Neurokinin Receptor
Inhibitory Selectivity
Isoform-specific Inhibitors
Neurokinin Receptor Products
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S1189 |
Aprepitant (MK-0869)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. |
HepT1, HepG2, and HuH6 cells were treated with increasing doses of aprepitant or SP [100 nM] and Western blot analysis was performed for the apoptotic markers PARP, Caspase-3, and BID. |
|
| S3038 |
Fosaprepitant dimeglumine saltFosaprepitant dimeglumine salt (MK-0517) is a water-soluble phosphoryl prodrug for Aprepitant which is a NK1 antagonist. |
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| S5476 |
RolapitantRolapitant (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. |
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| S0772 |
L-732138L-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. |
||
| S4654 |
NetupitantNetupitant (CID6451149) is a selective neurokinin 1 (NK1) receptor antagonist with potential antiemetic activity. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S1189 |
Aprepitant (MK-0869)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. |
HepT1, HepG2, and HuH6 cells were treated with increasing doses of aprepitant or SP [100 nM] and Western blot analysis was performed for the apoptotic markers PARP, Caspase-3, and BID. |
|
| S3038 |
Fosaprepitant dimeglumine saltFosaprepitant dimeglumine salt (MK-0517) is a water-soluble phosphoryl prodrug for Aprepitant which is a NK1 antagonist. |
||
| S5476 |
RolapitantRolapitant (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. |
||
| S0772 |
L-732138L-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. |
||
| S4654 |
NetupitantNetupitant (CID6451149) is a selective neurokinin 1 (NK1) receptor antagonist with potential antiemetic activity. |
