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Results for "

NK3 neurokinin receptors

" in MedChemExpress (MCE) Product Catalog:

26

Inhibitors & Agonists

8

Peptides

1

Natural
Products

1

Isotope-Labeled Compounds

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-19632
    Fezolinetant
    5 Publications Verification

    ESN-364

    		 Neurokinin Receptor Endocrinology
    Fezolinetant is an antagonist of the neurokinin 3 receptor (NK3R), used for the treatment of menopausal hot flushes.
    Fezolinetant
  • HY-14432
    Pavinetant
    3 Publications Verification

    MLE-4901; AZD2624; AZD4901

    		 Neurokinin Receptor Neurological Disease Endocrinology
    Pavinetant (MLE-4901) is a neurokinin-3 receptor (NK3R) antagonist.
    Pavinetant
  • HY-101249
    L-732138

    		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-P0242
    Neurokinin B

    		Neurokinin Receptor Neurological Disease Endocrinology
    Neurokinin B belongs to the tachykinin family of peptides. Neurokinin B binds a family of GPCRs-including neurokinin receptor 1 (NK1R), NK2R, and NK3R-to mediate their biological effect .
    Neurokinin B
  • HY-P0242A
    Neurokinin B TFA

    		Neurokinin Receptor Neurological Disease Endocrinology
    Neurokinin B TFA belongs to the tachykinin family of peptides. Neurokinin B binds a family of GPCRs-including neurokinin receptor 1 (NK1R), NK2R, and NK3R-to mediate their biological effect .
    Neurokinin B TFA
  • HY-107691
    GR 159897

    		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-117380
    SB 235375

    		Neurokinin Receptor Neurological Disease
    SB 235375 is a potent and selective antagonist of the human neurokinin-3 (hNK-3) receptor designed by optimizing the structure of 2-phenyl-4-quinolinecarboxylic acid amide. SB 235375 displays high affinity for the hNK-3 receptor, with significantly higher binding affinities than hNK-2 and hNK-1 receptors. In vitro studies demonstrated its ability to block NK-3 receptor-mediated contraction and calcium mobilization, while in vivo, SB 223412 demonstrated oral and intravenous activity against NK-3 receptor-driven responses in animal models .
    SB 235375
  • 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-P3862
    [MePhe7]-Neurokinin B

    		Neurokinin Receptor Neurological Disease Endocrinology
    [MePhe7]-Neurokinin B is an neurokinin NK-3 receptor (NK3R) agonist with an IC50 value of 3 nM. [MePhe7]-Neurokinin B is a potential regulator of pulsatile gonadotropin-releasing hormone (GnRH) secretion via activation of the neurokinin-3 receptor (NK3R) .
    [MePhe7]-Neurokinin B
  • HY-P3854
    GR 83074

    		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-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-116822
    SSR 146977

    		Neurokinin Receptor Neurological Disease
    SSR 146977 is a potent and selective antagonist of the tachykinin NK3 receptor. SSR 146977 inhibits the binding of radioactive neurokinin B to NK3 receptors in Chinese hamster ovary cells, with a Ki of 0.26 nM .
    SSR 146977
  • HY-P1198
    Hemokinin 1, human

    		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-P3802
    [D-Trp2,7,9] Substance P

    		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-P1198A
    Hemokinin 1, human TFA

    		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-116268
    GSK256471

    		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 .
    GSK256471
  • HY-19633
    CS-003 Free base

    		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-120167
    YM-44778

    		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 .
    YM-44778
  • HY-182423
    RO5328673

    		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 .
    RO5328673
  • HY-N9554
    WIN-64821

    		Neurokinin Receptor Endogenous Metabolite Calcium Channel 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 .
    WIN-64821
  • HY-14432R
    Pavinetant (Standard)

    MLE-4901 (Standard); AZD2624 (Standard); AZD4901 (Standard)

    		 Neurokinin Receptor Reference Standards Neurological Disease Endocrinology
    Pavinetant (Standard) is the analytical standard of Pavinetant. This product is intended for research and analytical applications. Pavinetant (MLE-4901) is a neurokinin-3 receptor (NK3R) antagonist.
    Pavinetant (Standard)
  • HY-149358
    NK3R-IN-1

    		Neurokinin Receptor Endocrinology
    NK3R-IN-1 (compound 16x), a imidazolepiperazine derivative, is an orally active Neurokinin Receptor NK3R inhibitor. NK3R-IN-1 decreases blood luteinizing hormone levels in ovariectomy (OVX) model .
    NK3R-IN-1
  • HY-122286
    SB 414240

    		Neurokinin Receptor Neurological Disease
    SB 414240 is a selective neurokinin-2 receptor (NK-2R) antagonist with Kis of 1 nM and 193 nM for human NK-3R and human NK-2R, respectively. SB 414240 does not bind the human μ-opioid receptor (hMOR). SB 414240 can be used for the study of neurological disease .
    SB 414240
  • HY-101249R
    L-732138 (Standard)

    		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-181682
    NK3R antagonist-1

    		Neurokinin Receptor Endocrinology
    NK3R antagonist-1 is an orally active neurokinin-3 receptor (NK3R) antagonist with an IC50 of 53.61 nM. NK3R antagonist-1 reduces plasma luteinizing hormone (LH) levels in ovariectomized rat models. NK3R antagonist-1 is applicable to research related to menopausal hot flushes .
    NK3R antagonist-1
  • HY-19632S
    Fezolinetant-d4

    ESN-364-d4

    		 Isotope-Labeled Compounds Neurokinin Receptor Metabolic Disease
    Fezolinetant-d4 (ESN-364-d4) is the deuterium labeled Fezolinetant (HY-19632). Fezolinetant is an antagonist of the neurokinin 3 receptor (NK3R), used for the treatment of menopausal hot flushes.
    Fezolinetant-d4

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