Netupitant

Netupitant (CID-6451149) is a highly potent, selective and orally active neurokinin-1 (NK1) receptor antagonist with a Ki of 0.95 nM for hNK1 in CHO cells. Netupitant has antiemetic affect[1][2][3].

Product Specifications

CAS Number

[290297-26-6]

Product Name Alternative

CID 6451149

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Neurokinin Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease; Endocrinology; Cancer

Assay Protocol

https://www.medchemexpress.com/Netupitant.html

Concentration

10mM

Purity

99.90

Solubility

DMSO : 9.09 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

CN1CCN(C2=CC(C3=C(C)C=CC=C3)=C(N(C)C(C(C4=CC(C(F)(F)F)=CC(C(F)(F)F)=C4)(C)C)=O)C=N2)CC1

Molecular Formula

C30H32F6N4O

Molecular Weight

578.59

Precautions

H302, H315, H319, H335

References & Citations

[1]Hoffmann T, et al. Design and synthesis of a novel, achiral class of highly potent and selective, orally active neurokinin-1 receptor antagonists. Bioorg Med Chem Lett. 2006 Mar 1;16 (5) :1362-5.|[2]Rizzi A, et al. In vitro and in vivo pharmacological characterization of the novel NK1 receptor selective antagonist Netupitant. Peptides. 2012 Sep;37 (1) :86-97.|[3]Stefano Palea, et al. Netupitant, a Potent and Highly Selective NK1 Receptor Antagonist, Alleviates Acetic Acid-Induced Bladder Overactivity in Anesthetized Guinea-Pigs. Front Pharmacol. 2016 Aug 4;7:234.