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Results for "

NK1/NK2 receptor antagonist

" in MedChemExpress (MCE) Product Catalog:

19

Inhibitors & Agonists

8

Peptides

Cat. No. Product Name Target Research Areas Chemical Structure
  • 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-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-P1194
    Spantide I

    		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 .
    Spantide I
  • HY-120928
    S 16474

    		Neurokinin Receptor Neurological Disease Inflammation/Immunology
    S 16474 is a cyclic peptide with antagonistic effects on NK1 and NK2 receptors. S 16474 can be used in the study of neurogenic inflammation .
    S 16474
  • HY-129296
    YM-44781 free acid

    		Endogenous Metabolite Neurological Disease
    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 .
    YM-44781 free acid
  • HY-P1277
    GR 94800

    		Neurokinin Receptor Neurological Disease
    GR 94800 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 .
    GR 94800
  • HY-P1277A
    GR 94800 TFA

    		Neurokinin Receptor Neurological Disease
    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 .
    GR 94800 TFA
  • HY-118378
    ZD6021

    		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-P10588
    WIN 66306

    		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-116958
    SCH 206272

    		Neurokinin Receptor Inflammation/Immunology
    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 .
    SCH 206272
  • HY-P1194A
    Spantide I TFA

    		Neurokinin Receptor Inflammation/Immunology
    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 .
    Spantide I TFA
  • HY-128537
    DNK-333

    		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-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-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-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-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-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-105462
    MDL 105212A

    		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

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