Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Rolapitant (SCH619734) Hydrochloride is the hydrochloride salt form of rolapitant, an orally bioavailable, centrally-acting, selective, neurokinin 1 receptor (NK1-receptor) antagonist with potential antiemetic activity. Upon oral administration, rolapitant competitively binds to and blocks the activity of the NK1-receptor in the central nervous system, thereby inhibiting the binding of the endogenous ligand, substance P (SP). This may prevent both SP-induced emesis and chemotherapy-induced nausea and vomiting (CINV). The interaction of SP with the NK1-receptor plays a key role in the induction of nausea and vomiting caused by emetogenic cancer chemotherapy. Compared to other NK1-receptor antagonists, rolapitant has both a more rapid onset of action and a much longer half-life.
説明 | Rolapitant (SCH619734) Hydrochloride is the hydrochloride salt form of rolapitant, an orally bioavailable, centrally-acting, selective, neurokinin 1 receptor (NK1-receptor) antagonist with potential antiemetic activity. Upon oral administration, rolapitant competitively binds to and blocks the activity of the NK1-receptor in the central nervous system, thereby inhibiting the binding of the endogenous ligand, substance P (SP). This may prevent both SP-induced emesis and chemotherapy-induced nausea and vomiting (CINV). The interaction of SP with the NK1-receptor plays a key role in the induction of nausea and vomiting caused by emetogenic cancer chemotherapy. Compared to other NK1-receptor antagonists, rolapitant has both a more rapid onset of action and a much longer half-life. |
ターゲット&IC50 | NK1:0.66 nM. (Ki) |
別名 | SCH619734 |
分子量 | 500.48 |
分子式 | C25H26F6N2O2 |
CAS No. | 552292-08-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 30 mg/mL (59.94 mM)
You can also refer to dose conversion for different animals. 詳細
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Rolapitant 552292-08-7 GPCR/G Protein Neuroscience Neurokinin receptor SCH619734 foot tapping long-acting emesis retches NK receptor Neurokinin Receptor SCH 619734 vomits SCH-619734 anti-emetic Inhibitor inhibit orally active Mongolian Gerbils Tachykinin receptor ferret inhibitor