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Rolapitant

CAS No. : 552292-08-7

MCE 站：Rolapitant

产品活性：Rolapitant (SCH619734)是高效选择性具有口服活性的 neurokinin NK1 受体抑制剂，K_i值为0.66 nM。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：Neurokinin Receptor

In Vitro: Rolapitant has a high affinity for the human NK1 receptor with a K_i of 0.66 nM and high selectivity over the human NK2 and NK3 subtypes of more than 1000-fold, as well as preferential affinity for human, guinea pig, gerbil and monkey NK1 receptors over rat, mouse and rabbit.

In Vivo: Rolapitant reverses NK1 agonist-induced foot tapping in gerbils following both intravenous and oral administration up to 24 hours at a minimal effective dose (MED) of 0.1 mg/kg. Rolapitant is active at 0.1 and 1 mg/kg in both acute and delayed emesis models in ferrets, respectively, consistent with clinical data for other NK1 antagonists. Clinical efficacy of anti-emetics is highly correlated with efficacy in the ferret emesis model, suggesting rolapitant is a viable clinical candidate for this indication.

相关产品：Drug Repurposing Compound Library Plus  |  FDA-Approved Drug Library Plus  |  FDA-Approved Drug Library Mini  |  Bioactive Compound Library Plus  |  GPCR/G Protein Compound Library  |  Neuronal Signaling Compound Library  |  FDA-Approved Drug Library  |  Anti-Cancer Compound Library  |  Drug Repurposing Compound Library  |  Endocrinology Compound Library  |  Anti-COVID-19 Compound Library  |  Orally Active Compound Library  |  Neurotransmitter Receptor Compound Library  |  FDA Approved & Pharmacopeial Drug Library  |  Substance P  |  Aprepitant  |  Netupitant  |  Senktide  |  Fosaprepitant dimeglumine  |  SB-222200  |  Maropitant  |  Vapreotide  |  Neurokinin A TFA  |  Neurokinin B TFA  |  Saredutant  |  Talnetant  |  Vofopitant  |  L-732138  |  NKP608  |  [Sar9,Met(O2)11]-Substance P TFA  |  Eprazinone dihydrochloride  |  Y1 receptor antagonist 1  |  Substance P(1-7) TFA  |  GR 159897  |  Men 10376 TFA  |  Neurokinin A(4-10) TFA  |  Osanetant

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