mg/kg | p.o. | 29 mL/min/kg | 35 L/kg | 16 h | ~100 % |
In Vivo
MK-5661 (0.2-2 mg/kg; p.o.; single dose) significantly attenuates capsaicin-induced dermal flare area in rhesus macaques[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Humanized rats[1]
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Dosage:0.1 mg/kg, 0.3 mg/kg, 1.0 mg/kg, 3.0 mg/kg, 10.0 mg/kg
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Administration:p.o.; single dose
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Result:Produced a dose-dependent reduction in capsaicin-induced flinch counts.
Reached unbound plasma concentrations of 0.28 nM (0.1 mg/kg), 1.0 nM (0.3 mg/kg), 8.0 nM (1.0 mg/kg), 28 nM (3.0 mg/kg), and 150 nM (10.0 mg/kg), corresponding to 0.07-, 0.2-, 2-, 7-, and 35-fold the human NaV1.8 EC50 (4.3 nM), respectively.
Showed a significant main effect of treatment via one-way ANOVA.
Demonstrated significant flinch reductions at 0.3 mg/kg and 1.0, 3.0, 10.0 mg/kg relative to vehicle.
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Animal Model:Rhesus macaques[1]
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Dosage:0.2 mg/kg, 0.6 mg/kg, 2.0 mg/kg
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Administration:p.o.; single dose
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Result:Reduced capsaicin-induced flare area in a dose-dependent manner.
Reached unbound plasma concentrations of 9 nM (0.2 mg/kg), 42 nM (0.6 mg/kg), and 150 nM (2.0 mg/kg), corresponding to 1-, 5-, and 17-fold the rhesus NaV1.8 EC50 (8.9 nM), respectively.
Showed a significant main effect of treatment via repeated measures one-way ANOVA.
Demonstrated significant flare area reduction at 2.0 mg/kg relative to vehicle.
Chemical Information
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No. CAS 2417328-24-4
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Peso molecular 479.42
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Fòrmula C18H18F5N5O3S
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SMILES
C[C@H]1CN(CCC1(F)F)C2=NC=C(C=C2C(NC3=CC(S(N)(=O)=O)=NC=C3)=O)C(F)(F)F
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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-5661 Related Classifications
HY-183566 Related Classifications
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