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Netupitant

Catalog No. T6905   CAS 290297-26-6
Synonyms: Ro 67-31898/000, CID 6451149

Netupitant (CID 6451149) is a specific neurokinin 1 (NK1) receptor antagonist (Ki: 0.95 nM).

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Netupitant Chemical Structure
Netupitant, CAS 290297-26-6
Pack Size Availability Price/USD Quantity
5 mg In stock $ 47.00
10 mg In stock $ 68.00
25 mg In stock $ 122.00
50 mg In stock $ 210.00
100 mg In stock $ 378.00
200 mg In stock $ 558.00
500 mg In stock $ 886.00
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Purity: 99.95%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Netupitant (CID 6451149) is a specific neurokinin 1 (NK1) receptor antagonist (Ki: 0.95 nM).
Targets&IC50 NK1:0.95 nM(Ki)
In vitro Netupitant concentration-dependently antagonizes the stimulatory effects of substance P (SP) in CHO NK1 cells and shows insurmountable antagonism (pKb: 8.87). In cells expressing NK2/3 receptors, Netupitant is inactive.
In vivo In mice the intrathecal injection of SP elicited the typical scratching, biting and licking response is dose-dependently inhibited by Netupitant (1-10 mg/kg, i.p.). In gerbils, foot tapping behavior evoked by the intracerebroventricular injection of an NK1 agonist is dose-dependently counteracted by Netupitant gave intraperitoneally (ID50 1.5 mg/kg) or orally (ID50 0.5 mg/kg). In time course experiments in gerbils, Netupitant displayed long-lasting effects.
Kinase Assay zotarolimus (10 pM-1 μM) in buffer A (2% BSA and 0.2% Tween-20 in D-PBS) is used in the assay of Binding Affinity to FKBP12.
Cell Research Cell lines: NG108-15 cells. Concentrations: 1,3,10,30 nM. Method:cells are preincubated for 1 h at 37℃ with either growth media alone(control) or media containing antagonists.Antagonist concentrations are at least 30-fold the Kd value to ensure receptor saturation.After preincubation,antagonists are removed and cells are rinsed with growth media alone for an additional hour to allow for dissociation of antagonists still bound to the receptor.Cell media are then replaced with isosmotic HEPES buffer (pH 7.4,20 mM) containing NaCl (130 mM),KCl (2 mM),MgCl2 (1 mM) CaCl2 (2 mM),Fluo-4 acetoxymethyl (AM) ester (2 mM),pluronic acid (0.04%) and SP at various concentrations in the 3 nM to 1 mM range.The final incubation lasted for 1 h at 37 ℃.Pluronic acid is added as a nonionic surfactant to sequester the AM ester molecules into micelles for cellular uptake.
Animal Research Animal Models: Male Swiss mice. Formulation: Saline containing 5% DMSO and 5% Tween 80. Dosages: 1 and 10 mg/kg. Administration: i.p.
Synonyms Ro 67-31898/000, CID 6451149
Molecular Weight 578.59
Formula C30H32F6N4O
CAS No. 290297-26-6

Storage

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

Solubility Information

DMSO: 5.79 mg/mL (10 mM), Sonification is recommended

TargetMolReferences and Literature

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.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Neurodegenerative Disease Compound Library Anti-Cancer Drug Library Anti-Cancer Approved Drug Library Anti-Cancer Clinical Compound Library Inhibitor Library Neuronal Signaling Compound Library Anti-Cancer Compound Library Clinical Compound Library GPCR Compound Library FDA-Approved & Pharmacopeia Drug Library

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Keywords

Netupitant 290297-26-6 GPCR/G Protein Neuroscience Neurokinin receptor orally Neurokinin Receptor Tachykinin receptor Inhibitor substance P NK receptor CID6451149 Ro 67-31898/000 inhibit CHO CID-6451149 CID 6451149 antiemetic inhibitor

 

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