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NK Receptor

NK Receptor

Cat. No. Product Name CAS No. Information
CSN26517 Vofopitant 168266-90-8 Vofopitant (also known as GR-205,171) is an NK1 receptor antagonist. It has antiemetic effects as with other NK1 antagonists, and also shows anxiolytic actions in animals. It was trialled for applications such as the treatment of social phobia and post-traumatic stress disorder, but did not prove sufficiently effective to be marketed.
CSN19815 Tradipitant 622370-35-8 Tradipitant is the 2nd generation neurokinin-1 receptor antagonist, which showed activity in preclinical anxiety models.
CSN13678 Talnetant 174636-32-9 Talnetant is a potent and selective NK3 receptor antagonist ki14 nM hNK-3-CHO and is 100-fold selective for the hNK-3 versus hNK-2 receptor with no affinity for the hNK-1 at concentrations up to 100 M
CSN18094 Talnetant hydrochloride 204519-66-4 Talnetant HCl is a potent and selective NK3 receptor antagonist (ki=1.4 nM, hNK-3-CHO), 100-fold selective for the hNK-3 versus hNK-2 receptor, with no affinity for the hNK-1 at concentrations up to 100 μM.
CSN22504 Serlopitant 860642-69-9 Serlopitant is a selective Neurokinin-1 (NK-1) receptor antagonist.
CSN17283 SB-222200 174635-69-9 SB-222200 is a selective reversible and competitive antagonist of human NK-3 receptor Ki44 nM that effectively crosses the blood-brain barrier
CSN19715 Rolapitant 552292-08-7 Rolapitant inhibits CYP2D6 breast cancer resistance protein BCRP and Neurokinin NK1 Receptor
CSN16098 Rolapitant Hydrochloride Monohydrate   914462-92-3 Rolapitant HCl H2O is a long-acting selective and competitive NK-1 receptor antagonist
CSN16120 Netupitant   290297-26-6 Netupitant a potent and highly selective NK1 receptor antagonist with Ki of 095 nM
CSN19286 Pavinetant 941690-55-7 MLE4901 is an antagonist of Neurokinin 3 Receptor and a potential drug for Polycystic ovary syndrome and menopausal hot flushes
CSN22464 Ibodutant 522664-63-7 MEN 15596 is a potent and selective tachykinin NK2 receptor antagonist with a pKi of 101
CSN17887 Maropitant 147116-67-4 Maropitant is a neurokinin NK1 receptor antagonist
CSN25315 L-732138 148451-96-1 L-732138 is a potent and highly selective competitive tachykinin NK1 receptor antagonist with IC50 of 2.3 nM.
CSN18008 Fosaprepitant 172673-20-0 Fosaprepitant is a neurokinin-1 receptor antagonist for the prevention of chemotherapy-induced nausea and vomiting
CSN12336 Fosaprepitant dimeglumine   265121-04-8 Fosaprepitant Dimeglumine is a prodrug for aprepitant which is a selective and high-affinity antagonist of NK1 receptor.
CSN32902 Fezolinetant 1629229-37-3 Fezolinetant is Neurokinin-3 (NK-3) receptor antagonist.
CSN26553 Casopitant mesylate 414910-30-8 Casopitant mesylate is the mesylate salt of a centrally-acting neurokinin 1 (NK1) receptor antagonist with antidepressant and antiemetic activities. Casopitant competitively binds to and blocks the activity of the NK1 receptor, thereby inhibiting NK1-receptor binding of the endogenous tachykinin neuropeptide substance P (SP), which may result in antiemetic effects. SP is found in neurons of vagal afferent fibers innervating the brain-stem nucleus tractus solitarii and the area postrema, which contains the chemoreceptor trigger zone (CTZ), and may be elevated in response to chemotherapy. The NK1 receptor is a G-protein receptor coupled to the inositol phosphate signal-transduction pathway and is found in both the nucleus tractus solitarii and the area postrema.
CSN10324 Aprepitant   170729-80-3 Aprepitant is a selective and high-affinity neurokinin-1 receptor antagonist with IC50 of 0.1 nM.
CSN33661 Substance P Receptor Antagonist 1 225526-17-0
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