Powder: -20°C for 3 years
In solvent: -80°C for 2 years
Rolapitant 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.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
2 mg | In stock | $ 60.00 | |
5 mg | In stock | $ 85.00 | |
10 mg | In stock | $ 126.00 | |
25 mg | In stock | $ 198.00 | |
50 mg | In stock | $ 328.00 | |
100 mg | In stock | $ 490.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 93.00 |
Description | Rolapitant 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. |
Targets&IC50 | NK1:0.66 nM. (Ki) |
In vitro | Rolapitant has a high affinity for the human NK1 receptor with a Ki of 0.66 nM and high selectivity over the human NK2 and NK3 subtypes of more than 1000-fold. Rolapitant has a preferential affinity for human, guinea pig, gerbil, and monkey NK1 receptors over rat, mouse, and rabbit[1]. |
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 which is the same as clinical data for other NK1 antagonists. The 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[1]. |
Kinase Assay | Rolapitant is made at a stock concentration of 1 mM in 100% DMSO. For most receptor binding studies, the stock solution is diluted with the final concentrations ranged from 0.1 to 3 μM. Radioligand concentrations for competition binding studies ranged from 0.5 to 1 nM. For species comparison studies, 150 pM [125I]-BHSP is incubated with varying concentrations of protein (10-50 μg) prepared from gerbil, rabbit and monkey striata, and from cells expressing cloned rat, mouse and guinea pig NK receptors[1]. |
Synonyms | SCH619734 |
Molecular Weight | 500.48 |
Formula | C25H26F6N2O2 |
CAS No. | 552292-08-7 |
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
DMSO: 30 mg/mL (59.94 mM)
( < 1 mg/ml refers to the product slightly soluble or insoluble )
You can also refer to dose conversion for different animals. More
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
Rolapitant 552292-08-7 GPCR/G Protein Neuroscience Neurokinin receptor SCH619734 foot tapping long-acting emesis retches NK receptor Neurokinin Receptor vomits SCH 619734 SCH-619734 anti-emetic Inhibitor inhibit orally active Mongolian Gerbils Tachykinin receptor ferret inhibitor