2. Membrane Transporter/Ion Channel
  3. Sodium Channel
  4. TC-N 1752

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

TC-N 1752 Chemical Structure

CAS No. : 1211866-85-1

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Based on 1 publication(s) in Google Scholar

Other Forms of TC-N 1752:

TC-N 1752 Related Antibodies

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  • Purity & Documentation

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Description

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[1][2][3].

IC50 & Target[1][2]

hNav1.7

0.17 μM (IC50)

hNav1.8

0.1 μM (IC50)

hNav1.3

0.3 μM (IC50)

hNav1.4

0.4 μM (IC50)

hNav1.5

1.1 μM (IC50)

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.

TC-N 1752 Related Antibodies
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.
Molecular Weight

516.52

Formula

C25H27F3N6O3
CAS No.
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
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)

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
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)

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

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.

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
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TC-N 1752 Related Classifications

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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