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Rolapitant

Catalog No. T3716 CAS 552292-08-7

Synonyms: SCH619734

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.

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Rolapitant, CAS 552292-08-7

Pack Size	Availability	Price/USD
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

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Purity: 98%

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Chemical Properties

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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

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 30 mg/mL (59.94 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References 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 Approved Drug Library NO PAINS Compound Library Anti-Cancer Clinical Compound Library FDA-Approved & Pharmacopeia Drug Library Anti-Cancer Compound Library Inhibitor Library Anti-Cancer Drug Library Bioactive Compound Library Anti-Cancer Active Compound Library Bioactive Compounds Library Max

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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 vomits SCH 619734 SCH-619734 anti-emetic Inhibitor inhibit orally active Mongolian Gerbils Tachykinin receptor ferret inhibitor

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