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Netupitant

Netupitant
Netupitant (CID 6451149) is a specific neurokinin 1 (NK1) receptor antagonist (Ki: 0.95 nM).
Catalog No. T6905Cas No. 290297-26-6
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Purity:99.95%
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Netupitant

Catalog No. T6905Cas No. 290297-26-6

Netupitant (CID 6451149) is a specific neurokinin 1 (NK1) receptor antagonist (Ki: 0.95 nM).
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
Pack SizePriceAvailabilityQuantity
5 mg$47In Stock
10 mg$68In Stock
25 mg$122In Stock
50 mg$210In Stock
100 mg$378In Stock
200 mg$558In Stock
500 mg$886In Stock
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Product Introduction

Bioactivity
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.
AliasRo 67-31898/000, CID 6451149
Chemical Properties
Molecular Weight578.59
FormulaC30H32F6N4O
Cas No.290297-26-6
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 5.79 mg/mL (10 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.7283 mL8.6417 mL17.2834 mL86.4170 mL
5 mM0.3457 mL1.7283 mL3.4567 mL17.2834 mL
10 mM0.1728 mL0.8642 mL1.7283 mL8.6417 mL

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