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neurokinin-1 receptor antagonist

" in MedChemExpress (MCE) Product Catalog:

49

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4

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4

Isotope-Labeled Compounds

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-10052
    Aprepitant
    Maximum Cited Publications
    13 Publications Verification

    MK-0869; MK-869; L-754030

    Neurokinin Receptor Bacterial HIV Antibiotic Neurological Disease Endocrinology Cancer
    Aprepitant (MK-0869) is a selective and high-affinity neurokinin 1 receptor antagonist with a Kd of 86 pM.
    Aprepitant
  • 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-14407A
    Fosaprepitant dimeglumine
    3 Publications Verification

    MK-0517; L785298

    Neurokinin Receptor Neurological Disease Endocrinology Cancer
    Fosaprepitant dimeglumine (MK-0517) is a proagent of Aprepitant (HY-10052). Fosaprepitant dimeglumine is a neurokinin-1 receptor antagonist, which is development for the prevention of chemotherapy-induced nausea and vomiting (CINV) .
    Fosaprepitant dimeglumine
  • 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-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-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-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-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-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-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-14407

    L-758298

    Neurokinin Receptor Neurological Disease Endocrinology Cancer
    Fosaprepitant (L-785298) is a proagent of Aprepitant (HY-10052). Fosaprepitant is a neurokinin-1 receptor antagonist, which is development for the prevention of chemotherapy-induced nausea and vomiting (CINV) .
    Fosaprepitant
  • HY-10052R

    MK-0869 (Standard); MK-869 (Standard); L-754030 (Standard)

    Reference Standards Neurokinin Receptor Bacterial HIV Antibiotic Neurological Disease Endocrinology Cancer
    Aprepitant (Standard) is the analytical standard of Aprepitant. This product is intended for research and analytical applications. Aprepitant (MK-0869) is a selective and high-affinity neurokinin 1 receptor antagonist with a Kd of 86 pM.
    Aprepitant (Standard)
  • 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-19429A

    Neurokinin Receptor Neurological Disease
    SLV-317 is an antagonist of the neurokinin-1 receptor with oral activity. SLV-317 can effective antagonist of substance P-induced effects .
    SLV-317
  • HY-19429

    Neurokinin Receptor Metabolic Disease
    SLV-317 (free base) is an antagonist of the neurokinin-1 receptor with oral activity. SLV-317 (free base) can effective antagonist of substance P-induced effects .
    SLV-317 free base
  • HY-14407AS

    MK-0517-d4; L785298-d4

    Isotope-Labeled Compounds Neurokinin Receptor Neurological Disease Endocrinology Cancer
    Fosaprepitant-d4 (dimeglumine) is deuterium labeled Fosaprepitant (dimeglumine). Fosaprepitant dimeglumine (MK-0517) is a proagent of Aprepitant (HY-10052). Fosaprepitant dimeglumine is a neurokinin-1 receptor antagonist, which is development for the prevention of chemotherapy-induced nausea and vomiting (CINV) .
    Fosaprepitant-d4 dimeglumine
  • HY-14407AR

    MK-0517 (Standard); L785298 (Standard)

    Reference Standards Neurokinin Receptor Neurological Disease Endocrinology Cancer
    Fosaprepitant (dimeglumine) (Standard) is the analytical standard of Fosaprepitant (dimeglumine). This product is intended for research and analytical applications. Fosaprepitant dimeglumine (MK-0517) is a proagent of Aprepitant (HY-10052). Fosaprepitant dimeglumine is a neurokinin-1 receptor antagonist, which is development for the prevention of chemotherapy-induced nausea and vomiting (CINV) .
    Fosaprepitant dimeglumine (Standard)
  • 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-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-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-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-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-105137

    LY303870 dihydrochloride

    Neurokinin Receptor Neurological Disease Inflammation/Immunology
    Lanepitant dihydrochloride (LY303870 dihydrochloride) is a non-peptide neurokinin-1 receptor antagonist. Lanepitant dihydrochloride has analgesic and anti-inflammatory activities .
    Lanepitant dihydrochloride
  • 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-105534

    Neurokinin Receptor Neurological Disease
    TAK-637 is an orally active neurokinin-1 receptor antagonist. TAK-637 increases bladder storage capacity. TAK-637 can be used for research of functional bowel diseases such as irritable bowel syndrome .
    TAK-637
  • 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-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-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-12140

    GW597599

    Neurokinin Receptor Neurological Disease
    Vestipitant (GW597599) is a neurokinin-1 receptor antagonist (pKi: 9.4, hNK1) with hypnotic effects and the ability to suppress primary insomnia. Vestipitant can effectively block substance P-mediated extracellular regulated kinase phosphorylation and relieve anxiety and possible depression induced by the agonist GR73632 (HY-P1192) in gerbils. Vestipitant can also improve functional dyspnea, anxiety, insomnia, irritable bowel disease, gastroesophageal reflux disease, tinnitus and antiemetic effects .
    Vestipitant
  • HY-159842

    Neurokinin Receptor Neurological Disease
    Fosrolapitant is a neurokinin 1 (NK1) receptor antagonist .
    Fosrolapitant
  • 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-W777166

    MK-0869--13C2,d2; MK-869-13C2,d2; L-754030--13C2,d2

    Isotope-Labeled Compounds HIV Antibiotic Neurokinin Receptor Bacterial Neurological Disease Endocrinology Cancer
    Aprepitant- 13C2,d2 (Major) (MK-0869- 13C2,d2) is 13C labeled Aprepitant. Aprepitant (MK-0869) is a selective and high-affinity neurokinin 1 receptor antagonist with a Kd of 86 pM.
    Aprepitant-13C2,d2 (Major)
  • 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-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-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-19633A

    Endogenous Metabolite Neurological Disease
    CS-003 is a triple neurokinin receptor antagonist with activity in inhibiting neurokinin-related respiratory diseases. CS-003 exhibits high affinity for human neurokinin 1, 2 and 3 receptors, withKi values of 2.3 nM, 0.54 nM and 0.74 nM respectively. The Ki values of CS-003 on the guinea pig neurokinin receptor are 5.2 nM, 0.47 nM and 0.71 nM respectively, showing superior inhibitory effect. CS-003 significantly inhibits the formation of inositol phosphate involving substance P, neurokinin A and neurokinin B through competitive antagonism. CS-003 significantly inhibits citric acid-induced cough, and its effect is better than other selective neurokinin receptor antagonists .
    CS-003
  • 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-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-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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