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neurokinin NK1 receptor antagonist

" in MedChemExpress (MCE) Product Catalog:

60

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Cat. No. 상품명 Target 연구분야 Chemical Structure
  • 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-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-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-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-108483

    Neurokinin Receptor Neurological Disease Inflammation/Immunology
    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 .
    RP 67580
  • 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-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 .
    GR 159897
  • 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-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-151413
    MEN 10207
    1 Publications Verification

    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.
    MEN 10207
  • 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-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 .
    GR 83074
  • HY-109147A

    Neurokinin Receptor Neurological Disease
    Imnopitant dihydrochloride is a neurokinin NK1 receptor antagonist .
    Imnopitant dihydrochloride
  • 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-12114

    VPD-737; MK-0594

    Neurokinin Receptor Neurological Disease Endocrinology
    Serlopitant is a selective Neurokinin-1 (NK-1) receptor antagonist.
    Serlopitant
  • 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-128537

    Neurokinin Receptor Inflammation/Immunology
    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 .
    DNK-333
  • 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-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 .
    Maropitant-d3
  • 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-105346

    Neurokinin Receptor Neurological Disease
    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 .
    WIN 51708
  • 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-159842

    Neurokinin Receptor Neurological Disease
    Fosrolapitant is a neurokinin 1 (NK1) receptor antagonist .
    Fosrolapitant
  • HY-105436

    Neurokinin Receptor Neurological Disease
    FR 113680 is a tripeptide substance P antagonist that interacts selectively with the NK1 neurokinin receptor .
    FR 113680
  • HY-10049A

    Neurokinin Receptor Neurological Disease
    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 .
    CP 122721 hydrochloride
  • 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-P10588

    Neurokinin Receptor Others
    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 .
    WIN 66306
  • HY-105462

    Neurokinin Receptor Neurological Disease Inflammation/Immunology
    MDL 105212A is a potent and orally active nonpeptide neurokinin receptor (NK-1/NK-2) tachykinin receptor antagonist. MDL 105212A can be used for the researches of inflammation, immunology and neurological disease, such as asthma .
    MDL 105212A
  • HY-118463

    (-)-Benzomalvin A

    Neurokinin Receptor Neurological Disease
    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 .
    Benzomalvin A
  • HY-17012

    RPR 100893

    Neurokinin Receptor Inflammation/Immunology
    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 .
    Dapitant
  • 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-P3802

    Neurokinin Receptor Neurological Disease
    [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 .
    [D-Trp2,7,9] Substance P
  • 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-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-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-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.
    CS-003 Free base
  • 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 .
    Maropitant (Standard)
  • 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 .
    L 743310
  • 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 .
    Maropitant-13C,d3
  • 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-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

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