2. Metabolic Enzyme/Protease
  3. 11β-HSD
  4. Clofutriben

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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Clofutriben

Clofutriben Chemical Structure

CAS No. : 1204178-50-6

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Clofutriben Related Antibodies

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Description

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].

IC50 & Target[1]

11β-HSD1 (mouse)

2.6 nM (Ki)

11β-HSD1 (human)

5.3 nM (Ki)

11β-HSD1 (rat)

23 nM (Ki)

In Vitro

Clofutriben (6-15 nM) potently and competitively inhibits human, mouse, and rat recombinant 11β-HSD1 with Ki values of 5.3 nM, 2.6 nM, and 23 nM respectively[2].
Clofutriben (30 μM) does not inhibit human HEK293-EBNA cell-expressed 11β-HSD2 even at concentrations up to 30 μM[2].
Clofutriben (0.03-10 μM; 30 min before Cortisone) concentration-dependently inhibits Cortisone (HY-17461)-to-Cortisol (HY-N0583) conversion in ex vivo rat prefrontal cortex and spinal cord tissue, with near-complete inhibition at 10 μM[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clofutriben Related Antibodies
In Vivo

Clofutriben (0.03-0.3 mg/kg; p.o.; single dose; 0.03-0.3 μg per animal; i.t.; single dose) dose-dependently ameliorates mechanical allodynia in rats, with an oral ED50 of 0.087 mg/kg and a maximum improvement rate of 80% at 0.3 mg/kg[2].
Clofutriben (0.1-1 mg/kg; p.o.; single dose) at 0.3 and 1 mg/kg significantly ameliorates thermal hyperalgesia in rats, with a maximum improvement rate of 61% at 1 mg/kg[2].
Clofutriben (0.1-1 mg/kg; p.o.; single dose) at 0.3 and 1 mg/kg significantly ameliorates mechanical allodynia in STZ (HY-13753)-induced diabetic rats, with a maximum improvement rate of 52% at 1 mg/kg[2].
Clofutriben (0.1-1 mg/kg; p.o.; single dose) dose-dependently restores muscle pressure thresholds in rats, with an ED50 of 0.31 mg/kg and a maximum improvement rate of 82% at 1 mg/kg[2].
Clofutriben (0.1-1 mg/kg; p.o.; single dose) at doses up to 1 mg/kg has no effect on hot-plate test latency and only a weak effect on tail pinch test latency, indicating minimal activity against acute pain[2].
Clofutriben (0.3-3 mg/kg; p.o.; single dose) at doses up to 3 mg/kg does not impair motor coordination in healthy rats[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague-Dawley (male, 150-315 g, spinal nerve ligation-induced)[2]
Dosage: 0.03, 0.1, 0.3 mg/kg (p.o.); 0.03-0.3 μg per animal (i.t.)
Administration: p.o.; single dose; i.t.; single dose
Result: Significantly raised mechanical paw withdrawal thresholds 2 h post-administration at oral doses of 0.1 and 0.3 mg/kg.
Achieved an 80% improvement rate at 0.3 mg/kg, with an ED50 of 0.087 mg/kg.
Dose-dependently reduced mechanical allodynia following intrathecal administration of 0.03, 0.1, and 0.3 μg per animal, with statistically significant effects at 0.1 and 0.3 μg 60 min post-administration.
Diminished analgesic effect of intrathecal 0.3 μg when co-administered with 10 μg Corticosterone (HY-B1618).
Clinical Trial
Molecular Weight

424.80

Formula

C19H16ClF3N4O2
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Clofutriben Related Classifications

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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:

Clofutriben1204178-50-6ASP3662ASP 3662ASP-366211β-HSD11beta-HSD11β-hydroxysteroid dehydrogenases11 beta-hydroxysteroid dehydrogenaseHEK293-EBNAneuropathic painfibromyalgiaadjuvant-induced arthritispolymyalgia rheumaticahumanrat11β-HSD2mouse11β-hydroxysteroid dehydrogenase type 1Inhibitorinhibitorinhibit

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