Cat. No.: HY-107405

TC-N 1752

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Based on 1 Customer Validation

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.

For research use only. We do not sell to patients.

Purity: 99.67%
CAS No.: 1211866-85-1
Formula: C₂₅H₂₇F₃N₆O₃
Molecular Weight:516.52

Storage:

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

TC-N 1752 Chemical Structure

CAS No.: 1211866-85-1

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Use of MCE Products

Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

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)

All Sodium Channel Isoforms :

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.

Chemical Information

CAS No. 1211866-85-1
Appearance Solid
Molecular Weight 516.52
Formula C₂₅H₂₇F₃N₆O₃
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
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Molarity Calculator

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

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Dilution Calculator

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 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)
Handling Instructions (2659 KB)

References

[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]

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.

Complete Stock Solution Preparation Table

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.

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

Keywords

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TC-N 1752

Membrane Transporter/Ion Channel Compound Library

Neuroprotective Compound Library

Sodium Channel Blocker Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Ion Channel Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

All Sodium Channel Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

TC-N 1752

Membrane Transporter/Ion Channel Compound Library

Neuroprotective Compound Library

Sodium Channel Blocker Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Ion Channel Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

All Sodium Channel Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

TC-N 1752 Related Classifications

HY-107405 Related Classifications