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Neurokinin Receptor

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Neurokinin Receptor製品

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  • Neurokinin Receptor拮抗剤(8)
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S1189 Aprepitant Aprepitant is a potent and selective neurokinin-1 receptor antagonist with IC50 of 0.1 nM. Aprepitant reduces levels of pro-inflammatory cytokines including G-CSF, IL-6, IL-8 and TNFα. Aprepitant inhibits HIV infection of human macrophages.
Br J Cancer, 2024, 10.1038/s41416-024-02608-8
Inflammation, 2023, 46(1):256-269
Nat Commun, 2022, 13(1):4995
S4654 Netupitant Netupitant (CID6451149) is a selective neurokinin 1 (NK1) receptor antagonist with potential antiemetic activity.
Nat Commun, 2019, 10(1):17
S3038 Fosaprepitant dimeglumine salt Fosaprepitant dimeglumine salt (MK-0517) is a water-soluble phosphoryl prodrug for Aprepitant which is a NK1 antagonist.
Nat Cell Biol, 2024,
J Immunother Cancer, 2024, 12(11)e009805
E4624New Tradipitant Tradipitant(VLY-686, LY686017) is the 2nd generation antagonist of neurokinin-1 (NK-1). It exhibits potential for treating chemotherapy-induced nausea, depression, alcoholism, social anxiety disorder, and for developing imaging ligands.
S5476 Rolapitant Rolapitant (SCH-619734) is a selective and competitive antagonist of human substance P/NK1 receptors with antiemetic activity. It has a high affinity for the human NK1 receptor of 0.66 nM and high selectivity over the human NK2 and NK3 subtypes of >1000-fold, as well as preferential affinity for human, guinea pig, gerbil and monkey NK1 receptors over rat, mouse and rabbit.
Cell Commun Signal, 2024, 22(1):195
S0772 L-732138 L-732138 (L-732,138) is a selective, potent and competitive antagonist of neurokinin-1 (NK-1) receptor/substance P (SP) receptor. L-732138 inhibits the binding of 125I-SP to the human NK-1 receptor stably expressed in CHO cells with IC50 of 2.3 nM.
E4853New Rolapitant hydrochloride hydrate Rolapitant hydrochloride hydrate(SCH619734 hydrochloride hydrate) is a long-acting, extremely selective antagonist of the Nk-1 receptor antagonist (NK-1RA) with antiemetic activity. It significantly penetrates the central nervous system (CNS) and used clinically to prevent chemotherapy-induced nausea and vomiting (CINV) in cancer patients undergoing high and moderate emetogenic chemotherapy.
E0192 Maropitant citrate Maropitant citrate is a novel neurokinin type-1 (NK1) receptor antagonist with anti-inflammatory and analgesic properties.
S1189 Aprepitant Aprepitant is a potent and selective neurokinin-1 receptor antagonist with IC50 of 0.1 nM. Aprepitant reduces levels of pro-inflammatory cytokines including G-CSF, IL-6, IL-8 and TNFα. Aprepitant inhibits HIV infection of human macrophages.
Br J Cancer, 2024, 10.1038/s41416-024-02608-8
Inflammation, 2023, 46(1):256-269
Nat Commun, 2022, 13(1):4995
S4654 Netupitant Netupitant (CID6451149) is a selective neurokinin 1 (NK1) receptor antagonist with potential antiemetic activity.
Nat Commun, 2019, 10(1):17
S3038 Fosaprepitant dimeglumine salt Fosaprepitant dimeglumine salt (MK-0517) is a water-soluble phosphoryl prodrug for Aprepitant which is a NK1 antagonist.
Nat Cell Biol, 2024,
J Immunother Cancer, 2024, 12(11)e009805
E4624New Tradipitant Tradipitant(VLY-686, LY686017) is the 2nd generation antagonist of neurokinin-1 (NK-1). It exhibits potential for treating chemotherapy-induced nausea, depression, alcoholism, social anxiety disorder, and for developing imaging ligands.
S5476 Rolapitant Rolapitant (SCH-619734) is a selective and competitive antagonist of human substance P/NK1 receptors with antiemetic activity. It has a high affinity for the human NK1 receptor of 0.66 nM and high selectivity over the human NK2 and NK3 subtypes of >1000-fold, as well as preferential affinity for human, guinea pig, gerbil and monkey NK1 receptors over rat, mouse and rabbit.
Cell Commun Signal, 2024, 22(1):195
S0772 L-732138 L-732138 (L-732,138) is a selective, potent and competitive antagonist of neurokinin-1 (NK-1) receptor/substance P (SP) receptor. L-732138 inhibits the binding of 125I-SP to the human NK-1 receptor stably expressed in CHO cells with IC50 of 2.3 nM.
E4853New Rolapitant hydrochloride hydrate Rolapitant hydrochloride hydrate(SCH619734 hydrochloride hydrate) is a long-acting, extremely selective antagonist of the Nk-1 receptor antagonist (NK-1RA) with antiemetic activity. It significantly penetrates the central nervous system (CNS) and used clinically to prevent chemotherapy-induced nausea and vomiting (CINV) in cancer patients undergoing high and moderate emetogenic chemotherapy.
E0192 Maropitant citrate Maropitant citrate is a novel neurokinin type-1 (NK1) receptor antagonist with anti-inflammatory and analgesic properties.
E4624New Tradipitant Tradipitant(VLY-686, LY686017) is the 2nd generation antagonist of neurokinin-1 (NK-1). It exhibits potential for treating chemotherapy-induced nausea, depression, alcoholism, social anxiety disorder, and for developing imaging ligands.
E4853New Rolapitant hydrochloride hydrate Rolapitant hydrochloride hydrate(SCH619734 hydrochloride hydrate) is a long-acting, extremely selective antagonist of the Nk-1 receptor antagonist (NK-1RA) with antiemetic activity. It significantly penetrates the central nervous system (CNS) and used clinically to prevent chemotherapy-induced nausea and vomiting (CINV) in cancer patients undergoing high and moderate emetogenic chemotherapy.

Neurokinin Receptor阻害剤の選択性比較

Tags: Neurokinin Receptor inhibitor|Neurokinin Receptor agonist|Neurokinin Receptor activator|Neurokinin Receptor inducer|Neurokinin Receptor antagonist|Neurokinin Receptor signaling pathway|Neurokinin Receptor assay kit