Neurokinin Receptor

Inhibitory Selectivity

Neurokinin Receptor Products

Catalog No. Information Product Use Citations Product Validations
S1189

Aprepitant

Aprepitant (MK-0869, L-754030) 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.

S3038

Fosaprepitant dimeglumine salt

Fosaprepitant is a water-soluble phosphoryl prodrug for Aprepitant which is a NK1 antagonist.

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.

S0772New

L-732138

L-732138 is a selective, potent and competitive antagonist of neurokinin-1 (NK-1) receptor with 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-732133 reduces hyperalgesia and has antitumor activity.

S4654

Netupitant

Netupitant (CID6451149) is a selective neurokinin 1 (NK1) receptor antagonist with potential antiemetic activity.

Catalog No. Information Product Use Citations Product Validations
S1189

Aprepitant

Aprepitant (MK-0869, L-754030) 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.

S3038

Fosaprepitant dimeglumine salt

Fosaprepitant is a water-soluble phosphoryl prodrug for Aprepitant which is a NK1 antagonist.

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.

S0772New

L-732138

L-732138 is a selective, potent and competitive antagonist of neurokinin-1 (NK-1) receptor with 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-732133 reduces hyperalgesia and has antitumor activity.

S4654

Netupitant

Netupitant (CID6451149) is a selective neurokinin 1 (NK1) receptor antagonist with potential antiemetic activity.