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Chemical Structure : ASP3662
Catalog No.: PC-35375Not For Human Use, Lab Use Only.
ASP3662 is a potent, selective, CNS-penetrable and orally active inhibitor of 11β-HSD1 with Ki of 5.3, 2.6 and 23 nM for human, mouse and rat 11β-HSD1, does not inhibit human 11β-HSD2 at 30 uM.
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ASP3662 (Clofutriben) is a potent, selective, CNS-penetrable and orally active inhibitor of 11β-HSD1 with Ki of 5.3, 2.6 and 23 nM for human, mouse and rat 11β-HSD1, does not inhibit human 11β-HSD2 at 30 uM.
ASP3662 (Clofutriben) demonstrates no appreciable binding affinity to or inhibition against 87 off-targets (adenosine receptors, adrenergic receptors, angiotensin receptors, calcium channels, 5-HT receptors etc.)。
ASP3662 (Clofutriben) inhibits the in vitro conversion of glucocorticoid from its inactive to active form in the brain and spinal cord。
ASP3662 (Clofutriben) ameliorates mechanical allodynia in spinal nerve ligation (SNL) and streptozotocin-induced diabetic rats and thermal hyperalgesia in chronic constriction nerve injury rats.
| M.Wt | 424.808 | |
| Formula | C19H16ClF3N4O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Kiso T, et al. Br J Pharmacol. 2018 Jul 14. doi: 10.1111/bph.14448.
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