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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 .
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 .
Vofopitant dihydrochloride (GR 205171A) is a potent, selective and orally available tachykinin neurokinin 1(NK1) receptor antagonist, inhibits [ 3H]SP binding to the NK1 receptor with pKi values of 9.5 and 10.6 in rat and human membranes respectively, acts as a potential broad-spectrum anti-emetic agent .
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 .
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 .
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 .
Fosnetupitant (Pronetupitant) a methylene phosphate proagent of Netupitant. Fosnetupitant (Pronetupitant) exhibits a pKi of 9.5 for humanNK1 receptor .
rac-Vofopitant-d3 (rac-GR 205171-d3)is the deuterium labeledVofopitant(HY-12142) . Vofopitant is potent tachykinin NK1 receptor antagonist, with pKis of 10.6, 9.5, and 9.8 for human, rat and ferret NK1 receptor, respectively .
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.
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 .
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 .
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 .
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 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.
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.
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 .
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.
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 .
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.
rac-Vofopitant-d3 (rac-GR 205171-d3)is the deuterium labeledVofopitant(HY-12142) . Vofopitant is potent tachykinin NK1 receptor antagonist, with pKis of 10.6, 9.5, and 9.8 for human, rat and ferret NK1 receptor, respectively .
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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