TC-N 1752

Modify Date: 2024-01-22 05:26:27

TC-N 1752 Structure
TC-N 1752 structure
 Common Name TC-N 1752
CAS Number 1211866-85-1 Molecular Weight 516.52
Density 1.37±0.1 g/cm3(Predicted) Boiling Point N/A
Molecular Formula C25H27F3N6O3 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of 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[1][2][3].

 Names

Name N-(2-Methyl-3-{[4-(4-{[4-(trifluoromethoxy)benzyl]oxy}-1-piperidi nyl)-1,3,5-triazin-2-yl]amino}phenyl)acetamide
Synonym More Synonyms

 TC-N 1752 Biological Activity

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].
Related Catalog
Target

hNav1.7:0.17 μM (IC50)

hNav1.3:0.3 μM (IC50)

hNav1.4:0.4 μM (IC50)

hNav1.5:1.1 μM (IC50)

hNav1.8:0.1 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].
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]. 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.
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.

[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.

[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):e0138140.

 Chemical & Physical Properties

Density 1.37±0.1 g/cm3(Predicted)
Molecular Formula C25H27F3N6O3
Molecular Weight 516.52
Exact Mass 516.21000
PSA 108.22000
LogP 5.10260
Storage condition 2-8°C

 Synthetic Route

N-(3-(4-chloro-1,3,5-triazin-2-ylamino)-2-methylphenyl)acetamide structure

N-(3-(4-chloro-...

CAS#:1211876-60-6

4-(4-(trifluoromethoxy)benzyloxy)piperidine trifluoroacetate salt structure

4-(4-(trifluoro...

CAS#:1211875-20-5

~77%

TC-N 1752 Structure

TC-N 1752

CAS#:1211866-85-1

Literature: Bregman, Howard; Berry, Loren; Buchanan, John L.; Chen, April; Du, Bingfan; Feric, Elma; Hierl, Markus; Huang, Liyue; Immke, David; Janosky, Brett; Johnson, Danielle; Li, Xingwen; Ligutti, Joseph; Liu, Dong; Malmberg, Annika; Matson, David; McDermott, Jeff; Miu, Peter; Nguyen, Hanh Nho; Patel, Vinod F.; Waldon, Daniel; Wilenkin, Ben; Zheng, Xiao Mei; Zou, Anruo; McDonough, Stefan I.; Dimauro, Erin F. Journal of Medicinal Chemistry, 2011 , vol. 54, # 13 p. 4427 - 4445
4-[(4-trifluoromethoxy)phenyl]methoxypiperidine-1-formic acid tert-butyl ester structure

4-[(4-trifluoro...

CAS#:287952-21-0

~%

TC-N 1752 Structure

TC-N 1752

CAS#:1211866-85-1

Literature: Bregman, Howard; Berry, Loren; Buchanan, John L.; Chen, April; Du, Bingfan; Feric, Elma; Hierl, Markus; Huang, Liyue; Immke, David; Janosky, Brett; Johnson, Danielle; Li, Xingwen; Ligutti, Joseph; Liu, Dong; Malmberg, Annika; Matson, David; McDermott, Jeff; Miu, Peter; Nguyen, Hanh Nho; Patel, Vinod F.; Waldon, Daniel; Wilenkin, Ben; Zheng, Xiao Mei; Zou, Anruo; McDonough, Stefan I.; Dimauro, Erin F. Journal of Medicinal Chemistry, 2011 , vol. 54, # 13 p. 4427 - 4445
4-(Trifluoromethoxy)benzyl bromide structure

4-(Trifluoromet...

CAS#:50824-05-0

~%

TC-N 1752 Structure

TC-N 1752

CAS#:1211866-85-1

Literature: Bregman, Howard; Berry, Loren; Buchanan, John L.; Chen, April; Du, Bingfan; Feric, Elma; Hierl, Markus; Huang, Liyue; Immke, David; Janosky, Brett; Johnson, Danielle; Li, Xingwen; Ligutti, Joseph; Liu, Dong; Malmberg, Annika; Matson, David; McDermott, Jeff; Miu, Peter; Nguyen, Hanh Nho; Patel, Vinod F.; Waldon, Daniel; Wilenkin, Ben; Zheng, Xiao Mei; Zou, Anruo; McDonough, Stefan I.; Dimauro, Erin F. Journal of Medicinal Chemistry, 2011 , vol. 54, # 13 p. 4427 - 4445
N-(3-amino-2-methylphenyl)acetamide structure

N-(3-amino-2-me...

CAS#:65999-76-0

~%

TC-N 1752 Structure

TC-N 1752

CAS#:1211866-85-1

Literature: Bregman, Howard; Berry, Loren; Buchanan, John L.; Chen, April; Du, Bingfan; Feric, Elma; Hierl, Markus; Huang, Liyue; Immke, David; Janosky, Brett; Johnson, Danielle; Li, Xingwen; Ligutti, Joseph; Liu, Dong; Malmberg, Annika; Matson, David; McDermott, Jeff; Miu, Peter; Nguyen, Hanh Nho; Patel, Vinod F.; Waldon, Daniel; Wilenkin, Ben; Zheng, Xiao Mei; Zou, Anruo; McDonough, Stefan I.; Dimauro, Erin F. Journal of Medicinal Chemistry, 2011 , vol. 54, # 13 p. 4427 - 4445
N-BOC-4-Hydroxypiperidine structure

N-BOC-4-Hydroxy...

CAS#:109384-19-2

~%

TC-N 1752 Structure

TC-N 1752

CAS#:1211866-85-1

Literature: Bregman, Howard; Berry, Loren; Buchanan, John L.; Chen, April; Du, Bingfan; Feric, Elma; Hierl, Markus; Huang, Liyue; Immke, David; Janosky, Brett; Johnson, Danielle; Li, Xingwen; Ligutti, Joseph; Liu, Dong; Malmberg, Annika; Matson, David; McDermott, Jeff; Miu, Peter; Nguyen, Hanh Nho; Patel, Vinod F.; Waldon, Daniel; Wilenkin, Ben; Zheng, Xiao Mei; Zou, Anruo; McDonough, Stefan I.; Dimauro, Erin F. Journal of Medicinal Chemistry, 2011 , vol. 54, # 13 p. 4427 - 4445

 Synonyms

Cyclohexanamine,N-(2-methyl-2-propenylidene)-,(E)
N-(2-methyl-3-(4-(4-(4-(trifluoromethoxy)benzyloxy)piperidin-1-yl)-1,3,5-triazin-2-ylamino)phenyl)acetamide
N-(2-methyl-2-propen-1-ylidene)cyclohexylamine
Cyclohexanamine,N-(2-methyl-2-propenylidene)
Top Suppliers:I want be here

Get all suppliers and price by the below link:

TC-N 1752 suppliers

TC-N 1752 price

Related Compounds: More...
TC-N 22A
1314140-00-5
Sodium 2-[methyl(1-oxododecyl)amino]ethanesulphonate
4337-75-1
tc-5619
639494-67-0
TC ASK 10
1005775-56-3
TC-I 2000
1159996-20-9
TC-G 24
1257256-44-2
TC-S 7009
1422955-31-4
TC-E 5003
17328-16-4
TC NTR1 17
1146757-96-1
Chemsrc provides TC-N 1752(CAS#:1211866-85-1) MSDS, density, melting point, boiling point, structure, formula, molecular weight etc. Articles of TC-N 1752 are included as well.>> amp version: TC-N 1752

Home | MSDS/SDS Database Search | Journals | Product Classification | Biologically Active Compounds | Selling Leads | About Us | Disclaimer

Copyright © 2024 ChemSrc All Rights Reserved