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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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