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Medchemexpress LLC Rolapitant hydrochloride hydrate | 914462-92-3 | 98.36% | 554.95 | 100 MG
Supplier: Medchemexpress LLC HY16436100MG
Rolapitant hydrochloride hydrate is a potent, selective, long-acting, and orally active neurokinin 1 (NK1) receptor antagonist with a Ki of 0.66 nM. It does not interact with CYP3A4 and shows potent anti-emetic activity in a ferret emesis model.
- Potent, selective, long-acting, and orally active neurokinin 1 (NK1) receptor antagonist
- Ki of 0.66 nM for human NK1 receptor
- Does not interact with CYP3A4
- Shows potent anti-emetic activity in a ferret emesis model
- High selectivity over human NK2 and NK3 subtypes (more than 1000-fold)
- Preferential affinity for human, guinea pig, gerbil, and monkey NK1 receptors over rat, mouse, and rabbit
- Inhibits GR-73632 (an NK1 receptor agonist)-induced calcium efflux in a concentration-dependent and competitive manner in CHO cells expressing the human NK1 receptor.
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