rolapitant

Modify Date: 2024-01-01 19:20:13

rolapitant structure	Common Name	rolapitant
	CAS Number	552292-08-7	Molecular Weight	500.477
	Density	1.3±0.1 g/cm3	Boiling Point	523.5±50.0 °C at 760 mmHg
	Molecular Formula	C₂₅H₂₆F₆N₂O₂	Melting Point	N/A
	MSDS	N/A	Flash Point	270.4±30.1 °C

Use of rolapitant

Rolapitant (SCH619734) is a potent, selective and orally active neurokinin NK1 receptor antagonist with a Ki of 0.66 nM.

Name	(5S,8S)-8-[[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]methyl]-8-phenyl-1,9-diazaspiro[4.5]decan-2-one
Synonym	More Synonyms

Description	Rolapitant (SCH619734) is a potent, selective and orally active neurokinin NK1 receptor antagonist with a Ki of 0.66 nM.
Related Catalog	Signaling Pathways >> GPCR/G Protein >> Neurokinin Receptor Signaling Pathways >> Neuronal Signaling >> Neurokinin Receptor Research Areas >> Cancer
Target	Ki: 0.66 nM (neurokinin)[1]
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, as well as 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, 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[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].
References	[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.

Density	1.3±0.1 g/cm3
Boiling Point	523.5±50.0 °C at 760 mmHg
Molecular Formula	C₂₅H₂₆F₆N₂O₂
Molecular Weight	500.477
Flash Point	270.4±30.1 °C
Exact Mass	500.189850
PSA	53.85000
LogP	4.01
Vapour Pressure	0.0±1.4 mmHg at 25°C
Index of Refraction	1.542
Storage condition	-20℃

(5S,8S)-8-({(1R)-1-[3,5-Bis(trifluoromethyl)phenyl]ethoxy}methyl)-8-phenyl-1,7-diazaspiro[4.5]decan-2-one

UNII-NLE429IZUC

1,7-Diazaspiro[4.5]decan-2-one, 8-[[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]methyl]-8-phenyl-, (5S,8S)-

UNII:NLE429IZUC

rolapitant

DC Chemicals Limited
China
Product Name: Rolapitant
Price: $1100.0/250mg $2500.0/1g $600.0/100mg
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: Rolapitant
Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
Purity: 98.0%
Stocking Period: Inquiry
Contact: Ms Wang

Zhejiang Hangyu API Co., Ltd
China
Product Name: Rolapitant
Price: ￥Inquiry/1kg
Purity: 99.5%
Stocking Period: Inquiry
Contact: Vinnie

Henan Tianfu Chemical Co., Ltd.
China
Product Name: (5S,8S)-8-[[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]methyl]-8-phenyl-1,9-diazaspiro[4.5]decan-2-one
Price: $Inquiry/1kg $Inquiry/25kg $Inquiry/1000kg $Inquiry/10ton
Purity: 99.0%
Stocking Period: Inquiry
Contact: Anson

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Price: $159/10mM*1mLinDMSO

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rolapitant

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