1204178-50-6
Chemical Structure
Clofutriben
Synonym(s): ASP3662
- CAS No.: 1204178-50-6
- Formula:C19H16ClF3N4O2
- Molecular Weight:424.80
IUPAC Name: 4-(5-(2-(4-chloro-2,6-difluorophenoxy)propan-2-yl)-4-methyl-4H-1,2,4-triazol-3-yl)-3-fluorobenzamide
InChIKey: CMQOKZCYVZFZLZ-UHFFFAOYSA-N
SMILES: O=C(N)C1=CC=C(C2=NN=C(C(C)(OC3=C(F)C=C(Cl)C=C3F)C)N2C)C(F)=C1
Biological Activity: Clofutriben (ASP3662) is a selective, orally active and brain-penetrant 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with Ki values of 5.3 nM (human), 2.6 nM (mouse), and 23 nM (rat). Clofutriben inhibits conversion of inactive glucocorticoids to active glucocorticoids, reducing intracellular glucocorticoid exposure. Clofutriben ameliorates neuropathic pain, and restores muscle pressure thresholds in rodent models, while lacking effects in inflammatory pain[1][2].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Clofutriben | 98.07% | Clofutriben (ASP3662) is a selective, orally active and brain-penetrant 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with Ki values of 5.3 nM (human), 2.6 nM (mouse), and 23 nM (rat). Clofutriben inhibits conversion of inactive glucocorticoids to active glucocorticoids, reducing intracellular glucocorticoid exposure. Clofutriben ameliorates neuropathic pain, and restores muscle pressure thresholds in rodent models, while lacking effects in inflammatory pain. | ||||||||||||||||||||
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- [1]. Buttgereit F, et al. Effects of clofutriben, a selective 11β-hydroxysteroid dehydrogenase type 1 inhibitor, on the efficacy and toxicity of prednisolone in patients with polymyalgia rheumatica: a single-blind controlled trial with sequential cohorts. Ann Rheum Dis. 2025 Nov 11:S0003-4967(25)04454-1. [Content Brief]
- [2]. Kiso T, et al. Analgesic effects of ASP3662, a novel 11β-hydroxysteroid dehydrogenase 1 inhibitor, in rat models of neuropathic and dysfunctional pain. Br J Pharmacol. 2018;175(19):3784-3796. [Content Brief]
Keywords
