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Netupitant

Cat. No. M3882
Netupitant Structure
Synonym:

CHEBI441603, CID6451149, D05152

Size Price Availability Quantity
5mg USD 58.5  USD65 In stock
10mg USD 72  USD80 In stock
50mg USD 216  USD240 In stock
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Quality Control
Biological Activity

Netupitant competitively binds to and blocks the activity of the human substance P/NK1 receptors in the central nervous system (CNS), thereby inhibiting NK1-receptor binding of the endogenous tachykinin neuropeptide substance P (SP), which may result in the prevention of chemotherapy-induced nausea and vomiting (CINV). Recent mechanistic studies using NG108-15 cells have shown that palonosetron and netupitant, an NK1 receptor antagonist currently in phase 3 clinical trials, exhibited synergistic effects when inhibiting the substance P response.The present studies showed that both netupitant and palonosetron-induced NK1 receptor internalization in NG108-15 cells and that when used together receptor internalization was additive.Netupitant was well tolerated with most treatment emergent adverse events (AEs) being mild.Palonosetron and netupitant, either alone or in combination, were effective in reducing the induced elevated pPKA levels during the delayed phase.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 578.59
Formula C30H32F6N4O
CAS Number 290297-26-6
Purity 100.0%
Solubility DMSO 6 mg/mL heat to 50°C and ultrasonic
Storage at -20°C
References

Differential and additive suppressive effects of 5-HT3 (palonosetron)- and NK1 (netupitant)-receptor antagonists on cisplatin-induced vomiting and ERK1/2, PKA and PKC activation.
Darmani NA, et al. Pharmacol Biochem Behav. 2015 Feb 14;131C:104-111. PMID: 25687374.

Netupitant and palonosetron trigger NK1 receptor internalization in NG108-15 cells.
Thomas AG, et al. Exp Brain Res. 2014 Aug;232(8):2637-44. PMID: 24969614.

Efficacy and safety of repeated dosing of netupitant, a neurokinin-1 receptor antagonist, in treating overactive bladder.
Haab F, et al. Neurourol Urodyn. 2014 Mar;33(3):335-40. PMID: 23765630.

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Keywords: Netupitant, CHEBI441603, CID6451149, D05152 supplier, Neurokinin Receptor, inhibitors

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