NaV1.2/1.6 channel blocker-1

Name: NaV1.2/1.6 channel blocker-1
Brand: MedChemExpress
SKU: HY-152166
Rating: 4.5 (0 reviews)

Cat. No.: HY-152166: Fiche technique
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NaV1.2/1.6 channel blocker-1 is a potent NaV1.2/1.6 channel blocker, with IC₅₀s of 9.8 and 24.4 μM for rNaV1.6 and hNaV1.2, respectively. NaV1.2/1.6 channel blocker-1 can be used for the research of generalized epilepsy.

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NaV1.2/1.6 channel blocker-1 Chemical Structure

CAS No. : 1199944-04-1

Size	Stock	Quantité
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	En stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	En stock	Estimated Time of Arrival: December 31
Solid
5 mg	En stock	Estimated Time of Arrival: December 31
10 mg	En stock	Estimated Time of Arrival: December 31
25 mg	En stock	Estimated Time of Arrival: December 31
50 mg	En stock	Estimated Time of Arrival: December 31
100 mg	En stock	Estimated Time of Arrival: December 31
200 mg	Obtenir un devis
500 mg	Obtenir un devis

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Recommandations en vedette

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Voir tous les produits spécifiques à Isoform Sodium Channel:

Voir toutes les isoformes

Na_v1.1 Na_v1.2 Na_v1.3 Na_v1.4 Na_v1.5 Na_v1.6 Na_v1.7 Na_v1.8 Na_v1.9

Activité biologique
Pureté et documentation
Références
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Description

IC₅₀ & Target^[1]

rNaV1.6

9.8 μM (IC₅₀)

hNaV1.2

24.4 μM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	26.19 3 Compound: MV1035	Antiinvasive activity against human A549 cells assessed as reduction in cell invasion measured after 24 hrs using Diff-quick staining by light microscopy based Boyden chamber assay Antiinvasive activity against human A549 cells assessed as reduction in cell invasion measured after 24 hrs using Diff-quick staining by light microscopy based Boyden chamber assay	[PMID: 31937477]
A549	IC₅₀	26.19 3 Compound: MV1035	Antiinvasive activity against human A549 cells assessed as reduction in cell invasion measured after 24 hrs using Diff-quick staining by light microscopy based Boyden chamber assay Antiinvasive activity against human A549 cells assessed as reduction in cell invasion measured after 24 hrs using Diff-quick staining by light microscopy based Boyden chamber assay	[PMID: 31937477]
A549	IC₅₀	26.19 3 Compound: MV1035	Antiinvasive activity against human A549 cells assessed as reduction in cell invasion measured after 24 hrs using Diff-quick staining by light microscopy based Boyden chamber assay Antiinvasive activity against human A549 cells assessed as reduction in cell invasion measured after 24 hrs using Diff-quick staining by light microscopy based Boyden chamber assay	[PMID: 31937477]
NCI-H460	IC₅₀	10.12 3 Compound: MV1035	Antimigratory activity against human H460 cells assessed as inhibition of cell migration measured after 24 hrs by scratch wound healing assay Antimigratory activity against human H460 cells assessed as inhibition of cell migration measured after 24 hrs by scratch wound healing assay	[PMID: 31937477]
NCI-H460	IC₅₀	10.12 3 Compound: MV1035	Antimigratory activity against human H460 cells assessed as inhibition of cell migration measured after 24 hrs by scratch wound healing assay Antimigratory activity against human H460 cells assessed as inhibition of cell migration measured after 24 hrs by scratch wound healing assay	[PMID: 31937477]
NCI-H460	IC₅₀	17.78 3 Compound: MV1035	Antiinvasive activity against human H460 cells assessed as reduction in cell invasion measured after 24 hrs using Diff-quick staining by light microscopy based Boyden chamber assay Antiinvasive activity against human H460 cells assessed as reduction in cell invasion measured after 24 hrs using Diff-quick staining by light microscopy based Boyden chamber assay	[PMID: 31937477]
NCI-H460	IC₅₀	17.78 3 Compound: MV1035	Antiinvasive activity against human H460 cells assessed as reduction in cell invasion measured after 24 hrs using Diff-quick staining by light microscopy based Boyden chamber assay Antiinvasive activity against human H460 cells assessed as reduction in cell invasion measured after 24 hrs using Diff-quick staining by light microscopy based Boyden chamber assay	[PMID: 31937477]
NCI-H460	IC₅₀	10.12 3 Compound: MV1035	Antimigratory activity against human H460 cells assessed as inhibition of cell migration measured after 24 hrs by scratch wound healing assay Antimigratory activity against human H460 cells assessed as inhibition of cell migration measured after 24 hrs by scratch wound healing assay	[PMID: 31937477]
NCI-H460	IC₅₀	17.78 3 Compound: MV1035	Antiinvasive activity against human H460 cells assessed as reduction in cell invasion measured after 24 hrs using Diff-quick staining by light microscopy based Boyden chamber assay Antiinvasive activity against human H460 cells assessed as reduction in cell invasion measured after 24 hrs using Diff-quick staining by light microscopy based Boyden chamber assay	[PMID: 31937477]
U-87MG ATCC	IC₅₀	11.02 3 Compound: MV1035	Antimigratory activity against human U87MG cells assessed as inhibition of cell migration measured after 6 hrs by scratch wound healing assay Antimigratory activity against human U87MG cells assessed as inhibition of cell migration measured after 6 hrs by scratch wound healing assay	[PMID: 31937477]
U-87MG ATCC	IC₅₀	2.48 3 Compound: MV1035	Antiinvasive activity against human U87MG cells assessed as reduction in cell invasion measured after 24 hrs using Diff-quick staining by light microscopy based Boyden chamber assay Antiinvasive activity against human U87MG cells assessed as reduction in cell invasion measured after 24 hrs using Diff-quick staining by light microscopy based Boyden chamber assay	[PMID: 31937477]
U-87MG ATCC	IC₅₀	11.02 3 Compound: MV1035	Antimigratory activity against human U87MG cells assessed as inhibition of cell migration measured after 6 hrs by scratch wound healing assay Antimigratory activity against human U87MG cells assessed as inhibition of cell migration measured after 6 hrs by scratch wound healing assay	[PMID: 31937477]
U-87MG ATCC	IC₅₀	2.48 3 Compound: MV1035	Antiinvasive activity against human U87MG cells assessed as reduction in cell invasion measured after 24 hrs using Diff-quick staining by light microscopy based Boyden chamber assay Antiinvasive activity against human U87MG cells assessed as reduction in cell invasion measured after 24 hrs using Diff-quick staining by light microscopy based Boyden chamber assay	[PMID: 31937477]
U-87MG ATCC	IC₅₀	11.02 3 Compound: MV1035	Antimigratory activity against human U87MG cells assessed as inhibition of cell migration measured after 6 hrs by scratch wound healing assay Antimigratory activity against human U87MG cells assessed as inhibition of cell migration measured after 6 hrs by scratch wound healing assay	[PMID: 31937477]
U-87MG ATCC	IC₅₀	2.48 3 Compound: MV1035	Antiinvasive activity against human U87MG cells assessed as reduction in cell invasion measured after 24 hrs using Diff-quick staining by light microscopy based Boyden chamber assay Antiinvasive activity against human U87MG cells assessed as reduction in cell invasion measured after 24 hrs using Diff-quick staining by light microscopy based Boyden chamber assay	[PMID: 31937477]

In Vitro

NaV1.2/1.6 channel blocker-1 (compound 13) (1-100 μM) blocks the NaV1.6 and NaV1.2 sodium currents by 48.5% and 34.0% in HEK 293 stably expressing human NaV1.2 and rat NaV1.6 isoforms, respectively^[1].

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

Masse moléculaire

258.34

Formule

C₁₄H₁₄N₂OS

CAS No.

1199944-04-1

Appearance

Solid

Color

White to off-white

SMILES

S=C1OC2=CC=CC=C2C3=NC(C)=C(CCC)N13

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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

Solvant et solubilité

In Vitro:

DMSO : 12.5 mg/mL (48.39 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.8709 mL	19.3543 mL	38.7087 mL
5 mM	0.7742 mL	3.8709 mL	7.7417 mL
10 mM	0.3871 mL	1.9354 mL	3.8709 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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Volume _(start)

Concentration _(final)

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In Vivo Dissolution Calculator

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Working solution concentration: mg/mL

Pureté et documentation

Fiche technique (276 KB) SDS (252 KB) Instruction de manipulation (2659 KB)

Références

[1]. Rivara M, et, al. Biological Evaluation of Imidazobenzoxazines, Imidazobenzoxazin-5-ones and Imidazobenzoxazin-5-thiones as Sodium Channel Blockers. Letters in Drug Design & Discovery, 2014, 11, 90-97.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.8709 mL	19.3543 mL	38.7087 mL	96.7717 mL
	5 mM	0.7742 mL	3.8709 mL	7.7417 mL	19.3543 mL
	10 mM	0.3871 mL	1.9354 mL	3.8709 mL	9.6772 mL
	15 mM	0.2581 mL	1.2903 mL	2.5806 mL	6.4514 mL
	20 mM	0.1935 mL	0.9677 mL	1.9354 mL	4.8386 mL
	25 mM	0.1548 mL	0.7742 mL	1.5483 mL	3.8709 mL
	30 mM	0.1290 mL	0.6451 mL	1.2903 mL	3.2257 mL
	40 mM	0.0968 mL	0.4839 mL	0.9677 mL	2.4193 mL