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Cat. No.: HY-101789

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Nav1.7-IN-3

Name: Nav1.7-IN-3
Brand: MedChemExpress
SKU: HY-101789
Price: 400.00 USD
Availability: InStock
Rating: 5 (1 reviews)

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Nav1.7-IN-3 is a selective, orally bioavailable voltage-gated sodium channel Nav1.7 inhibitor with an IC₅₀ of 8 nM. Pain relief. Limited CNS penetration.

Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.

Pureté: 98.21%
CAS No.: 1788872-06-9
Formule: C₁₇H₂₀ClFN₄O₂S₂
Masse moléculaire:430.95

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Nav1.7-IN-3 Chemical Structure

CAS No.: 1788872-06-9

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vivo
Chemical Information
Solvant et solubilité
- In Vitro
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
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Activité biologique

Description

Nav1.7-IN-3 is a selective, orally bioavailable voltage-gated sodium channel Nav1.7 inhibitor with an IC₅₀ of 8 nM. Pain relief. Limited CNS penetration^[1].

IC₅₀ & Target^[1]

Na_v1.7

8 nM (IC₅₀)

Voir tous les produits spécifiques à Isoform Sodium Channel :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	8 nM Compound: 5	Inhibition of 50% inactivated human Nav1.7alpha expressed in HEK293 cells at holding potential of -60 mV incubated for 5 mins measured at 10 secs interval by PatchXpress electrophysiology assay Inhibition of 50% inactivated human Nav1.7alpha expressed in HEK293 cells at holding potential of -60 mV incubated for 5 mins measured at 10 secs interval by PatchXpress electrophysiology assay	[PMID: 28389149]
HEK293	IC₅₀	>30000 nM Compound: 5	Inhibition of 50% inactivated human Nav1.5alpha expressed in HEK293 cells at holding potential of -60 mV incubated for 5 mins measured at 10 secs interval by PatchXpress electrophysiology assay Inhibition of 50% inactivated human Nav1.5alpha expressed in HEK293 cells at holding potential of -60 mV incubated for 5 mins measured at 10 secs interval by PatchXpress electrophysiology assay	[PMID: 28389149]
HEK293	IC₅₀	2.2 nM Compound: 3	Inhibition of human Nav1.5 inactivated state form expressed in HEK293 cells at -60 mV holding potential by by automated patch clamp electrophysiology assay Inhibition of human Nav1.5 inactivated state form expressed in HEK293 cells at -60 mV holding potential by by automated patch clamp electrophysiology assay	[PMID: 28818462]
HEK293	IC₅₀	>30000 nM Compound: 3	Inhibition of human Nav1.5 inactivated state form expressed in HEK293 cells at -50 mV holding potential by by automated patch clamp electrophysiology assay Inhibition of human Nav1.5 inactivated state form expressed in HEK293 cells at -50 mV holding potential by by automated patch clamp electrophysiology assay	[PMID: 28818462]
HEK293	IC₅₀	3.9 nM Compound: 2	Inhibition of recombinant mouse Nav1.7 expressed in HEK293 cells at -70 mV holding potential by patch clamp electrophysiology method Inhibition of recombinant mouse Nav1.7 expressed in HEK293 cells at -70 mV holding potential by patch clamp electrophysiology method	[PMID: 30576602]

In Vivo

Nav1.7-IN-3 (compound 5) shows excellent potency, selectivity, behavioral efficacy in a rodent pain model (30 mg/kg, oral, 35 minutes), and efficacy in a mouse itch model (30 mg/kg, oral, 30 minutes)^[1].

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

Animal Model:

C57BL/6 male mice (n=8/group, 25-30g)
Dosage:

1, 3, and 10 mg/kg
Administration:

Oral (0-35 mintues)
Result:

Nav1.7-IN-3 demonstrates statistically significant, dose-dependent reversal of these effects in the acute phase of the experiment (0-5 min period post formalin injection) and the tonic phase of the experiment (20-35 min period post formalin injection) with full reversal of formalin effects in the tonic phase^[1]

Chemical Information

CAS No. 1788872-06-9
Appearance Solid
Masse moléculaire 430.95
Formule C₁₇H₂₀ClFN₄O₂S₂
Color White to off-white
SMILES

FC1=C(S(=O)(NC2=NC=CS2)=O)C=C(Cl)C(NCC34CCCN3CCC4)=C1
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvant et solubilité

In Vitro:

DMSO : < 1 mg/mL (insoluble or slightly soluble)

View the Complete Stock Solution Preparation Table

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (274 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Roecker AJ, et al. Discovery of selective, orally bioavailable, N-linked arylsulfonamide Nav1.7 inhibitors with pain efficacy in mice. Bioorg Med Chem Lett. 2017 May 15;27(10):2087-2093. [Content Brief]

Calculators

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

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Volume Volume

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Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

Minimum order quantity

100 mg

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Activité biologique
- Description
- IC₅₀ & Target
- In Vivo
Chemical Information
Solvant et solubilité
- In Vitro
Pureté et documentation
Références

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CAS No.:
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Nav1.7-IN-3

GDC-0310

PF-06456384 trihydrochloride

NaV1.7 inhibitor-1

GX-201

Voir tous les produits spécifiques à Isoform Sodium Channel

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Calculators

Help & FAQs

Bioz

Nav1.7-IN-3

GDC-0310

PF-06456384 trihydrochloride

NaV1.7 inhibitor-1

GX-201

Voir tous les produits spécifiques à Isoform Sodium Channel

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Calculators

Help & FAQs

Nav1.7-IN-3 Related Classifications

HY-101789 Related Classifications

Bioz