An NK2 receptor antagonist (pA2 = 8.08 in endothelium-deprived isolated rabbit pulmonary artery); selective for NK2 receptors in isolated rabbit pulmonary artery over NK2 receptors in isolated hamster trachea (pA2 = 5.64) and NK1 receptors in isolated guinea pig ileum (pA2 = 5.66)

MEN10376 – 500 µg

Brand:
Cayman
CAS:
135306-85-3
Storage:
-20
UN-No:
Non-Hazardous - /

MEN10376 is a peptide neurokinin-2 (NK2) receptor antagonist.{41380} It inhibits contractions induced by neurokinin A (NKA) in endothelium-deprived isolated rabbit pulmonary artery (pA2 = 8.08), which is endogenously enriched in NK2 receptors. It is selective for NK2 receptors in isolated rabbit pulmonary artery over NK2 receptors in isolated hamster trachea (pA2 = 5.64 using NKA as an agonist) and NK1 receptors in isolated guinea pig ileum (pA2 = 5.66 using substance P methyl ester as an agonist), tissues that highly express these respective receptors, as well as NK3 receptors in isolated guinea pig cerebral cortex membranes (Ki = >10 μM). In vivo, MEN10376 (1 and 3 μmol/kg) inhibits increases in bladder motility induced by the NK2 receptor agonist [β-Ala8]-NKA(4-10) in anesthetized rats, as well as [β-Ala8]-NKA(4-10)-induced increases in bronchoconstriction in anesthetized guinea pigs.  

 

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SKU: 31142 - 500 µg Category:

Description

An NK2 receptor antagonist (pA2 = 8.08 in endothelium-deprived isolated rabbit pulmonary artery); selective for NK2 receptors in isolated rabbit pulmonary artery over NK2 receptors in isolated hamster trachea (pA2 = 5.64) and NK1 receptors in isolated guinea pig ileum (pA2 = 5.66), tissues that highly express these respective receptors, as well as NK3 receptors in isolated guinea pig cerebral cortex membranes (Ki = >10 μM); inhibits [β-Ala8]-NKA(4-10)-induced increases in bladder motility in anesthetized rats, as well as [β-Ala8]-NKA(4-10)-induced increases in bronchoconstriction in anesthetized guinea pig, at 1 and 3 μmol/kg

Formal name: L-α-aspartyl-L-tyrosyl-D-tryptophyl-L-valyl-D-tryptophyl-D-tryptophyl-L-lysinamide

Synonyms:  Asp-Tyr-Trp-Val-Trp-Trp-Lys-NH2|DYWVWWK-NH2

Molecular weight: 1,081.20

CAS: 135306-85-3

Purity: ≥98%

Formulation: A crystalline solid

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