1235406-89-9

Basic information

• Product Name: N-(2,4-diMethoxybenzyl)-2,4,5-trifluoro-N-(1,2,4-thiadiazol-5-yl)benzenesulfonaMide
• Synonyms: N-(2,4-diMethoxybenzyl)-2,4,5-trifluoro-N-(1,2,4-thiadiazol-5-yl)benzenesulfonaMide
• CAS NO: 1235406-89-9
• Molecular Formula: C₁₇H₁₄F₃N₃O₄S₂
• Molecular Weight: 445.4359696
• Mol File: 1235406-89-9.mol
• Article Data: 6

Chemical Properties

• Appearance: /
• Storage Temp.: Sealed in dry,Room Temperature
• CAS DataBase Reference: N-(2,4-diMethoxybenzyl)-2,4,5-trifluoro-N-(1,2,4-thiadiazol-5-yl)benzenesulfonaMide(CAS DataBase Reference)
• NIST Chemistry Reference: N-(2,4-diMethoxybenzyl)-2,4,5-trifluoro-N-(1,2,4-thiadiazol-5-yl)benzenesulfonaMide(1235406-89-9)
• EPA Substance Registry System: N-(2,4-diMethoxybenzyl)-2,4,5-trifluoro-N-(1,2,4-thiadiazol-5-yl)benzenesulfonaMide(1235406-89-9)

Safety Data

• Hazardous Substances Data: 1235406-89-9(Hazardous Substances Data)

Upstream product

• 220227-21-4 2,4,5-trifluorobenzene-1-sulfonyl chloride 
• 1063733-41-4 N-[(2,4-dimethoxyphenyl)methyl]-1,2,4-thiadiazol-5-amine 
• 613-45-6 2,4-Dimethoxybenzaldehyde 

Downstream Products

• 1432912-69-0 4-(4-chloro-2-(7-(4-methoxybenzyl)-8-oxo-7,8-dihydroimidazo[1,5-a]pyrazin-5-yl)phenoxy)-N-(2,4-dimethoxybenzyl)-2,5-difluoro-N-(1,2,4-thiadiazol-5-yl)benzenesulfonamide 
• 1432913-99-9 4-(2-(1H-benzo[d]imidazol-5-yl)-4-chlorophenoxy)-N-(2,4-dimethoxybenzyl)-2,5-difluoro-N-(1,2,4-thiadiazol-5-yl)benzenesulfonamide 
• 1432914-05-0 4-(4-chloro-2-(2-oxoindolin-5-yl)phenoxy)-N-(2,4-dimethoxybenzyl)-2,5-difluoro-N-(1,2,4-thiadiazol-5-yl)benzenesulfonamide 
• 1432913-35-3 4-(4-chloro-2-(pyrazolo[1,5-a]pyrimidin-3-yl)phenoxy)-2,5-difluoro-N-(1,2,4-thiadiazol-5-yl)benzenesulfonamide 
• 1432913-72-8 4-(3-(3-aminobenzo[d]isoxazol-5-yl)-2-oxopyridin-1(2H)-yl)-N-(2,4-dimethoxybenzyl)-2,5-difluoro-N-(1,2,4-thiadiazol-5-yl)benzenesulfonamide 
• 1432913-73-9 4-((3-(3-aminobenzo[d]isoxazol-5-yl)pyridin-2-yl)oxy)-N-(2,4-dimethoxybenzyl)-2,5-difluoro-N-(1,2,4-thiadiazol-5-yl)benzenesulfonamide 
• 1432913-43-3 4-(2-(6-amino-9H-purin-9-yl)-4-chlorophenoxy)-2,5-difluoro-N-(1,2,4-thiadiazol-5-yl)benzenesulfonamide 
• 1432912-84-9 di-tert-butyl (5-{4-[(2,4-dimethoxybenzyl)(1,2,4-thiadiazol-5-yl)sulfamoyl]-2,5-difluorophenoxy}-1,2-benzoxazol-3-yl)imidodicarbonate 
• 1432912-68-9 4-(2-(6-aminopyridin-2-yl)-4-chlorophenoxy)-N-(2,4-dimethoxybenzyl)-2,5-difluoro-N-(1,2,4-thiadiazol-5-yl)benzenesulfonamide 
• 1432912-87-2 4-(4-chloro-2-(imidazo[1,2-a]pyrimidin-5-yl)phenoxy)-N-(2,4-dimethoxybenzyl)-2,5-difluoro-N-(1,2,4-thiadiazol-5-yl)benzenesulfonamide 
• 1432913-93-3 tert-butyl (5-(5-chloro-2-(4-(N-(2,4-dimethoxybenzyl)-N-(1,2,4-thiadiazol-5-yl)sulfamoyl)-2,5-difluorophenoxy)phenyl)benzo[d]isoxazol-3-yl)carbamate 
• 1432912-73-6 tert-butyl 3-[bis(tert-butoxycarbonyl)amino]-5-(5-chloro-2-{4-[(2,4-dimethoxybenzyl)-(1,2,4-thiadiazol-5-yl)sulfamoyl]-2,5-difluorophenoxy}phenyl)-1H-indazole-1-carboxylate 
• 1432912-70-3 4-(4-chloro-2-(imidazo[1,5-a]pyrazin-3-yl)phenoxy)-N-(2,4-dimethoxybenzyl)-2,5-difluoro-N-(1,2,4-thiadiazol-5-yl)benzenesulfonamide 
• 1432913-34-2 4-(4-chloro-2-(imidazo[1,5-a]pyrazin-3-yl)phenoxy)-2,5-difluoro-N-(1,2,4-thiadiazol-5-yl)benzenesulfonamide 

Relevant articles and documents

Sulfonamide compound used as sodium channel blocker, and application thereof

The invention provides a sulfonamide compound used as a sodium channel blocker, and an application thereof. The sulfonamide compound has dual inhibitory activity on Nav1.7 and Nav1.3 at the same time,and can be used as a medicine for widely treating pains

Development of New Benzenesulfonamides As Potent and Selective Nav1.7 Inhibitors for the Treatment of Pain

By taking advantage of certain features in piperidine 4, we developed a novel series of cyclohexylamine- and piperidine-based benzenesulfonamides as potent and selective Nav1.7 inhibitors. However, compound 24, one of the early analogs, failed to reduce phase 2 flinching in the mouse formalin test even at a dose of 100 mpk PO due to insufficient dorsal root ganglion (DRG) exposure attributed to poor membrane permeability. Two analogs with improved membrane permeability showed much increased DRG concentrations at doses of 30 mpk PO, but, confoundingly, only one of these was effective in the formalin test. More data are needed to understand the disconnect between efficacy and exposure relationships.

Discovery of Aryl Sulfonamides as Isoform-Selective Inhibitors of NaV1.7 with Efficacy in Rodent Pain Models

We report on a novel series of aryl sulfonamides that act as nanomolar potent, isoform-selective inhibitors of the human sodium channel hNaV1.7. The optimization of these inhibitors is described. We aimed to improve potency against hNaV1.7 while minimizing off-target safety concerns and generated compound 3. This agent displayed significant analgesic effects in rodent models of acute and inflammatory pain and demonstrated that binding to the voltage sensor domain 4 site of NaV1.7 leads to an analgesic effect in vivo. Our findings corroborate the importance of hNaV1.7 as a drug target for the treatment of pain.