NBI 30545
CAS No. : 195054-99-0
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| Cat. No. : | HY-119247 |
| M.Wt: | 398.51 |
| Formula: | C22H30N4O3 |
| Purity: | >98 % |
| Solubility: |
NBI 30545 is a blood-brain barrier permeable CRF1R antagonist with a Ki value of 3.4 nM for the human receptor. NBI 30545 inhibits CRF-stimulated intracellular cAMP accumulation and ACTH release. NBI 30545 can be used in the research of depression, anxiety disorders and stress-related diseases[1].
In Vitro:NBI 30545 inhibits CRF-stimulated cAMP accumulation in cells expressing the human CRF1 receptor with an IC50 of 76 nM[1].
NBI 30545 inhibits CRF-stimulated ACTH release in cultured rat anterior pituitary cells with an IC50 of 37 nM[1].
In Vivo:NBI 30545 (Compound 18n) (10 mg/kg; i.v., p.o.; single dose) achieves good oral plasma and brain exposure in rats with a 30.5% bioavailability and 1.2 brain/plasma ratio, along with extensive tissue distribution and a short half-life after intravenous administration[1].
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