Netupitant

SKU: orb1222408

Description

Netupitant is a selective neurokinin 1 (NK1) receptor antagonist with potential antiemetic 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).(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).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.(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).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.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 290297-26-6
• MW: 578.59
• Purity: >98% (HPLC)
• Formula: C₃₀H₃₂F₆N₄O
• SMILES: Cc1ccccc1c1cc(ncc1N(C)C(=O)C(C)(C)c1cc(cc(c1)C(F)(F)F)C(F)(F)F)N1CCN(CC1)C
• Target: NK1
• Solubility: DMSO : 23.2 mg/mL; 40.10 mM

Bioactivity

• 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 1.5 mg/kg) or orally (ID50 0.5 mg/kg). 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.
• 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). 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AGE94200 | AGE 94200 | Ro 67-3189 | Netupitant

Quick Database Links

Gene Symbol

NK1