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neurokinin-1 (NK1) receptor

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48

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-P0201
    Substance P
    Maximum Cited Publications
    31 Publications Verification

    neurokinin P

    Neurokinin Receptor Endogenous Metabolite Infection Neurological Disease Metabolic Disease Cancer
    Substance P (Neurokinin P) is a CNS-penetrant 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).
    Substance P
  • HY-16346
    Netupitant
    4 Publications Verification

    CID 6451149

    Neurokinin Receptor Neurological Disease Endocrinology Cancer
    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 .
    Netupitant
  • HY-14751

    SCH619734

    Neurokinin Receptor Neurological Disease
    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 .
    Rolapitant
  • HY-W011978

    Endogenous Metabolite Mitochondrial Metabolism Neurokinin Receptor Caspase Interleukin Related Neurological Disease Inflammation/Immunology
    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 .
    N-Acetyl-L-tryptophan
  • HY-101249

    Neurokinin Receptor Neurological Disease Cancer
    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 .
    L-732138
  • HY-P0061A
    Vapreotide acetate
    1 Publications Verification

    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.
    Vapreotide acetate
  • HY-16436

    SCH619734 hydrochloride hydrate

    Neurokinin Receptor Neurological Disease Cancer
    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 .
    Rolapitant hydrochloride hydrate
  • HY-14406A
    L-733060 hydrochloride
    1 Publications Verification

    Neurokinin Receptor Neurological Disease Cancer
    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 .
    L-733060 hydrochloride
  • HY-P0061
    Vapreotide
    1 Publications Verification

    RC160; BMY 41606

    Neurokinin Receptor Cancer
    Vapreotide is a neurokinin-1 (NK1) receptor antagonist, with an IC50 of 330 nM.
    Vapreotide
  • 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.
    Hemokinin 1 (mouse)
  • HY-122347A

    GW823296 maleate

    Neurokinin Receptor Neurological Disease Inflammation/Immunology
    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 .
    Orvepitant maleate
  • 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 .
    Eprazinone dihydrochloride
  • HY-P0201A
    Substance P TFA
    Maximum Cited Publications
    31 Publications Verification

    neurokinin P TFA

    Neurokinin Receptor Endogenous Metabolite Neurological Disease Metabolic Disease Cancer
    Substance P TFA (Neurokinin P TFA) is a CNS-penetrant 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) .
    Substance P TFA
  • 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) .
    Biotin-Substance P
  • 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) .
    Casopitant mesylate
  • HY-P1722
    Spantide II
    1 Publications Verification

    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 .
    Spantide II
  • 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 .
    Vofopitant dihydrochloride
  • 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 .
    NKP608
  • HY-16346S

    CID-6451149-d6

    Neurokinin Receptor Neurological Disease Endocrinology
    Netupitant-d6 is the deuterium labeled Netupitant (CID-6451149), which is a highly potent and selective, orally active neurokinin-1 (NK1) receptor antagonist .
    Netupitant-d6
  • 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) .
    Substance P, FAM-labeled TFA
  • 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 .
    [Glp5,(Me)Phe8,Sar9] Substance P (5-11)
  • HY-19665

    LY303870

    Neurokinin Receptor Neurological Disease Inflammation/Immunology
    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 .
    Lanepitant
  • HY-12114

    VPD-737; MK-0594

    Neurokinin Receptor Neurological Disease Endocrinology
    Serlopitant is a selective Neurokinin-1 (NK-1) receptor antagonist.
    Serlopitant
  • HY-178269

    Drug Metabolite Neurokinin Receptor Neurological Disease
    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 .
    SCH-720881
  • 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 .
    Neurokinin Receptor (393-407), rat
  • 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 .
    CJ-17493
  • HY-14406

    Neurokinin Receptor Neurological Disease Cancer
    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 .
    L-733060
  • HY-P0061B

    RC160 diacetate; BMY 41606 diacetate

    Neurokinin Receptor Cancer
    Vapreotide diacetate is a neurokinin-1 (NK1) receptor antagonist, with an IC50 of 330 nM.
    Vapreotide diacetate
  • HY-P0255

    Neurokinin Receptor Neurological Disease Endocrinology
    Physalaemin, a non-mammalian tachykinin, binds selectively to neurokinin-1 (NK1) receptor with high affinity.
    Physalaemin
  • HY-P1198

    Neurokinin Receptor Neurological Disease
    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 .
    Hemokinin 1, human
  • HY-W011978S

    Isotope-Labeled Compounds Endogenous Metabolite Mitochondrial Metabolism Neurokinin Receptor Caspase Interleukin Related Neurological Disease Inflammation/Immunology
    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 .
    N-Acetyl-L-tryptophan-d3
  • HY-122347

    GW823296

    Neurokinin Receptor Neurological Disease Cancer
    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 .
    Orvepitant
  • 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 .
    CP-99994
  • HY-119552

    LL-S490β

    Endogenous Metabolite Neurokinin Receptor Neurological Disease
    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 .
    Acetylaszonalenin
  • HY-106982

    CJ-11,974

    Neurokinin Receptor Neurological Disease Metabolic Disease
    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 .
    Ezlopitant
  • HY-172514

    Neurokinin Receptor Cancer
    (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 .
    (1R,2S,3R)-Aprepitant
  • 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 .
    Netupitant (Standard)
  • 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.
    Benzomalvin C
  • HY-159842

    Neurokinin Receptor Neurological Disease
    Fosrolapitant is a neurokinin 1 (NK1) receptor antagonist .
    Fosrolapitant
  • HY-P1198A

    Neurokinin Receptor Neurological Disease
    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 .
    Hemokinin 1, human TFA
  • HY-118378

    Neurokinin Receptor Neurological Disease Endocrinology
    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 .
    ZD6021
  • HY-14751A

    SCH619734 hydrochloride

    Neurokinin Receptor Neurological Disease Cancer
    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 .
    Rolapitant hydrochloride
  • 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 .
    CP-99994 hydrochloride
  • 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 .
    Rolapitant (Standard)
  • 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) .
    Casopitant
  • HY-101249R

    Neurokinin Receptor Reference Standards Neurological Disease Cancer
    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 .
    L-732138 (Standard)
  • 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 .
    R116031
  • HY-19203

    Neurokinin Receptor Neurological Disease
    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 .
    CGP-49823

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