2. Signaling Pathways
  3. GPCR/G Protein
    Neuronal Signaling
  4. Neurokinin Receptor
  5. NK1R Isoform
  6. NK1R Antagonist

NK1R Antagonist

NK1R Antagonists (30):

Cat. No. Product Name Effect Purity
  • HY-P3802
    [D-Trp2,7,9] Substance P
    		Antagonist
    [D-Trp2,7,9] Substance P is a tachykinin (Neurokinin Receptor) antagonist with Ki values of 1 μM, 1.3 μM, and ~9 μM for NK-1, NK-2,and NK-3 receptor, respectively.
  • HY-109147
    Imnopitant
    		Antagonist
    Imnopitant is a NK1 receptor antagonist (WO2020132716, compound 1) .
  • HY-119095
    L-741671
    		Antagonist
    L-741671 is a selective and brain-permeable antagonist of neurokininl (hNKI) receptor, with Kis of 64 nM, 0.03 nM and 0.7 nM in rat, human and ferret, respectively.
  • HY-14751A
    Rolapitant hydrochloride
    		Antagonist
    Rolapitant (SCH619734) hydrochloride is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a Ki of 0.66 nM. Rolapitant hydrochloride does not interact with CYP3A4. Rolapitant hydrochloride shows potent anti-emetic activity in a ferret emesis model.
  • HY-10049A
    CP 122721 hydrochloride
    		Antagonist
    CP 122721 hydrochloride is a potent, non-peptide and selective nonpeptide neurokinin NK1 antagonist, with a pIC50 of 9.8 for human NK1 receptor expressed in IM-9 cells. CP 122721 hydrochloride exhibits anxiolytic and antidepressant-like effects.
  • HY-P3881
    (D-Arg1,D-Pro2,D-Phe7,D-His9)-Substance P
    		Antagonist
    (D-Arg1,D-Pro2,D-Phe7,D-His9)-Substance P is a selective NK1 receptor antagonist.
  • HY-12140
    Vestipitant
    		Antagonist
    Vestipitant (GW597599) is a neurokinin-1 receptor antagonist (pKi: 9.4, hNK1) with hypnotic effects and the ability to suppress primary insomnia. Vestipitant can effectively block substance P-mediated extracellular regulated kinase phosphorylation and relieve anxiety and possible depression induced by the agonist GR73632 (HY-P1192) in gerbils. Vestipitant can also improve functional dyspnea, anxiety, insomnia, irritable bowel disease, gastroesophageal reflux disease, tinnitus and antiemetic effects.
  • HY-19670
    Befetupitant
    		Antagonist
    Befetupitant is a high-affinity, nonpeptide, competitive tachykinin 1 receptor (NK1R) antagonist.
  • HY-159842
    Fosrolapitant
    		Antagonist
    Fosrolapitant is a neurokinin 1 (NK1) receptor antagonist.
  • HY-U00207
    MEN11467
    		Antagonist
    MEN11467 is a selective and orally- effective peptidomimetic tachykinin NK1 receptor antagonist.