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Rolapitant

Catalog No. T3716   CAS 552292-08-7
Synonyms: SCH619734

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.

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Rolapitant Chemical Structure
Rolapitant, CAS 552292-08-7
Pack Size Availability Price/USD Quantity
1 mg In stock $ 43.00
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
500 mg In stock $ 1,090.00
1 mL * 10 mM (in DMSO) In stock $ 93.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description 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.
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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 30 mg/mL (59.94 mM)

TargetMolReferences and Literature

1. Duffy RA, et al. Rolapitant (SCH 619734): a potent, selective and orally active neurokininNK1 receptor antagonist with centrally-mediated antiemetic effects inferrets. Pharmacol Biochem Behav. 2012 Jul;102(1):95-100.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Drug Library Anti-Cancer Approved Drug Library Anti-Cancer Clinical Compound Library Highly Selective Inhibitor Library Clinical Compound Library GPCR Compound Library Inhibitor Library PPI Inhibitor Library FDA-Approved & Pharmacopeia Drug Library Drug Repurposing Compound Library

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Keywords

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

 

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