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Chemical Structure : CVN45502
Catalog No.: PC-21731Not For Human Use, Lab Use Only.
CVN45502 (CVN 45502) is a potent, orally bioavailable, highly selective orexin 1 receptor (Hcrtr1, OX1R) antagonist with binding affinity (pKi) of 7.86 (human Hcrtr1), significantly reduces feeding and body weight in diet-induced obese (DIO).
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CVN45502 (CVN 45502) is a potent, orally bioavailable, highly selective orexin 1 receptor (Hcrtr1, OX1R) antagonist with binding affinity (pKi) of 7.86 (human Hcrtr1), significantly reduces feeding and body weight in diet-induced obese (DIO).
CVN45502 displays 1000-fold selectivity over human Hcrtr2 receptor (pKi=4.66), CVN45502 (10 µM) also does not engage a broad panel of 125 receptors, ion channels, enzymes and transporters.
CVN45502 is highly brain penetrant with a concentration in the brain of 1.1 ± 0.17 µM 30 minutes after a 3 mg/kg dose and a brain to plasma ratio of 0.7 at 30 minutes and 0.9 at 60 minutes.
CVN45502 fully inhibits the intracellular calcium released in cells expressing Hcrtr1 in response to orexin A with IC50 of 0.02 uM.
CVN45502 (30 mg/kg) ameliorates energy-balance defects after DIO in mice, does not show an alteration of total sleep time or locomotor activity.
CVN45502 (30 mg/kg) leads to a reduction in food intake with no major changes in energy expenditure in leptin deficient genetic obese ob/ob mice.
| M.Wt | 432.41 | |
| Formula | C19H19F3N8O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Marc Schneeberger, et al. Nat Metab. 2022 Nov;4(11):1495-1513.
2. Fieldhouse, C., et al. US patent US-10011588-B2 (2018)
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