1204178-50-6
1204178-50-6 structure
- Name: ASP3662
- Chemical Name: ASP3662
- CAS Number: 1204178-50-6
- Molecular Formula: C19H16ClF3N4O2
- Molecular Weight: 424.808
- Catalog: Research Areas Metabolic Disease
- Create Date: 2020-01-12 11:08:50
- Modify Date: 2025-12-02 18:30:52
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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; demonstrates no appreciable binding affinity to or inhibition against 87 off-targets (adenosine receptors, adrenergic receptors, angiotensin receptors, calcium channels, 5-HT receptors etc.); inhibits the in vitro conversion of glucocorticoid from its inactive to active form in the brain and spinal cord; ameliorates mechanical allodynia in spinal nerve ligation (SNL) and streptozotocin-induced diabetic rats and thermal hyperalgesia in chronic constriction nerve injury rats. Alzheimer Disease Phase 2 Discontinued
| Name | ASP3662 |
|---|
| Description | 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; demonstrates no appreciable binding affinity to or inhibition against 87 off-targets (adenosine receptors, adrenergic receptors, angiotensin receptors, calcium channels, 5-HT receptors etc.); inhibits the in vitro conversion of glucocorticoid from its inactive to active form in the brain and spinal cord; ameliorates mechanical allodynia in spinal nerve ligation (SNL) and streptozotocin-induced diabetic rats and thermal hyperalgesia in chronic constriction nerve injury rats. Alzheimer Disease Phase 2 Discontinued |
|---|---|
| References | References 1. Kiso T, et al. Br J Pharmacol. 2018 Jul 14. doi: 10.1111/bph.14448. View Related Products by Target 11β-HSD Alzheimer Disease |
| Molecular Formula | C19H16ClF3N4O2 |
|---|---|
| Molecular Weight | 424.808 |