2. Membrane Transporter/Ion Channel
  3. Sodium Channel
  4. 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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MK-5661

MK-5661 Chemical Structure

CAS No. : 2417328-24-4

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Description

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[1].

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.

MK-5661 Related Antibodies
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 (0.1-10 mg/kg; p.o.; single dose) dose-dependently inhibits capsaicin-induced nocifensive behavior in humanized rats[1].
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.

Animal Model: Humanized rats[1]
Dosage: 0.1 mg/kg, 0.3 mg/kg, 1.0 mg/kg, 3.0 mg/kg, 10.0 mg/kg
Administration: p.o.; single dose
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.
Animal Model: Rhesus macaques[1]
Dosage: 0.2 mg/kg, 0.6 mg/kg, 2.0 mg/kg
Administration: p.o.; single dose
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.
Molecular Weight

479.42

Formula

C18H18F5N5O3S
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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MK-5661 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MK-56612417328-24-4MK5661MK 5661Sodium ChannelNa channelsNa+ channelsrhesus monkeyscapsaicin-induced spontaneous nocifensive behaviorNaV1.7painNaV1.8 voltage-gated sodium channelhumanized ratsperipheral nociceptive signaling mediatorsHEK 293 cellsNaV1.2capsaicin-induced dermal flare responsesInhibitorinhibitorinhibit

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