[CAS NO. 290297-26-6] Netupitant

Name: Netupitant
Brand: Arctom Scientific
SKU: SLK-S4654

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PRODUCTS SPECIFICATIONS [290297-26-6]

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Catalog

SLK-S4654

Brand

Selleck

CAS

290297-26-6

DESCRIPTION [290297-26-6]

Overview

MDL	-
Molecular Weight	578.59
Molecular Formula	C30H32F6N4O
SMILES	N(C(C(C)(C)C1=CC(C(F)(F)F)=CC(C(F)(F)F)=C1)=O)(C)C=2C(=CC(=NC2)N3CCN(C)CC3)C4=C(C)C=CC=C4

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	1.7283 mL	8.6417 mL	17.2834 mL
5 mM	0.3457 mL	1.7283 mL	3.4567 mL
10 mM	0.1728 mL	0.8642 mL	1.7283 mL
50 mM	0.0346 mL	0.1728 mL	0.3457 mL

Description

Netupitant (CID6451149) is a selective antagonist with potential antiemetic activity.

Targets

Neurokinin-1 receptor ^[1]

In vitro

In CHO NK1 cells, Netupitant concentration-dependently antagonizes the stimulatory effects of substance P (SP) showing insurmountable antagonism (pKB 8.87). In cells expressing NK2 or NK3 receptors, Netupitant is inactive.

In vivo

Netupitant behaves as a brain penetrant, orally active, potent and selective NK1 antagonist. In mice the intrathecal injection of SP elicited the typical scratching, biting and licking response that is dose-dependently inhibited by Netupitant given intraperitoneally in the 1-10 mg/kg dose range. In gerbils, foot tapping behavior evoked by the intracerebroventricular injection of a NK1 agonist is dose-dependently counteracted by Netupitant given intraperitoneally (ID50 1.5 mg/kg) or orally (ID50 0.5 mg/kg). In time course experiments in gerbils Netupitant displayed long lasting effects.

References

[1] Rizzi A, et al. Peptides. 2012, 37(1):86-97.
[2] Stathis M, et al. Eur J Pharmacol. 2012, 689(1-3):25-30.

Synonyms

Benzeneacetamide, N,α,α-trimethyl-N-[4-(2-methylphenyl)-6-(4-methyl-1-piperazinyl)-3-pyridinyl]-3,5-bis(trifluoromethyl)-

N,α,α-Trimethyl-N-[4-(2-methylphenyl)-6-(4-methyl-1-piperazinyl)-3-pyridinyl]-3,5-bis(trifluoromethyl)benzeneacetamide

Netupitant

Ro 67-31898/000

2-[3,5-Bis(trifluoromethyl)phenyl]-N-[6-(4-methylpiperazin-1-yl)-4-o-tolylpyridin-3-yl]-N-methylisobutyramide

2-[3,5-Bis(trifluoromethyl)phenyl]-N,2-dimethyl-N-[4-(2-methylphenyl)-6-(4-methylpiperazin-1-yl)pyridin-3-yl]propanamide