Search Result
Results for "
NK1 receptors
" in MedChemExpress (MCE) Product Catalog:
6
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-P0201
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- HY-16346
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- HY-109171
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NT-814; BAY3427080
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Neurokinin Receptor
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Cardiovascular Disease
Neurological Disease
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Elinzanetant is an orally active and selective NK-1 and NK-3 receptor antagonist. Elinzanetant alleviates menopause-associated vasomotor symptoms, including hot flashes and night sweats. Elinzanetant reduces estradiol and progesterone levels. Elinzanetant can be used for the research of moderate to severe vasomotor and sleep disorders associated with menopause .
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- HY-14751
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SCH619734
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Neurokinin Receptor
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Neurological Disease
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Rolapitant (SCH619734) is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a Ki of 0.66 nM. Rolapitant does not interact with CYP3A4. Rolapitant shows potent anti-emetic activity in a ferret emesis model .
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- HY-101249
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Neurokinin Receptor
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Neurological Disease
Cancer
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L-732138 is a selective, potent and competitive neurokinin-1 (NK-1) receptor antagonist with an IC50 of 2.3 nM. L-732138 has 200-fold more potent in cloned human NK-1 receptors than cloned rat NK-1 receptors, and has > 1000-fold more potent than human NK-2 and NK-3 receptors. L-732138 can reduce hyperalgesia and has antitumor action .
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- HY-P1192
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Neurokinin Receptor
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Neurological Disease
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GR-73632 is a tachykinin NK1 receptor agonist. GR-73632 activates spinal NK1 receptors to induce scratching, biting and licking behaviors. GR-73632 activates peripheral NK1 receptors to trigger lacrimation in guinea pigs, and activates central NK1 receptors to induce repetitive hind paw tapping behavior in gerbils. GR-73632 is applicable to research related to pruritus .
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- HY-16436
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SCH619734 hydrochloride hydrate
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Neurokinin Receptor
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Neurological Disease
Cancer
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Rolapitant hydrochloride hydrate (SCH619734 hydrochloride hydrate) is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a Ki of 0.66 nM. Rolapitant hydrochloride hydrate does not interact with CYP3A4. Rolapitant hydrochloride hydrate shows potent anti-emetic activity in a ferret emesis model .
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- HY-108483
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Neurokinin Receptor
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Neurological Disease
Inflammation/Immunology
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RP 67580 is a non-peptide antagonist of substance P (SP), competitively inhibits the binding of [3H]SP to neurokinin receptor 1 (NK1 receptor) in rat brain membranes with a Ki value of 4.16 nM. RP 67580 is a specific antagonist of NK1 receptors and can be used in the research of pain and neurogenic inflammation .
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- HY-10053
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- HY-P0061A
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RC-160 acetate; BMY-41606 acetate
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Neurokinin Receptor
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Cancer
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Vapreotide acetate (RC-160 acetate; BMY-41606 acetate) is a neurokinin-1 (NK1) receptor antagonist, with an IC50 of 330 nM.
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- HY-14406A
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Neurokinin Receptor
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Neurological Disease
Cancer
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L-733060 hydrochloride is a selective neurokinin-1 (NK-1) receptor antagonist. L-733060 hydrochloride mainly regulates pain transmission and neural plasticity by blocking the binding of Substance P (P substance) to the NK-1 receptor. L-733060 hydrochloride blocks the promoting effect of Substance P on long-term potentiation (LTP) in the hippocampus. L-733060 hydrochloride reverses the orofacial hyperalgesia induced by experimental occlusal interference (EOI) in rats. L-733060 hydrochloride hydrochloride inhibits neurogenic plasma extravasation at a dose that does not cause adverse cardiovascular effects in rodents, and also acts as an anti-tumor agent. L-733060 hydrochloride can be used for the study of chronic orofacial pain .
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- HY-P0061
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- HY-P0201A
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- HY-P1194
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Neurokinin Receptor
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Inflammation/Immunology
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Spantide I, a substance P analog, is a selective NK1 receptor antagonist, with Ki values of 230 nM and 8150 nM for NK1 and NK2 receptor, respectively. Spantide I provides an approach to reduce type 1 and enhance the type 2 cytokine IL-10 in the infected cornea, leading to a significant reduction in corneal perforation .
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- HY-P2546
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Neurokinin Receptor
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Neurological Disease
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Biotin-Substance P is the biotin tagged Substance P. Substance P (Neurokinin P) is a neuropeptide, acting as a neurotransmitter and as a neuromodulator in the CNS. The endogenous receptor for substance P is neurokinin 1 receptor (NK1-receptor, NK1R) .
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- HY-P1030
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Neurokinin Receptor
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Endocrinology
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Hemokinin 1 (mouse) is a selective agonist of neurokinin-1 receptor, with Ki of 0.175 nM and 560 nM for human NK1 receptor and human NK2 receptor, respectively.
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- HY-122347A
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GW823296 maleate
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Neurokinin Receptor
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Neurological Disease
Inflammation/Immunology
|
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Orvepitant maleate (GW823296 maleate) is potent, selective, orally active and well-tolerated neurokinin-1 receptor (NK-1) antagonist with a pKi of 10.2 for human neurokinin-1 receptor. Orvepitant maleate can across the blood-brain barrier. Orvepitant maleate has the potential for depressive disorder and chronic refractory cough (CRC) treatment .
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- HY-P1278
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Neurokinin Receptor
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Neurological Disease
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GR 64349 is a potent and highly selective NK2 receptor peptide agonist, with an EC50 of 3.7 nM in rat colon. GR 64349 exhibits selectivity >1000 and >300-fold with respect to NK1 and NK3 receptors, respectively .
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- HY-133206A
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Pronetupitant chloride monohydrochloride
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Neurokinin Receptor
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Cancer
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Fosnetupitant chloride monohydrochloride (Pronetupitant chloride monohydrochloride) is an NK1 antagonist with pKi values of 9.5, 6.1 for human NK1 and NK3 receptor, respectively. Fosnetupitant chloride monohydrochloride is a methylene phosphate prodrug of Netupitant .
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- HY-P1012
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- HY-145250
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- HY-P2000
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- HY-17615
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- HY-P3092
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Neurokinin Receptor
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Neurological Disease
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Phyllomedusin, an tachykinin decapeptide, is a NK1 receptor agonist. Phyllomedusin has vasodilating activity and provokes the contraction of the pylorus .
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- HY-16346S
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- HY-151413
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Neurokinin Receptor
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Neurological Disease
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MEN 10207 is a selective NK-2 tachykinin receptor (Neurokinin Receptor) antagonist. MEN 10207 has pA2 values of 5.2, 7.9 and 4.9 in three monoreceptor in vitro assays for NK-1, NK-2 and NK-3 tachykinin receptors, respectively.
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- HY-178269
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Drug Metabolite
Neurokinin Receptor
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Neurological Disease
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SCH-720881 is the active metabolite of Rolapitant (HY-14751). Rolapitant (SCH619734) is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a Ki of 0.66 nM. Rolapitant does not interact with CYP3A4. Rolapitant shows potent anti-emetic activity in a ferret emesis model .
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- HY-19665
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LY303870
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Neurokinin Receptor
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Neurological Disease
Inflammation/Immunology
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Lanepitant (LY303870) is a selective neurokinin-1 (NK-1) receptor antagonist. Lanepitant blocks neurogenic inflammation and pain transmission by preventing the binding of substance P to NK-1 receptors on both neuronal and non-neuronal tissues. Lanepitant can be used to study osteoarthritis .
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- HY-P1738
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- HY-P3890A
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Neurokinin Receptor
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Neurological Disease
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Substance P (5-11) TFA TFA, the C-terminal heptapeptide of Substance P (HY-P0201), is a neuropeptide. Substance P (5-11) TFA TFA binds to NK-1 tachykinin receptor .
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- HY-108479
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SR140333
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Neurokinin Receptor
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Neurological Disease
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Nolpitantium (SR140333) is a potent, selective, competitive, non-peptide tachykinin NK1 receptor antagonist. Nolpitantium blocks the activation of rat thalamic neurons after nociceptive stimulation .
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- HY-P1277
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- HY-P3881
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- HY-12114
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- HY-108480
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Neurokinin Receptor
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Neurological Disease
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SDZ NKT 343 is a selective, orally active NK1 receptor antagonist with an IC50 of 0.62 nM against human NK1 receptor. SDZ NKT 343 has good analgesic activity .
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- HY-P1193
-
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Neurokinin Receptor
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Neurological Disease
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GR 82334 is a potent and specific reversible tachykinin NK1 receptor antagonist . GR 82334 inhibits substance P-induced sensitization by blocking SP NK1 receptors in naked mole-rats .
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- HY-P10599
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Neurokinin Receptor
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Neurological Disease
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Scyliorhinin I is a tachykinin-1 (NK-1) and tachykinin-2 (NK-2) receptor agonist with a Ki value of 0.9 nM for rat submandibular gland NK-1 receptor and 2 nM for hamster bladder NK-2 receptor. Scyliorhinin I has the ability to contract the longitudinal muscles of the guinea pig ileum .
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- HY-G0012
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- HY-U00207
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- HY-P2475
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- HY-P1379
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- HY-P3890
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- HY-117216
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- HY-10053A
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- HY-P3889
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Neurokinin Receptor
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Neurological Disease
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Substance P (6-11) is the C-terminal hexapeptideamide of Substance P (HY-P0201). Substance P (6-11) binds to NK-1 tachykinin receptor. Substance P (6-11) shows depolarization of motoneurons and a hypotensive effect .
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- HY-137462
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L-Leucyl-L-phenylalaninamide
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Neurokinin Receptor
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Neurological Disease
Inflammation/Immunology
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Leucyl-phenylalanine amide (L-Leucyl-L-phenylalaninamide) is a dipeptide analog. Leucyl-phenylalanine amide is a ligand of SP1-7 with a Ki value of 10.2 nM. Leucyl-phenylalanine amide shows no binding activity to human NK-1 or NK-3 receptors .
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- HY-14406
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Neurokinin Receptor
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Neurological Disease
Cancer
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L-733060 is a selective neurokinin-1 (NK-1) receptor antagonist. L-733060 mainly regulates pain transmission and neural plasticity by blocking the binding of Substance P (P substance) to the NK-1 receptor. L-733060 blocks the promoting effect of Substance P on long-term potentiation (LTP) in the hippocampus. L-733060 reverses the orofacial hyperalgesia induced by experimental occlusal interference (EOI) in rats. L-733060 hydrochloride inhibits neurogenic plasma extravasation at a dose that does not cause adverse cardiovascular effects in rodents, and also acts as an anti-tumor agent. L-733060 can be used for the study of chronic orofacial pain .
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- HY-118356
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Neurokinin Receptor
mAChR
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Neurological Disease
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WIN 62,577 is a rat-specific, but non-human, NK1 receptor antagonist. WIN 62,577 interacts with M1-M4 mAChRs and is an allosteric enhancer of acetylcholine affinity targeting the M3 receptor.
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- HY-P1198
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Neurokinin Receptor
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Neurological Disease
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Hemokinin 1, human is a selective tachykinin neurokinin 1 (NK1) receptor full agonist. Hemokinin 1, human is a full agonist at NK2 and NK3 receptor. Hemokinin 1, human can produces an opioid-independent analgesia .
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- HY-109147A
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- HY-128537
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Neurokinin Receptor
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Inflammation/Immunology
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DNK-333 is a potent and balanced dual NK1 and NK2 receptor antagonist with IC50 values of 4.8 nM and 5.5 nM, respectively. DNK-333 blocks the Neurokinin A (NKA) (HY-P0197)-induced bronchoconstriction in asthma .
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- HY-120928
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- HY-P3891
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- HY-105346
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Neurokinin Receptor
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Neurological Disease
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WIN 51708 is a nonpeptide antagonist of neurokinin (NK)-1 receptor. WIN 51708 has a higher affinity for the rat NK-1 receptor compared to the human NK-1 receptor .
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- HY-106659
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NK-1 Antagonist 1
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Neurokinin Receptor
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Neurological Disease
Endocrinology
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SCH 900978 (NK-1 Antagonist 1) is an antagonist of NK-1 receptor, used in the research of NK-1 related diseases and conditions such as cough, overactive bladder, alcohol dependency and depression .
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- HY-108481
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Neurokinin Receptor
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Neurological Disease
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L-760735 is a high affinity, selective and orally active NK1 receptor antagonist with an IC50 of 0.19 nM for human NK1 receptors. L-760735 exhibits anxiolytic and antidepressant-like effects .
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- HY-159842
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- HY-P0061B
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RC160 diacetate; BMY 41606 diacetate
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Neurokinin Receptor
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Cancer
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Vapreotide diacetate is a neurokinin-1 (NK1) receptor antagonist, with an IC50 of 330 nM.
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- HY-109147
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- HY-12141
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GW597599 mesylate; GW597599B
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Neurokinin Receptor
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Neurological Disease
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Vestipitant (GW597599) mesylate is a selective, orally active, and blood-brain barrier penetrant NK1 receptor antagonist. Vestipitant mesylate exhibits high affinity for the human NK1 receptor (pKi: 9.65). Vestipitant mesylate can be used in the research of diseases such as depression, anxiety disorders, and nausea and vomiting .
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- HY-10049A
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Neurokinin Receptor
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Neurological Disease
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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 .
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- HY-G0011
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- HY-105436
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- HY-P0255
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- HY-P1194A
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Neurokinin Receptor
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Inflammation/Immunology
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Spantide I TFA, a substance P analog, is a selective NK1 receptor antagonist, with Ki values of 230 nM and 8150 nM for NK1 and NK2 receptor, respectively. Spantide I provides an approach to reduce type 1 and enhance the type 2 cytokine IL-10 in the infected cornea, leading to a significant reduction in corneal perforation .
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- HY-131463
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Neurokinin Receptor
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Cancer
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ASN-1377642 is a NK1 receptor antagonist with a Ki value of 251 nM. ASN-1377642 shows antitumor action in breast cancer cells with NK1R-Tr high expression .
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- HY-P1194B
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- HY-10053B
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- HY-10051
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- HY-119005A
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- HY-17012
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RPR 100893
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Neurokinin Receptor
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Inflammation/Immunology
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Dapitant (RPR 100893) is a non-peptide Substance P antagonist with high affinity for the human NK1 receptor. It belongs to the 7,7,4-trimethylperhydroisoindole class of compounds. Dapitant inhibits the binding of Substance P to NK1 receptors, thereby blocking its neurokinin-mediated effects. This novel antagonist represents a potential therapeutic option for conditions involving Substance P, such as neurogenic inflammation and pain modulation .
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- HY-P1012A
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- HY-117216B
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- HY-117216A
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- HY-P3802
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Neurokinin Receptor
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Neurological Disease
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[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 .
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- HY-P10588
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Neurokinin Receptor
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Others
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WIN 66306 is a cyclic heptapeptide that can be isolated from an Aspergillus species. WIN 66306 is a neurokinin antagonist with antagonistic effects on both NK1 and NK2 receptors .
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- HY-118378
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Neurokinin Receptor
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Neurological Disease
Endocrinology
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ZD6021 is an orally active Neurokinin 1 Receptor antagonist, with Ki values of 0.12 nM for NK1 and 0.62 nM for NK2. At a concentration of 100 nM, ZD6021 has a pKB value of 8.9 for human pulmonary artery NK1 receptors, and a pKB value of 7.3 for human bronchial NK2 receptors. ZD6021 effectively reduces ASMSP-induced plasma protein extravasation in guinea pigs, with an ED50 of 0.5 mg/kg, and also decreases NK2 mediated bronchoconstriction, with an ED50 of 13 mg/kg .
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- HY-116958
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Neurokinin Receptor
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Inflammation/Immunology
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SCH 206272 is a selective antagonist of the tachykinin (NK) receptor. SCH 206272 inhibits binding at human tachykinin NK(1), NK(2), and NK(3) receptors (Ki = 1.3, 0.4, and 0.3 nM, respectively). SCH 206272 has an orally active .
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- HY-P1277A
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Neurokinin Receptor
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Neurological Disease
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GR 94800 TFA is a potent and selective NK2 receptor peptide antagonist, with pKB values of 9.6, 6.4 and 6.0 for NK2, NK1 and NK3 receptors, respectively .
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- HY-157743
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Neurokinin Receptor
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Neurological Disease
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SCH 60057 (Compound 7) is a neurokinin (NK) receptor inhibitor that can be isolated from Acremonium sp., with IC50 values of 6 μM and 12 μM for NK1 and NK2, respectively .
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- HY-161835
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- HY-118463
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(-)-Benzomalvin A
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Neurokinin Receptor
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Neurological Disease
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Benzomalvin A is a potent antagonist of neurokinin receptor isolated from Penicillium sp. Benzomalvin A shows inhibitory activity against substance P with Ki values of 12, 42 and 43 μM at the guinea pig, rat and human neurokinin NK1 receptors, respectively .
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- HY-122347
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GW823296
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Neurokinin Receptor
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Neurological Disease
Cancer
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Orvepitant (GW823296) is potent, selective, orally active and well-tolerated neurokinin-1 receptor (NK-1) antagonist with a pKi of 10.2 for human neurokinin-1 receptor. Orvepitant can across the blood-brain barrier. Orvepitant has the potential for depressive disorder and chronic refractory cough (CRC) treatment .
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- HY-P1278A
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Neurokinin Receptor
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Neurological Disease
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GR 64349 is a potent and highly selective NK2 receptor peptide agonist, with an EC50 of 3.7 nM in rat colon. GR 64349 exhibits selectivity >1000 and >300-fold with respect to NK1 and NK3 receptors, respectively .
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- HY-106982
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CJ-11,974
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Neurokinin Receptor
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Neurological Disease
Metabolic Disease
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Ezlopitant (CJ-11,974) is a selective, non-peptidic neurokinin-1 (NK-1)-receptor antagonist. Ezlopitant inhibits both acute and delayed emetic reactions induced by Cisplatin (HY-17394) in ferrets via acting on NK1 receptors in the central nervous system. Ezlopitant has the potential for pain, chemotherapy-induced emesis and irritable bowel syndrome research .
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- HY-P1379A
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Neurokinin Receptor
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Neurological Disease
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C14TKL-1 acetate is the acetate salt form of C14TKL-1 (HY-P1379). C14TKL-1 acetate is a tachykinin-like peptide and exhibits an agonistic activity for neurokinin receptor 1 (NK-1) .
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- HY-169501
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- HY-120308
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SR140603
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Neurokinin Receptor
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Neurological Disease
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(R)-Nolpitantium is the R-enantiomer of Nolpitantium (HY-108479). Nolpitantium (SR140333) is a potent, selective, competitive, non-peptide tachykinin NK1 receptor antagonist. Nolpitantium blocks the activation of rat thalamic neurons after nociceptive stimulation .
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- HY-119552
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LL-S490β
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Endogenous Metabolite
Neurokinin Receptor
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Neurological Disease
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Acetylaszonalenin, a prenylated indole derivative, is a fungal metabolite.Acetylaszonalenin is a potent neurokinin-1 (NK1) receptor antagonist. Acetylaszonalenin shows inhibition of [ 3H]-SP binding to human astrocytoma cells with a Ki of 170 μM .
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- HY-P1198A
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Neurokinin Receptor
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Neurological Disease
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Hemokinin 1, human TFA is a selective tachykinin neurokinin 1 (NK1) receptor full agonist. Hemokinin 1, human TFA is a full agonist at NK2 and NK3 receptor. Hemokinin 1, human TFA can produces an opioid-independent analgesia .
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- HY-P10619
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- HY-19403
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Neurokinin Receptor
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Neurological Disease
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TKA-731 is an NK1 receptor antagonist. TKA-731 can reverse mechanical hyperalgesia and has shown analgesic effects in a neuropathic pain model in guinea pigs. TKA-731 can be used in the research of neuropathic pain .
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- HY-172514
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Neurokinin Receptor
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Cancer
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(1R,2S,3R)-Aprepitant (Compound ent-4) is a competitive human neurokinin-1 (NK-1) receptor antagonist. (1R,2S,3R)-Aprepitant is promising for research of cancers and postoperative nausea and vomiting .
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- HY-14751A
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SCH619734 hydrochloride
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Neurokinin Receptor
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Neurological Disease
Cancer
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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 .
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- HY-129296
-
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Endogenous Metabolite
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Neurological Disease
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YM-44781 free acid is a non-peptide neuropeptide receptor antagonist with efficient NK(2) and NK(1) receptor antagonist activity. YM-44781 exhibits significant binding affinity on the NK(2) receptor (pKi = 9.94) and also on the NK(1) receptor Higher binding affinity (pKi = 9.09). In addition, YM-44781 also showed significant inhibitory effects on bladder contraction induced by selective NK(1) receptor agonists .
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- HY-101249R
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Neurokinin Receptor
Reference Standards
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Neurological Disease
Cancer
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L-732138 (Standard) is the analytical standard of L-732138 (HY-101249). This product is intended for research and analytical applications. L-732138 is a selective, potent and competitive neurokinin-1 (NK-1) receptor antagonist with an IC50 of 2.3 nM. L-732138 has 200-fold more potent in cloned human NK-1 receptors than cloned rat NK-1 receptors, and has > 1000-fold more potent than human NK-2 and NK-3 receptors. L-732138 can reduce hyperalgesia and has antitumor action .
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- HY-P2139
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Neurokinin Receptor
Phospholipase
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Others
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Ranakinin is a NK1R agonist. Ranakinin inhibits the binding of selective NK1 radioligands to NK1 receptors. Ranakinin activates phospholipase C (Phospholipase C), thereby enhancing polyphosphoinositide hydrolysis. Ranakinin stimulates inositol phosphate production and reduces membrane polyphosphoinositide levels. Ranakinin stimulates corticosterone and aldosterone secretion .
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- HY-19203
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Neurokinin Receptor
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Neurological Disease
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CGP-49823 is an orally active and highly selective antagonist of the neurokinin 1 receptor (NK1 receptor). CGP-49823‘s potency is significantly higher in isolated spinal cords of hamsters than in those of rats. CGP 49823 exhibits a significant anti-anxiety effect in social interaction experiments of rats, and its tolerance develops slowly, without causing anxiety-like withdrawal reactions after discontinuation. CGP-49823 can be used in anxiety and depression research .
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- HY-N9554
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Neurokinin Receptor
Endogenous Metabolite
Calcium Channel
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Neurological Disease
Inflammation/Immunology
|
|
WIN-64821 is a secondary metabolite produced by Aspergillus species, and acts as a Neurokinin Receptor antagonist. The Ki values of WIN-64821 for NK1, NK2 and NK3 receptors are 0.24 (human astrocytoma cells), 0.26 (rat duodenum) and 15.2 (guinea pig forebrain) μM, respectively. WIN-64821 inhibits apamin-induced contraction of rat vas deferens, blocks substance P-induced contraction of guinea pig ileum and Ca 2+ efflux in human astrocytoma cells. WIN-64821 is applicable to analgesic and anti-inflammatory research .
|
-
- HY-123497
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
R116031 is a selective Neurokinin-1 (NK-1) receptor antagonist with a Ki of 0.45 nM for human NK-1 receptor. R116031 inhibits Substance P (HY-P0201)-induced peripheral effects (skin reactions and plasma extravasation in guinea pigs) and a central effect (thumping in gerbils).R116031 labeled with 3H significantly accumulate in the striatum, olfactory tubercule, olfactory bulb and locus coeruleus in gerbils models. R116031 can be used as a positron emission tomography (PET) ligand for PET imaging .
|
-
- HY-P0187
-
|
|
Neurokinin Receptor
|
Neurological Disease
Endocrinology
|
|
Senktide is a potent, selective agonist of the neuromedin K3 (NK3) receptor (EC50=0.5-3 nM). Senktide less potently agonizes the NK1 receptor (EC50=35 µM). Senktide is promising for research of neurological disease .
|
-
- HY-W755425
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
Senktide TFA is a potent, selective agonist of the neuromedin K3 (NK3) receptor (EC50=0.5-3 nM). Senktide TFA less potently agonizes the NK1 receptor (EC50=35 µM). Senktide TFA is promising for research of neurological disease .
|
-
- HY-10053S
-
|
|
Isotope-Labeled Compounds
Neurokinin Receptor
|
Neurological Disease
Endocrinology
|
|
Maropitant-d3 is the deuterium labeled Maropitant. Maropitant is a selective and orally active neurokinin (NK1) receptor antagonist. Maropitant acts by blocking the binding of substance P within the emetic center and the chemoreceptor trigger zone (CRTZ). Maropitant is highly effective in preventing vomiting .
|
-
- HY-117952
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
L 743310 is a non-peptide, selective antagonist of the human neurokinin hNK1 receptor, with high affinity for primate and cloned human hNK1 receptors and lower affinity for rodent NK1 receptors. L 743310 inhibits resiniferatoxin-induced plasma protein extravasation in guinea pig esophagus. L 743310 has a dose-dependent inhibitory effect on cisplatin-induced emesis .
|
-
- HY-12145
-
|
|
Endogenous Metabolite
Neurokinin Receptor
p38 MAPK
|
Neurological Disease
|
|
CP-99994 hydrochloride is a Tachykinin neurokinin 1 (NK-1) receptor antagonist with a Ki of 0.25 nM. CP-99994 hydrochloride prevents colorectal sensitization in the context of visceral hypersensitivity. CP-99994 hydrochloride reduces colorectal hypersensitivity induced by acetic acid injections in a model of bladder-colon cross-sensitization. CP-99994 hydrochloride attenuates the neuroglial interactions and MAPK-p38 phosphorylation associated with visceral hypersensitivity .
|
-
- HY-12144
-
|
|
Neurokinin Receptor
p38 MAPK
|
Neurological Disease
|
|
CP-99994 is a Tachykinin neurokinin 1 (NK-1) receptor antagonist with a Ki of 0.25 nM. CP-99994 prevents colorectal sensitization in the context of visceral hypersensitivity. CP-99994 reduces colorectal hypersensitivity induced by acetic acid injections in a model of bladder-colon cross-sensitization. CP-99994 hydrochloride attenuates the neuroglial interactions and MAPK-p38 phosphorylation associated with visceral hypersensitivity .
|
-
- HY-10053R
-
|
|
Reference Standards
Neurokinin Receptor
|
Neurological Disease
Endocrinology
|
|
Maropitant (Standard) is the analytical standard of Maropitant. This product is intended for research and analytical applications. Maropitant is a selective and orally active neurokinin (NK1) receptor antagonist. Maropitant acts by blocking the binding of substance P within the emetic center and the chemoreceptor trigger zone (CRTZ). Maropitant is highly effective in preventing vomiting .
|
-
- HY-16346R
-
|
CID 6451149 (Standard)
|
Reference Standards
Neurokinin Receptor
|
Neurological Disease
Endocrinology
|
|
Netupitant (Standard) is the analytical standard of Netupitant. This product is intended for research and analytical applications. 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 .
|
-
- HY-180376
-
|
|
Neurokinin Receptor
|
Inflammation/Immunology
|
|
TAC 363 is a selective tachykinin NK-2 receptor antagonist. TAC 363 shows a rightward shift in the contractile response curve induced by Neurokinin A (HY-P0197) with a pA2 of 9.82. TAC 363 has a weak antagonistic effect on NK-1 receptors. TAC 363 can inhibit Neurokinin A-induced bronchoconstriction in guinea pigs with an ED50 of 0.3 mg/kg. TAC 363 can be used for the research of bronchial asthma .
|
-
- HY-10053S1
-
|
|
Isotope-Labeled Compounds
Neurokinin Receptor
|
Neurological Disease
Endocrinology
|
|
Maropitant- 13C,d3 is the 13C- and deuterium labeled Maropitant. Maropitant is a selective and orally active neurokinin (NK1) receptor antagonist. Maropitant acts by blocking the binding of substance P within the emetic center and the chemoreceptor trigger zone (CRTZ). Maropitant is highly effective in preventing vomiting .
|
-
- HY-105215
-
|
|
Neurokinin Receptor
|
Inflammation/Immunology
|
|
FK888 is a potent, selective, and high affinity dipeptide NK1 receptor antagonist. FK888 displaces [3H]-SP binding with a Ki value of 0.69 nM and 0.45 microM. FK888 also inhibits SP-induced airway oedema in guinea-pig after both intravenous and oral administration .
|
-
- HY-19633
-
|
|
Neurokinin Receptor
|
Infection
Endocrinology
|
|
CS-003 Free base (CS-003), a triple tachykinin receptor antagonist, shows high affinities for human (Neurokinin) NK1, NK2 and NK3 receptors with Ki values of 2.3 nM, 0.54 nM and 0.74 nM, respectively. CS-003 Free base (CS-003) has therapeutic efficacy on respiratory diseases associated with neurokinins.
|
-
- HY-10050
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
CJ-17493 is a neurokinin-1 (NK1) receptor antagonist, with a Ki of 0.2 nM. CJ-17493 shows moderate affinity for the verapamil-binding site of L-type Ca 2+ channels (IC50 = 164 nM) and site 2 of sodium channels (IC50 = 48 nM). CJ-17493 can be used for the study of neurological diseases .
|
-
- HY-14751R
-
|
SCH619734 (Standard)
|
Reference Standards
Neurokinin Receptor
|
Neurological Disease
Cancer
|
|
Rolapitant (Standard) is the analytical standard of Rolapitant. This product is intended for research and analytical applications. Rolapitant (SCH619734) is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a Ki of 0.66 nM. Rolapitant does not interact with CYP3A4. Rolapitant shows potent anti-emetic activity in a ferret emesis model .
|
-
- HY-10049
-
|
|
Neurokinin Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
CP 122721 is an orally active NK1 receptor antagonist. CP 122721 attenuates cisplatin-induced vomiting in ferrets (ID50: 0.08 mg/kg). CP 122721 inhibits kainate (KA)-induced seizure activity and CA1 neuronal cell death in rats. CP 122721 is useful in the study of depression, asthma, and irritable bowel syndrome (IBS) .
|
-
- HY-14405
-
|
GW679769
|
Neurokinin Receptor
Cytochrome P450
|
Neurological Disease
|
|
Casopitant (GW679769) is a potent, selective, brain-penetrant and orally active neurokinin 1 (NK1) receptor antagonist. Casopitant antagonizes the emetic effects of Substance P (HY-P0201). Casopitant is also a substrate and weak to moderate inhibitor of CYP3A4. Casopitant is indicated for chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea and vomiting (PONV) .
|
-
- HY-120167
-
|
|
Neurokinin Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
YM-44778 is a neurokinin receptor antagonist. The pKi values for NK1, NK2 and NK3 are 8.08, 8.55 and 8.24, respectively. YM-44778 inhibits the increase of bladder pressure induced by substance [Sar9,Met(O2)11] -P (HY-P1012) in anestheticized rats .
|
-
- HY-14405A
-
|
GW679769B
|
Neurokinin Receptor
Cytochrome P450
|
Neurological Disease
Cancer
|
|
Casopitant mesylate (GW679769B) is a potent, selective, brain permeable and orally active neurokinin 1 (NK1) receptor antagonist. Casopitant mesylate is a second in the class of antiemetics that acts to antagonise the emetogenic effect of Substance P (HY-P0201). Casopitant mesylate is also a substrate and a weak-to-moderate inhibitor of CYP3A4. Casopitant mesylate can be used for chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea and vomiting (PONV) .
|
-
- HY-116620
-
|
|
Neurokinin Receptor
|
Infection
|
|
Benzomalvin C is a weak antagonist of the neurokinin-1 (NK1) receptor inhibiting binding of substance P by 46% when used at 100 μg/mL in vitro. It is also a weak inhibitor of indolamine 2,3-dioxygenase (IDO) with an IC50 value of 130 μM for recombinant IDO. It is isolated from Penicillium and contains an epoxide group at C-19 and C-20, which is not present in benzomalvins A, B, or E.
|
-
- HY-107691
-
|
|
Neurokinin Receptor
|
Neurological Disease
Endocrinology
Cancer
|
|
GR 159897 is a highly potent, selective, competitive, brain-penetrated non-peptide neurokinin 2 (NK2) receptor antagonist. GR 159897 has little or no affinity for NK1 and NK3 receptors. GR 159897 inhibits binding of [ 3H]GR100679 to human NK2 (hNK2)-CHO cells and rat colon membranes with pKis of 9.51 and 10, respectively. Antagonizes bronchoconstriction. Anxiolytic-like and anti-tumor effects .
|
-
- HY-12143
-
|
GR 205171A
|
Neurokinin Receptor
|
Neurological Disease
|
|
Vofopitant dihydrochloride (GR 205171A) is a blood-brain barrier-permeable NK1 receptor inhibitor with a pKi of 9.02 in mice. Vofopitant dihydrochloride blocks vomiting-related responses and inhibits pseudoptyalism. Vofopitant dihydrochloride exerts anxiolytic effects, regulates 5-HT receptor function and increases central 5-HT release. Vofopitant dihydrochloride improves hyperarousal symptoms of post-traumatic stress disorder. Vofopitant dihydrochloride can be used in research related to depression, anxiety, vomiting and postoperative nausea and vomiting .
|
-
- HY-12142
-
|
GR 205171
|
Neurokinin Receptor
|
Neurological Disease
|
|
Vofopitant (GR 205171A) is a blood-brain barrier-permeable NK1 receptor inhibitor with a pKi of 9.02 in mice. Vofopitant blocks vomiting-related responses and inhibits pseudoptyalism. Vofopitant exerts anxiolytic effects, regulates 5-HT receptor function and increases central 5-HT release. Vofopitant improves hyperarousal symptoms of post-traumatic stress disorder. Vofopitant can be used in research related to depression, anxiety, vomiting and postoperative nausea and vomiting .
|
-
- HY-116268
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
GSK256471 is a non-peptide tachykinin NK3 receptor antagonist with a pKi of 8.9 for the human recombinant NK3 receptor and 8.4 for the guinea pig native receptor. GSK256471 exhibits >100-fold selectivity for NK1 (pKi = 5.2) and NK2 (pKi = 7.3) receptors. GSK256471 noncompetitively inhibits neurokinin B (NKB) (HY-P0242)-induced inositol phosphate accumulation, and this inhibition is irreversible. GSK256471 inhibits wet dog shaking behavior and suppresses dopamine release. GSK256471 could be used to study schizophrenia .
|
-
- HY-W013375
-
|
|
Neprilysin
|
Neurological Disease
|
|
Thiorphan is a selective neprilysin (NEP) inhibitor with an IC50 of 6.9 nM. Thiorphan competitively binds to NEP and blocks its activity, preventing the degradation of neuropeptides such as substance P (SP) and neurokinin NKA. In the field of neonatal brain injury research, Thiorphan can increase the levels of SP and NKA, activate NK1 and NK2 receptors and downstream transduction pathways, and inhibit excessive activation of NMDA receptors. Thus, Thiorphan can protect neocortical neurons from excitotoxic cell death. Thiorphan may also inhibit NEP from enhancing bronchoconstriction and can be used in the study of respiratory diseases .
|
-
- HY-12142S
-
|
rac-GR 205171-d3
|
Isotope-Labeled Compounds
Neurokinin Receptor
|
Neurological Disease
|
|
rac-Vofopitant-d3 (rac-GR 205171-d3) is a racemic form of deuterated Vofopitant (HY-12142). Vofopitant (GR 205171A) is a blood-brain barrier-permeable NK1 receptor inhibitor with a pKi of 9.02 in mice. Vofopitant blocks vomiting-related responses and inhibits pseudoptyalism. Vofopitant exerts anxiolytic effects, regulates 5-HT receptor function and increases central 5-HT release. Vofopitant improves hyperarousal symptoms of post-traumatic stress disorder. Vofopitant can be used in research related to depression, anxiety, vomiting and postoperative nausea and vomiting .
|
-
- HY-18006
-
NKP608
1 Publications Verification
|
Neurokinin Receptor
Wnt
Bcl-2 Family
β-catenin
Cyclin G-associated Kinase (GAK)
VEGFR
Caspase
Cadherin
Apoptosis
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
NKP608 is a non-peptidic derivative of 4-aminopiperidine, a highly selective, orally active, neurokinin-1 (NK1) receptor antagonist with IC50 of 2.6 nM. NKP608 is active both in vitro and in vivo, showing extremely low affinity for NK2, NK3 receptors. NKP608 exerts its effects by blocking the NK₁ receptor, regulate cell proliferation and apoptosis, affect neurotransmitter functions and gastric mucosal repair mechanisms, and suppress the Wnt/β-catenin pathway in antitumor research. NKP608 is applicable to research related to various diseases, including cough, anxiety disorders, depression, gastric mucosal injury, and colorectal cancer .
|
-
- HY-14405B
-
|
(R)-GW679769
|
Neurokinin Receptor
|
Cancer
|
|
(R)-Casopitant ((R)-GW679769) is the isomer of Casopitant (HY-14405). Casopitant is a NK(1)-receptor antagonist. Casopitant can be used for the research of chemotherapy-induced nausea and vomiting .
|
-
- HY-105462
-
-
- HY-P1722
-
|
|
Neurokinin Receptor
|
Inflammation/Immunology
|
|
Spantide II, an undecapeptide substance P (SP) analog, is a potent neurokinin-1 receptor (NK-1R) antagonist. Spantide II binds with NK-1R and blocks proinflammatory activities associated with SP. Spantide II can be used in the research of inflammatory skin disorders, such as psoriasis and contact dermatitis .
|
-
- HY-P3852
-
|
SPR393-407
|
Neurokinin Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
Neurokinin Receptor (393-407), rat (SPR393–407) is a rat neurokinin 1 receptor (NK1R) fragment. NK1R is rapidly internalized by endocytosis and recycled to the plasma membrane when binding to substance P (SP). Neurokinin Receptor (393-407), rat can be used in the research of neurogenic inflammation .
|
-
- HY-19670
-
-
- HY-P3854
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
GR 83074 is a potent and selective NK-2 (Neurokinin Receptor) antagonist with a pKB of 8.23. GR 83074 is inactive as an NK-3 antagonist and exhibits a 340-fold NK-2/NK-1 selectivity .
|
-
- HY-W011978
-
-
- HY-114673
-
|
|
Neurokinin Receptor
|
Others
|
|
Benzomalvin B is the less active analogs of Benzomalvin A. Benzomalvin B is weakly active against substance P .
|
-
- HY-W011978S
-
-
- HY-P0201AF
-
|
|
Fluorescent Dye
Endogenous Metabolite
|
Cancer
|
|
Substance P, FAM-labeled (TFA) is Substance P TFA (HY-P02101A) labeled with FAM fluorophore. Substance P TFA (Neurokinin P TFA) is a neuropeptide that acts as a neurotransmitter and neuromodulator in the central nervous system. The endogenous receptor of Substance P is neurokinin 1 receptor (NK1R) .
|
-
- HY-P0242
-
-
- HY-P0242A
-
-
- HY-B2078A
-
|
|
Neurokinin Receptor
|
Inflammation/Immunology
|
|
Eprazinone dihydrochloride is a gent with mucolytic, secretolytic, antitussive, and bronchial antispasmodic properties. Eprazinone dihydrochloride is a neurokinin 1 receptor (NK1R) ligand. Eprazinone dihydrochloride has the potential for chronic bronchitis treatment that improved pulmonary function and arterial partial pressure of oxygen .
|
-
- HY-P11312
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
[S5K, F6Y, L9mL, M10Mox] neurokinin A (4-10) is a neuropeptide A analog and a peptide fragment of EB1002 (HY-P10746). [S5K, F6Y, L9mL, M10Mox] neurokinin A (4-10) is highly selective for mouse tachykinin receptors and human tachykinin receptor NK1R .
|
-
- HY-109171R
-
|
NT-814 (Standard); BAY3427080 (Standard)
|
Reference Standards
Neurokinin Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
Elinzanetant (Standard) is the analytical standard of Elinzanetant. This product is intended for research and analytical applications. Elizanetant (NT-814) is an orally active, selective NK-1,3 receptor antagonist. Elizanetant can reduce the levels of estradiol and progesterone, and is used in the study of vascular motor symptoms and sleep disorders related to menopause in women .
|
-
- HY-109171S
-
-
- HY-182423
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
RO5328673 is an orally active, blood-brain barrier permeable neurokinin receptor antagonist that effectively targets human NK3 receptors (Ki=0.4 nM, Ka=0.1 nM), human NK2 receptors (Ki=1.1 nM, Ka=0.9 nM), and guinea pig NK3 receptors (Ka=0.1 nM and 0.13 nM). RO5328673 acts as an insurmountable antagonist of NK3 receptors with a slow dissociation rate, while it shows rapid association and dissociation rates at human NK2 receptors. RO5328673 potently inhibits senktide (HY-P0187)-induced enhancement of spontaneous activity in dopaminergic neurons and reverses senktide-induced changes in motor activity of gerbils. RO5328673 is widely applicable to research related to schizophrenia .
|
-
- HY-P2593
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
L-659874 is a selective NK2 receptor antagonist with an IC50 value of 0.49 μM in hamsters. L-659874 inhibits NK2 receptor-mediated hydrolysis of inositol phospholipids. L-659874 could be used for research on the correlation between pain signal transduction and smooth muscle responses. .
|
-
- HY-P3801
-
|
DiMe-C7
|
Neurokinin Receptor
|
Neurological Disease
Metabolic Disease
|
|
[Glp5,(Me)Phe8,Sar9] Substance P (5-11) (DiMe-C7) is a Substance P (HY-P0201) analogue that has approximately the same effects as Substance P (HY-P0201) on neurokinin 1 receptor (NK1R) in rat brain, but with a much longer duration of action. [Glp5,(Me)Phe8,Sar9] Substance P (5-11) selectively activates dopamine metabolism in the mesencephalon and midbrain cortex of the rat brain. [Glp5,(Me)Phe8,Sar9] Substance P (5-11) also increases motor activity and induces recovery of addictive agent-seeking behavior in rats .
|
-
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P0201
-
-
- HY-P0187
-
|
|
Neurokinin Receptor
|
Neurological Disease
Endocrinology
|
|
Senktide is a potent, selective agonist of the neuromedin K3 (NK3) receptor (EC50=0.5-3 nM). Senktide less potently agonizes the NK1 receptor (EC50=35 µM). Senktide is promising for research of neurological disease .
|
-
- HY-P1192
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
GR-73632 is a tachykinin NK1 receptor agonist. GR-73632 activates spinal NK1 receptors to induce scratching, biting and licking behaviors. GR-73632 activates peripheral NK1 receptors to trigger lacrimation in guinea pigs, and activates central NK1 receptors to induce repetitive hind paw tapping behavior in gerbils. GR-73632 is applicable to research related to pruritus .
|
-
- HY-P0061A
-
|
RC-160 acetate; BMY-41606 acetate
|
Neurokinin Receptor
|
Cancer
|
|
Vapreotide acetate (RC-160 acetate; BMY-41606 acetate) is a neurokinin-1 (NK1) receptor antagonist, with an IC50 of 330 nM.
|
-
- HY-P0242
-
-
- HY-P0242A
-
-
- HY-P0061
-
-
- HY-P0201A
-
-
- HY-P1194
-
|
|
Neurokinin Receptor
|
Inflammation/Immunology
|
|
Spantide I, a substance P analog, is a selective NK1 receptor antagonist, with Ki values of 230 nM and 8150 nM for NK1 and NK2 receptor, respectively. Spantide I provides an approach to reduce type 1 and enhance the type 2 cytokine IL-10 in the infected cornea, leading to a significant reduction in corneal perforation .
|
-
- HY-P2546
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
Biotin-Substance P is the biotin tagged Substance P. Substance P (Neurokinin P) is a neuropeptide, acting as a neurotransmitter and as a neuromodulator in the CNS. The endogenous receptor for substance P is neurokinin 1 receptor (NK1-receptor, NK1R) .
|
-
- HY-P1030
-
|
|
Neurokinin Receptor
|
Endocrinology
|
|
Hemokinin 1 (mouse) is a selective agonist of neurokinin-1 receptor, with Ki of 0.175 nM and 560 nM for human NK1 receptor and human NK2 receptor, respectively.
|
-
- HY-P1278
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
GR 64349 is a potent and highly selective NK2 receptor peptide agonist, with an EC50 of 3.7 nM in rat colon. GR 64349 exhibits selectivity >1000 and >300-fold with respect to NK1 and NK3 receptors, respectively .
|
-
- HY-P1012
-
-
- HY-P2000
-
-
- HY-P3092
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
Phyllomedusin, an tachykinin decapeptide, is a NK1 receptor agonist. Phyllomedusin has vasodilating activity and provokes the contraction of the pylorus .
|
-
- HY-P1722
-
|
|
Neurokinin Receptor
|
Inflammation/Immunology
|
|
Spantide II, an undecapeptide substance P (SP) analog, is a potent neurokinin-1 receptor (NK-1R) antagonist. Spantide II binds with NK-1R and blocks proinflammatory activities associated with SP. Spantide II can be used in the research of inflammatory skin disorders, such as psoriasis and contact dermatitis .
|
-
- HY-151413
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
MEN 10207 is a selective NK-2 tachykinin receptor (Neurokinin Receptor) antagonist. MEN 10207 has pA2 values of 5.2, 7.9 and 4.9 in three monoreceptor in vitro assays for NK-1, NK-2 and NK-3 tachykinin receptors, respectively.
|
-
- HY-P0201AF
-
|
|
Fluorescent Dye
Endogenous Metabolite
|
Cancer
|
|
Substance P, FAM-labeled (TFA) is Substance P TFA (HY-P02101A) labeled with FAM fluorophore. Substance P TFA (Neurokinin P TFA) is a neuropeptide that acts as a neurotransmitter and neuromodulator in the central nervous system. The endogenous receptor of Substance P is neurokinin 1 receptor (NK1R) .
|
-
- HY-P3801
-
|
DiMe-C7
|
Neurokinin Receptor
|
Neurological Disease
Metabolic Disease
|
|
[Glp5,(Me)Phe8,Sar9] Substance P (5-11) (DiMe-C7) is a Substance P (HY-P0201) analogue that has approximately the same effects as Substance P (HY-P0201) on neurokinin 1 receptor (NK1R) in rat brain, but with a much longer duration of action. [Glp5,(Me)Phe8,Sar9] Substance P (5-11) selectively activates dopamine metabolism in the mesencephalon and midbrain cortex of the rat brain. [Glp5,(Me)Phe8,Sar9] Substance P (5-11) also increases motor activity and induces recovery of addictive agent-seeking behavior in rats .
|
-
- HY-P1738
-
-
- HY-P3890A
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
Substance P (5-11) TFA TFA, the C-terminal heptapeptide of Substance P (HY-P0201), is a neuropeptide. Substance P (5-11) TFA TFA binds to NK-1 tachykinin receptor .
|
-
- HY-P3854
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
GR 83074 is a potent and selective NK-2 (Neurokinin Receptor) antagonist with a pKB of 8.23. GR 83074 is inactive as an NK-3 antagonist and exhibits a 340-fold NK-2/NK-1 selectivity .
|
-
- HY-P1277
-
-
- HY-P3881
-
-
- HY-P11312
-
|
|
Neurokinin Receptor
|
Neurological Disease
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[S5K, F6Y, L9mL, M10Mox] neurokinin A (4-10) is a neuropeptide A analog and a peptide fragment of EB1002 (HY-P10746). [S5K, F6Y, L9mL, M10Mox] neurokinin A (4-10) is highly selective for mouse tachykinin receptors and human tachykinin receptor NK1R .
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- HY-P1193
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Neurokinin Receptor
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Neurological Disease
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GR 82334 is a potent and specific reversible tachykinin NK1 receptor antagonist . GR 82334 inhibits substance P-induced sensitization by blocking SP NK1 receptors in naked mole-rats .
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- HY-P10599
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Neurokinin Receptor
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Neurological Disease
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Scyliorhinin I is a tachykinin-1 (NK-1) and tachykinin-2 (NK-2) receptor agonist with a Ki value of 0.9 nM for rat submandibular gland NK-1 receptor and 2 nM for hamster bladder NK-2 receptor. Scyliorhinin I has the ability to contract the longitudinal muscles of the guinea pig ileum .
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- HY-P2475
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- HY-P1379
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- HY-P3890
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- HY-P3852
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SPR393-407
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Neurokinin Receptor
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Neurological Disease
Inflammation/Immunology
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Neurokinin Receptor (393-407), rat (SPR393–407) is a rat neurokinin 1 receptor (NK1R) fragment. NK1R is rapidly internalized by endocytosis and recycled to the plasma membrane when binding to substance P (SP). Neurokinin Receptor (393-407), rat can be used in the research of neurogenic inflammation .
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- HY-P3889
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Neurokinin Receptor
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Neurological Disease
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Substance P (6-11) is the C-terminal hexapeptideamide of Substance P (HY-P0201). Substance P (6-11) binds to NK-1 tachykinin receptor. Substance P (6-11) shows depolarization of motoneurons and a hypotensive effect .
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- HY-P1198
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Neurokinin Receptor
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Neurological Disease
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Hemokinin 1, human is a selective tachykinin neurokinin 1 (NK1) receptor full agonist. Hemokinin 1, human is a full agonist at NK2 and NK3 receptor. Hemokinin 1, human can produces an opioid-independent analgesia .
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- HY-P3891
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- HY-P0061B
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RC160 diacetate; BMY 41606 diacetate
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Neurokinin Receptor
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Cancer
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Vapreotide diacetate is a neurokinin-1 (NK1) receptor antagonist, with an IC50 of 330 nM.
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- HY-105436
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- HY-P1194A
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Neurokinin Receptor
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Inflammation/Immunology
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Spantide I TFA, a substance P analog, is a selective NK1 receptor antagonist, with Ki values of 230 nM and 8150 nM for NK1 and NK2 receptor, respectively. Spantide I provides an approach to reduce type 1 and enhance the type 2 cytokine IL-10 in the infected cornea, leading to a significant reduction in corneal perforation .
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- HY-P1194B
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- HY-P1012A
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- HY-P3802
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Neurokinin Receptor
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Neurological Disease
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[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 .
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- HY-P10588
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Neurokinin Receptor
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Others
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WIN 66306 is a cyclic heptapeptide that can be isolated from an Aspergillus species. WIN 66306 is a neurokinin antagonist with antagonistic effects on both NK1 and NK2 receptors .
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- HY-P1277A
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Neurokinin Receptor
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Neurological Disease
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GR 94800 TFA is a potent and selective NK2 receptor peptide antagonist, with pKB values of 9.6, 6.4 and 6.0 for NK2, NK1 and NK3 receptors, respectively .
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- HY-P1278A
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Neurokinin Receptor
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Neurological Disease
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GR 64349 is a potent and highly selective NK2 receptor peptide agonist, with an EC50 of 3.7 nM in rat colon. GR 64349 exhibits selectivity >1000 and >300-fold with respect to NK1 and NK3 receptors, respectively .
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- HY-P1379A
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Neurokinin Receptor
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Neurological Disease
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C14TKL-1 acetate is the acetate salt form of C14TKL-1 (HY-P1379). C14TKL-1 acetate is a tachykinin-like peptide and exhibits an agonistic activity for neurokinin receptor 1 (NK-1) .
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- HY-P1198A
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Neurokinin Receptor
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Neurological Disease
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Hemokinin 1, human TFA is a selective tachykinin neurokinin 1 (NK1) receptor full agonist. Hemokinin 1, human TFA is a full agonist at NK2 and NK3 receptor. Hemokinin 1, human TFA can produces an opioid-independent analgesia .
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- HY-P10619
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- HY-W755425
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Neurokinin Receptor
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Neurological Disease
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Senktide TFA is a potent, selective agonist of the neuromedin K3 (NK3) receptor (EC50=0.5-3 nM). Senktide TFA less potently agonizes the NK1 receptor (EC50=35 µM). Senktide TFA is promising for research of neurological disease .
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- HY-P2139
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Neurokinin Receptor
Phospholipase
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Others
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Ranakinin is a NK1R agonist. Ranakinin inhibits the binding of selective NK1 radioligands to NK1 receptors. Ranakinin activates phospholipase C (Phospholipase C), thereby enhancing polyphosphoinositide hydrolysis. Ranakinin stimulates inositol phosphate production and reduces membrane polyphosphoinositide levels. Ranakinin stimulates corticosterone and aldosterone secretion .
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- HY-P2593
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Neurokinin Receptor
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Neurological Disease
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L-659874 is a selective NK2 receptor antagonist with an IC50 value of 0.49 μM in hamsters. L-659874 inhibits NK2 receptor-mediated hydrolysis of inositol phospholipids. L-659874 could be used for research on the correlation between pain signal transduction and smooth muscle responses. .
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
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- HY-16346S
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Netupitant-d6 is the deuterium labeled Netupitant (CID-6451149), which is a highly potent and selective, orally active neurokinin-1 (NK1) receptor antagonist .
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- HY-10053S
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Maropitant-d3 is the deuterium labeled Maropitant. Maropitant is a selective and orally active neurokinin (NK1) receptor antagonist. Maropitant acts by blocking the binding of substance P within the emetic center and the chemoreceptor trigger zone (CRTZ). Maropitant is highly effective in preventing vomiting .
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- HY-W011978S
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N-Acetyl-L-tryptophan-d3 is the deuterium labeled N-Acetyl-L-tryptophan (HY-W011978). N-Acetyl-L-tryptophan is an antagonist of the neurokinin-1 receptor (NK-1R), disrupting the binding of substance P (SP) to NK-1R. This action provides neuroprotective effects, improving memory deficits and motor impairments. N-Acetyl-L-tryptophan is also an inhibitor of cytochrome c (Cytochrome c), and it exerts antioxidant and anti-inflammatory effects by inhibiting the expression of IL-1β and the activation of caspase-1. N-Acetyl-L-tryptophan holds promise for research in neurodegenerative and inflammatory diseases .
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- HY-10053S1
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Maropitant- 13C,d3 is the 13C- and deuterium labeled Maropitant. Maropitant is a selective and orally active neurokinin (NK1) receptor antagonist. Maropitant acts by blocking the binding of substance P within the emetic center and the chemoreceptor trigger zone (CRTZ). Maropitant is highly effective in preventing vomiting .
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- HY-12142S
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rac-Vofopitant-d3 (rac-GR 205171-d3) is a racemic form of deuterated Vofopitant (HY-12142). Vofopitant (GR 205171A) is a blood-brain barrier-permeable NK1 receptor inhibitor with a pKi of 9.02 in mice. Vofopitant blocks vomiting-related responses and inhibits pseudoptyalism. Vofopitant exerts anxiolytic effects, regulates 5-HT receptor function and increases central 5-HT release. Vofopitant improves hyperarousal symptoms of post-traumatic stress disorder. Vofopitant can be used in research related to depression, anxiety, vomiting and postoperative nausea and vomiting .
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- HY-109171S
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Elinzanetant-d3 (NT-814-d3) is deuterium labeled Elinzanetant. Elizanetant (NT-814) is an orally active, selective NK-1,3 receptor antagonist. Elizanetant can reduce the levels of estradiol and progesterone, and is used in the study of vascular motor symptoms and sleep disorders related to menopause in women .
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| Cat. No. |
Product Name |
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Classification |
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- HY-105346
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Alkynes
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WIN 51708 is a nonpeptide antagonist of neurokinin (NK)-1 receptor. WIN 51708 has a higher affinity for the rat NK-1 receptor compared to the human NK-1 receptor .
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