2. Membrane Transporter/Ion Channel Metabolic Enzyme/Protease
  3. Sodium Channel Cytochrome P450
  4. Nav1.7-IN-8

Nav1.7-IN-8 is a potent blockage of NaV1.7 with high selectivity for the inhibition of NaV1.7 over the subtypes hNaV1.1 and hNaV1.5. Nav1.7-IN-8 inhibits CYP2C9 and CYP3A4 with an IC50 of 0.17 μM and 0.077 μM, respectively. Nav1.7-IN-8 displays significant analgesic effects in rodent models of acute and inflammatory pain.

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Nav1.7-IN-8 Chemical Structure

Nav1.7-IN-8 Chemical Structure

CAS No. : 1432913-44-4

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Nav1.7-IN-8 Related Antibodies

Top Publications Citing Use of Products

View All Sodium Channel Isoform Specific Products:

View All Isoforms
Nav1.1 Nav1.2 Nav1.3 Nav1.4 Nav1.5 Nav1.6 Nav1.7 Nav1.8

View All Cytochrome P450 Isoform Specific Products:

View All Isoforms
CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Nav1.7-IN-8 is a potent blockage of NaV1.7 with high selectivity for the inhibition of NaV1.7 over the subtypes hNaV1.1 and hNaV1.5. Nav1.7-IN-8 inhibits CYP2C9 and CYP3A4 with an IC50 of 0.17 μM and 0.077 μM, respectively. Nav1.7-IN-8 displays significant analgesic effects in rodent models of acute and inflammatory pain[1].

IC50 & Target[1]

CYP2C9

0.17 μM (IC50)

Nav1.7

 

CYP3A4

0.077 μM (IC50)

Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
0.4 nM
Compound: 3
Inhibition of full length human Nav1.7 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -60 mV by automated voltage clamp analysis
Inhibition of full length human Nav1.7 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -60 mV by automated voltage clamp analysis
[PMID: 26985315]
HEK293 IC50
0.4 nM
Compound: 3
Inhibition of full length human Nav1.7 channel expressed in HEK cells co-expressing human sodium channel subunit beta3 at -150 mV by manual voltage clamp analysis
Inhibition of full length human Nav1.7 channel expressed in HEK cells co-expressing human sodium channel subunit beta3 at -150 mV by manual voltage clamp analysis
[PMID: 26985315]
HEK293 IC50
11 nM
Compound: 3
Inhibition of full length human Nav1.6 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -35 mV by automated voltage clamp analysis
Inhibition of full length human Nav1.6 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -35 mV by automated voltage clamp analysis
[PMID: 26985315]
HEK293 IC50
1380 nM
Compound: 3
Inhibition of full length human Nav1.5 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -60 mV by automated voltage clamp analysis
Inhibition of full length human Nav1.5 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -60 mV by automated voltage clamp analysis
[PMID: 26985315]
HEK293 IC50
3080 nM
Compound: 3
Inhibition of full length human Nav1.1 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -40 mV by automated voltage clamp analysis
Inhibition of full length human Nav1.1 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -40 mV by automated voltage clamp analysis
[PMID: 26985315]
HEK293 IC50
4.2 nM
Compound: 3
Inhibition of full length human Nav1.2 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -35 mV by automated voltage clamp analysis
Inhibition of full length human Nav1.2 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -35 mV by automated voltage clamp analysis
[PMID: 26985315]
In Vitro

Nav1.7-IN-8 plasma protein binding is very high in rat with a free fraction of ∼1.1 %[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Nav1.7-IN-8 Related Antibodies
In Vivo

Nav1.7-IN-8 (0~100 mpk, i.p.; 1 hour) shows a reduction of the pain response in phase 2a of the formalin assay in a dose dependent manner and produces a substantial inhibition of the pain response[1].
. Nav1.7-IN-8 (10~100 mpk, i.p.; 2 days) displays a dose-dependent reduction of the pain response[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Rats[1]
Dosage: 0~100 mpk
Administration: I.p.; 1 hour
Result: Showed a reduction of the pain response in phase 2a of the formalin assay in a dose dependent manner and produced a substantial inhibition of the pain response.
Animal Model: Mice[1]
Dosage: 10~100 mpk
Administration: I.p.; 2 days
Result: Displayed a dose-dependent reduction of the pain response.
Molecular Weight

535.93

Formula

C21H12ClF2N5O4S2
CAS No.
SMILES

O=S(NC1=NC=NS1)(C2=C(F)C=C(OC3=C(C4=CC=C5ON=C(C5=C4)N)C=C(Cl)C=C3)C(F)=C2)=O
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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Nav1.7-IN-8 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:

Nav1.7-IN-81432913-44-4Sodium ChannelCytochrome P450Na channelsNa+ channelsCYPspotentselectivityhNaV1.1hNaV1.5analgesicacuteinflammatorypainInhibitorinhibitorinhibit

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