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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 humanNK-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 .
Hemokinin 1 (mouse) is a selective agonist of neurokinin-1 receptor, with Ki of 0.175 nM and 560 nM for humanNK1 receptor and human NK2 receptor, respectively.
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 .
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 .
Fosnetupitant chloride monohydrochloride (Pronetupitant chloride monohydrochloride) is an NK1 antagonist with pKi values of 9.5, 6.1 for humanNK1 and NK3 receptor, respectively. Fosnetupitant chloride monohydrochloride is a methylene phosphate prodrug of Netupitant .
Fosnetupitant (Pronetupitant) a methylene phosphate proagent of Netupitant. Fosnetupitant (Pronetupitant) exhibits a pKi of 9.5 for humanNK1 receptor .
[S5K, F6Y, L9mL, M10Mox] neurokinin A (4-10) is a neuropeptide A analog and a peptide fragment of EB1002 (HY-P10746). [S5K, F6Y, L9mL, M10Mox] neurokinin A (4-10) is highly selective for mouse tachykinin receptors and human tachykinin receptor NK1R .
SDZ NKT 343 is a selective, orally active NK1 receptor antagonist with an IC50 of 0.62 nM against humanNK1 receptor. SDZ NKT 343 has good analgesic activity .
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 humanNK-1 receptor .
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 humanNK-1 or NK-3 receptors .
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 .
WIN 62,577 is a rat-specific, but non-human, NK1 receptor antagonist. WIN 62,577 interacts with M1-M4 mAChRs and is an allosteric enhancer of acetylcholine affinity targeting the M3 receptor.
RO4583298 is a potent, orally active dual antagonist of NK1 (human and gerbil)/NK3 (human, cynomolgus monkey, gerbil and guinea-pig). RO4583298 inhibits senktide-induced potentiation of spontaneous activity of dopaminergic neurons. RO4583298 can block gerbil foot tapping response and inhibits mouse tail whips .
L-760735 is a high affinity, selective and orally active NK1 receptor antagonist with an IC50 of 0.19 nM for humanNK1 receptors. L-760735 exhibits anxiolytic and antidepressant-like effects .
CP 122721 hydrochloride is a potent, non-peptide and selective nonpeptide neurokinin NK1 antagonist, with a pIC50 of 9.8 for humanNK1 receptor expressed in IM-9 cells. CP 122721 hydrochloride exhibits anxiolytic and antidepressant-like effects .
Vestipitant (GW597599) mesylate is a selective, orally active, and blood-brain barrier penetrant NK1 receptor antagonist. Vestipitant mesylate exhibits high affinity for the humanNK1 receptor (pKi: 9.65). Vestipitant mesylate can be used in the research of diseases such as depression, anxiety disorders, and nausea and vomiting .
Dapitant (RPR 100893) is a non-peptide Substance P antagonist with high affinity for the humanNK1 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 .
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 .
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 .
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 .
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 .
(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 .
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 .
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 .
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 .
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.
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 .
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 humanNK-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 .
R116031 is a selective Neurokinin-1 (NK-1) receptor antagonist with a Ki of 0.45 nM for humanNK-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 .
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 .
Hemokinin 1 (mouse) is a selective agonist of neurokinin-1 receptor, with Ki of 0.175 nM and 560 nM for humanNK1 receptor and human NK2 receptor, respectively.
[S5K, F6Y, L9mL, M10Mox] neurokinin A (4-10) is a neuropeptide A analog and a peptide fragment of EB1002 (HY-P10746). [S5K, F6Y, L9mL, M10Mox] neurokinin A (4-10) is highly selective for mouse tachykinin receptors and human tachykinin receptor NK1R .
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 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 .
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 .
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 .
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 .
The CD160 protein is found on immune cells and acts as a receptor that transmits stimulatory or inhibitory signals, complexly regulating cell activation and differentiation. It exists in a GPI-anchored and transmembrane form and may initiate different signaling pathways in NK cells and T cells. CD160 Protein, Human (HEK293, His-Avi) is the recombinant human-derived CD160 protein, expressed by HEK293 , with C-Avi, C-His labeled tag.
B3GAT1 Protein is pivotal in L2/HNK-1 carbohydrate epitope biosynthesis on glycoproteins and glycosaminoglycan biosynthesis.Catalyzing substrates like ASOR and asialo-fetuin, its enzymatic function depends on sphingomyelin presence, with stearoyl-sphingomyelin being the most effective.Notably, it exclusively acts on saturated fatty acids in sphingomyelin, showing no reactivity with unsaturated fatty acids, regardless of acyl group length.B3GAT1 Protein, Human (HEK293, His) is the recombinant human-derived B3GAT1 protein, expressed by HEK293 , with N-6*His labeled tag.
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 humanNK-1 receptor .
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Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
MedchemExpress Validation 03
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
MedchemExpress Validation 04
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
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