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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
16 Results for "
human NK3 receptor
" in MedChemExpress (MCE) Product Catalog:
Products (16)
16 Results for "human NK3 receptor" in MCE Product Catalog:
1
1 Cited Publications
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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 .
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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 .
Synonyms: Pronetupitant chloride monohydrochloride
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Fosnetupitant chloride monohydrochloride (Pronetupitant chloride monohydrochloride) is an NK1 antagonist with pKi values of 9.5, 6.1 for human NK1 and NK3 receptor, respectively. Fosnetupitant chloride monohydrochloride is a methylene phosphate prodrug of Netupitant .
Cat. No.: HY-117380
CAS No.: 224961-34-6
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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 .
Cat. No.: HY-137462
CAS No.: 38678-60-3
Synonyms: L-Leucyl-L-phenylalaninamide
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Leucyl-phenylalanine amide (L-Leucyl-L-phenylalaninamide) is a dipeptide analog. Leucyl-phenylalanine amide is a ligand of SP1-7 with a Ki value of 10.2 nM. Leucyl-phenylalanine amide shows no binding activity to human NK-1 or NK-3 receptors .
Cat. No.: HY-P1198
CAS No.: 491851-53-7
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Cat. No.: HY-116958
CAS No.: 226915-43-1
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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 .
Cat. No.: HY-116268
CAS No.: 1133706-08-7
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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 .
Cat. No.: HY-P1198A
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Cat. No.: HY-182423
CAS No.: 1310817-94-7
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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 .
Cat. No.: HY-19633
CAS No.: 191672-52-3
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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.
Cat. No.: HY-121164
CAS No.: 1133705-99-3
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GSK172981 is a brain-penetrant tachykinin NK3 receptor antagonist with pKi values of 7.7 and 7.8 for human and native guinea pig NK3 receptors, respectively. GSK172981 can be used for the study of schizophrenia .
Cat. No.: HY-N9554
CAS No.: 150881-27-9
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Cat. No.: HY-122286
CAS No.: 272104-60-6
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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 .
Cat. No.: HY-101249R
CAS No.: 148451-96-1
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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 .
Cat. No.: HY-184769
CAS No.: 909856-46-8
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NK3R antagonist-2 (Compound 45) is a small-molecule antagonist of tachykinin NK3R, with an IC50 of 1100 nM and a Ki of 1800 nM. NK3R antagonist-2 can be used in the research of schizophrenia .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
