1. GPCR/G Protein
    Neuronal Signaling
  2. Neurokinin Receptor
  3. Netupitant

Netupitant (Synonyms: CID 6451149)

Cat. No.: HY-16346 Purity: 99.93%
Handling Instructions

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.

For research use only. We do not sell to patients.

Netupitant Chemical Structure

Netupitant Chemical Structure

CAS No. : 290297-26-6

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5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 90 In-stock
Estimated Time of Arrival: December 31
50 mg USD 260 In-stock
Estimated Time of Arrival: December 31
100 mg USD 460 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

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].

In Vitro

Netupitant (CID-6451149) binds with high affinity the human NK1 receptor (pKi=9.0) with more than 1000 fold selectivity over the NK2 and NK3 (pKi=5.8 for both sites)[2].
Netupitant (1, 10, 100 nM) concentration-dependently antagonizes the stimulatory effects of substance P (SP) showing insurmountable antagonism (pKB=8.87) in CHO NK1 cells[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Netupitant (CID-6451149; 1-10 mg/kg; ip) dose-dependently inhibits SP-elicited the typical scratching, biting and licking response in mice. In gerbils, foot tapping behavior evoked by the intracerebroventricular injection of a NK1 agonist is dose-dependently counteracted by Netupitant given intraperitoneally (ID50 1.5mg/kg) or orally (ID50 0.5mg/kg)[2].
Netupitant (0.1-3 mg/kg; i.v.) produces a concentration-dependent inhibition (mean pKB=9.24) of the responses to SP-methylester (SP-OMe) in the detrusor muscle. Netupitant decreases the frequency of reflex bladder contractions[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

578.59

Formula

C₃₀H₃₂F₆N₄O

CAS No.
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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 2 mg/mL (3.46 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7283 mL 8.6417 mL 17.2834 mL
5 mM --- --- ---
10 mM --- --- ---
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

NetupitantCID 6451149CID6451149CID-6451149Neurokinin ReceptorNK receptororallyCHOantiemeticsubstance PInhibitorinhibitorinhibit

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Netupitant
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HY-16346
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