TC-N 1752

Name: TC-N 1752
Brand: MedChemExpress
SKU: HY-107405
Rating: 4.5 (0 reviews)

Cat. No.: HY-107405 Pureté: 99.67%: Fiche technique
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TC-N 1752 is a potent and orally active inhibitor of Nav1.7, with IC₅₀s of 0.17 μM, 0.3 μM, 0.4 μM, 1.1 μM and 2.2 μM at hNav1.7, hNav1.3, hNav1.4, hNaV1.5 and rNav1.8, respectively. TC-N 1752 also inhibits tetrodotoxin-sensitive sodium channels. TC-N 1752 shows analgesic efficacy in the Formalin model of pain.

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TC-N 1752 Chemical Structure

CAS No. : 1211866-85-1

Size	Stock	Quantité

Échantillon gratuit (0.1 - 0.2 mg)	Appliquer maintenant
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
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500 mg	Obtenir un devis

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Other Forms of TC-N 1752:

TC-N 1752-d₅ Obtenir un devis
TC-N 1752 (Standard) Obtenir un devis

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

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Description

IC₅₀ & Target^[1]^[2]

hNa_v1.7

0.17 μM (IC₅₀)

hNa_v1.8

0.1 μM (IC₅₀)

hNa_v1.3

0.3 μM (IC₅₀)

hNa_v1.4

0.4 μM (IC₅₀)

hNa_v1.5

1.1 μM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	>10 μM Compound: 52	Inhibition of fully inactivated TTX-resistant human sodium channel Nav1.3 expressed in human HEK293 cells at 1 uM by patch-clamp electrophysiological assay Inhibition of fully inactivated TTX-resistant human sodium channel Nav1.3 expressed in human HEK293 cells at 1 uM by patch-clamp electrophysiological assay	[PMID: 21634377]
HEK293	IC₅₀	>10 μM Compound: 52	Inhibition of fully inactivated TTX-resistant human sodium channel Nav1.4 expressed in human HEK293 cells at 1 uM by patch-clamp electrophysiological assay Inhibition of fully inactivated TTX-resistant human sodium channel Nav1.4 expressed in human HEK293 cells at 1 uM by patch-clamp electrophysiological assay	[PMID: 21634377]
HEK293	IC₅₀	>10 μM Compound: 52	Inhibition of fully inactivated TTX-resistant human sodium channel Nav1.5 expressed in human HEK293 cells at 1 uM by patch-clamp electrophysiological assay Inhibition of fully inactivated TTX-resistant human sodium channel Nav1.5 expressed in human HEK293 cells at 1 uM by patch-clamp electrophysiological assay	[PMID: 21634377]
HEK293	IC₅₀	>10 μM Compound: 52	Inhibition of human Erg expressed in human HEK293 cells by patch-clamp electrophysiological assay Inhibition of human Erg expressed in human HEK293 cells by patch-clamp electrophysiological assay	[PMID: 21634377]
HEK293	IC₅₀	0.3 μM Compound: 52	Inhibition of 20% inactivated TTX-resistant human sodium channel Nav1.3 expressed in human HEK293 cells at 1 uM by patch-clamp electrophysiological assay Inhibition of 20% inactivated TTX-resistant human sodium channel Nav1.3 expressed in human HEK293 cells at 1 uM by patch-clamp electrophysiological assay	[PMID: 21634377]
HEK293	IC₅₀	0.4 μM Compound: 52	Inhibition of 20% inactivated TTX-resistant human sodium channel Nav1.4 expressed in human HEK293 cells at 1 uM by patch-clamp electrophysiological assay Inhibition of 20% inactivated TTX-resistant human sodium channel Nav1.4 expressed in human HEK293 cells at 1 uM by patch-clamp electrophysiological assay	[PMID: 21634377]
HEK293	IC₅₀	0.5 μM Compound: 52	Inhibition of human sodium channel Nav1.7 expressed in human HEK293 cells by patch-clamp electrophysiological assay Inhibition of human sodium channel Nav1.7 expressed in human HEK293 cells by patch-clamp electrophysiological assay	[PMID: 21634377]
HEK293	IC₅₀	1.1 μM Compound: 52	Inhibition of 20% inactivated TTX-resistant human sodium channel Nav1.5 expressed in human HEK293 cells at 1 uM by patch-clamp electrophysiological assay Inhibition of 20% inactivated TTX-resistant human sodium channel Nav1.5 expressed in human HEK293 cells at 1 uM by patch-clamp electrophysiological assay	[PMID: 21634377]
HEK293	IC₅₀	170 nM Compound: 52	Inhibition of 20% inactivated human sodium channel Nav1.7 expressed in human HEK293 cells by patch-clamp electrophysiological assay Inhibition of 20% inactivated human sodium channel Nav1.7 expressed in human HEK293 cells by patch-clamp electrophysiological assay	[PMID: 21634377]
HEK293	IC₅₀	2.2 μM Compound: 52	Inhibition of 20% inactivated TTX-resistant rat sodium channel Nav1.8 expressed in human HEK293 cells at 1 uM by patch-clamp electrophysiological assay Inhibition of 20% inactivated TTX-resistant rat sodium channel Nav1.8 expressed in human HEK293 cells at 1 uM by patch-clamp electrophysiological assay	[PMID: 21634377]
HEK293	IC₅₀	3.3 μM Compound: 52	Inhibition of 20% inactivated human sodium channel Nav1.7 expressed in human HEK293 cells by patch-clamp electrophysiological assay in presence of 5% human serum albumin Inhibition of 20% inactivated human sodium channel Nav1.7 expressed in human HEK293 cells by patch-clamp electrophysiological assay in presence of 5% human serum albumin	[PMID: 21634377]
HEK293	IC₅₀	3.6 μM Compound: 52	Inhibition of fully inactivated human sodium channel Nav1.7 expressed in human HEK293 cells by patch-clamp electrophysiological assay Inhibition of fully inactivated human sodium channel Nav1.7 expressed in human HEK293 cells by patch-clamp electrophysiological assay	[PMID: 21634377]
HEK293	IC₅₀	5.2 μM Compound: 52	Inhibition of human cardiac sodium channel Nav1.5 expressed in human HEK293 cells by patch-clamp electrophysiological assay Inhibition of human cardiac sodium channel Nav1.5 expressed in human HEK293 cells by patch-clamp electrophysiological assay	[PMID: 21634377]

In Vitro

TC-N 1752 (compound 52) state-dependently inhibits Nav1.7, with IC₅₀ of 170 nM on channels that are 20% inactivated and IC₅₀ of 3.6 μM on fully noninactivated channels^[1].
TC-N 1752 inhibits hNav1.7, hNav1.8, hNav1.9, rNav1.9, and mNav1.9 with IC₅₀s of 0.2, 0.1, 1.6, 0.5 and 1.4 μM, respectively^[2].

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

In Vivo

TC-N 1752 (compound 52) (3-30 mg/kg; p.o.) dose-dependently shows analgesic effect in the Formalin model^[1].
TC-N 1752 (3-30 mg/kg; p.o.) decreases thermal hyperalgesia produced by inflammation^[3].
TC-N 1752 (5 mg/mL; 500 μL; i.v.) attenuates complete Freund’s adjuvant (CFA)-induced sensitization of C-fiber nociceptors^[3].

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

Animal Model:	Rats were injected intraplantar with Formalin^[1]
Dosage:	3, 10, 20, 30 mg/kg
Administration:	Administered p.o. 120 min prior to Formalin
Result:	Showed analgesic efficacy starting at the dose of 3 mg/kg, with full efficacy at 20 mg/kg dose.

Masse moléculaire

516.52

Formule

C₂₅H₂₇F₃N₆O₃

CAS No.

1211866-85-1

Appearance

Solid

Color

White to off-white

SMILES

FC(F)(F)OC(C=C1)=CC=C1COC(CC2)CCN2C3=NC=NC(NC4=C(C(NC(C)=O)=CC=C4)C)=N3

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 : 125 mg/mL (242.00 mM; Need ultrasonic; 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	1.9360 mL	9.6802 mL	19.3603 mL
5 mM	0.3872 mL	1.9360 mL	3.8721 mL
10 mM	0.1936 mL	0.9680 mL	1.9360 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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Working solution concentration: mg/mL

Pureté et documentation

Purity: 99.67%

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Fiche technique (272 KB) SDS (251 KB)

COA (246 KB) HNMR (291 KB) LCMS (95 KB)

Instruction de manipulation (2659 KB)

Références

[1]. Bregman H, et, al. Identification of a potent, state-dependent inhibitor of Nav1.7 with oral efficacy in the formalin model of persistent pain. J Med Chem. 2011 Jul 14;54(13):4427-45. [Content Brief]

[2]. Lin Z, et, al. Biophysical and Pharmacological Characterization of Nav1.9 Voltage Dependent Sodium Channels Stably Expressed in HEK-293 Cells. PLoS One. 2016 Aug 24;11(8):e0161450. [Content Brief]

[3]. Matson DJ, et, al. Inhibition of Inactive States of Tetrodotoxin-Sensitive Sodium Channels Reduces Spontaneous Firing of C-Fiber Nociceptors and Produces Analgesia in Formalin and Complete Freund's Adjuvant Models of Pain. PLoS One. 2015 Sep 17;10(9):e013 [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.9360 mL	9.6802 mL	19.3603 mL	48.4008 mL
	5 mM	0.3872 mL	1.9360 mL	3.8721 mL	9.6802 mL
	10 mM	0.1936 mL	0.9680 mL	1.9360 mL	4.8401 mL
	15 mM	0.1291 mL	0.6453 mL	1.2907 mL	3.2267 mL
	20 mM	0.0968 mL	0.4840 mL	0.9680 mL	2.4200 mL
	25 mM	0.0774 mL	0.3872 mL	0.7744 mL	1.9360 mL
	30 mM	0.0645 mL	0.3227 mL	0.6453 mL	1.6134 mL
	40 mM	0.0484 mL	0.2420 mL	0.4840 mL	1.2100 mL
	50 mM	0.0387 mL	0.1936 mL	0.3872 mL	0.9680 mL
	60 mM	0.0323 mL	0.1613 mL	0.3227 mL	0.8067 mL
	80 mM	0.0242 mL	0.1210 mL	0.2420 mL	0.6050 mL
	100 mM	0.0194 mL	0.0968 mL	0.1936 mL	0.4840 mL

TC-N 1752 Related Classifications

Neurological Disease

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:

TC-N 17521211866-85-1Sodium ChannelNa channelsNa+ channelsFormalinpainanalgesicInhibitorinhibitorinhibit

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TC-N 1752

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Other Forms of TC-N 1752:

TC-N 1752 Related Antibodies

Recommandations en vedette

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Voir tous les produits spécifiques à Isoform Sodium Channel:

Activité biologique

Pureté et documentation

Références

Avis client

TC-N 1752 Related Antibodies

Calculateur de molarité

Calculateur de dilution

Complete Stock Solution Preparation Table

TC-N 1752 Related Classifications

Keywords:

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