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Clofutriben

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Clofutriben

Cas 1204178-50-6

HCL 1203941-88-1

  • ASP 3662
  • 4-(5-(2-(4-Chloro-2,6-difluorophenoxy)propan-2-yl)-4-methyl-4H-1,2,4-triazol-3-yl)-3-fluorobenzamide
  • 4-{5-[2-(4-Chloro-2,6-difluorophenoxy)propan-2-yl]-4-methyl-4H-1,2,4-triazol-3-yl}-3-fluorobenzamide
  • 4-[5-[2-(4-chloro-2,6-difluorophenoxy)propan-2-yl]-4-methyl-1,2,4-triazol-3-yl]-3-fluorobenzamide
  • 4L1TY1U5VC
Molecular Weight424.80
FormulaC19H16ClF3N4O2

Clofutriben (ASP3662) is a 11β-hydroxysteroid dehydrogenase type 1 inhibitor.


Clofutriben is an orally bioavailable selective inhibitor of the enzyme 11beta-hydroxysteroid dehydrogenase type 1 (11b-HSD1; 11bHSD1; HSD11B1; HSD1; HSD-1), with potential protective activity for disorders of corticosteroid excess. Upon oral administration, clofutriben selectively binds to and inhibits the activity of HSD-1. This prevents the conversion of cortisone to the active hormone cortisol and thereby preventing the activation of the glucocorticoid receptors (GRs). By blocking cortisol production in metabolic tissues, clofutriben may inhibit the adverse metabolic effects that are caused by exogenous administration of glucocorticoids or in disorders in which cortisol is secreted in excess. HSD-1 is highly expressed in metabolic tissues, such as liver, skeletal muscle, and adipose tissue. It plays a crucial role in regulating the production of cortisol to activate the GRs.

SCHEME

PATENTS

Clinical and Translational Science (2019), 12(3), 291-301

British Journal of Pharmacology (2018), 175(19), 3784-3796

Sparrow Pharmaceuticals, Inc. WO2020106337

WO2019075394

WO2018117063

WO2010001946

PATENT

PDT PAT FOR HCL SALT, WO2012033070

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2012033070

PATENT

PDT PAT FOR BASE, WO2018117063

PATENT

WO2010001946 

[1]. Kiso T, et al. Analgesic effects of ASP3662, a novel 11尾-hydroxysteroid dehydrogenase 1 inhibitor, in rat models of neuropathic and dysfunctional pain. Br J Pharmacol. 2018 Oct;175(19):3784-3796.  [Content Brief]

////////////Clofutriben, ASP 3662, orphan drug, 4L1TY1U5VC, Sparrow Pharmaceuticals,


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