An NK2 receptor antagonist
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MEN10207 (acetate)

Item No. 43055

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
L-α-aspartyl-L-tyrosyl-D-tryptophyl-L-valyl-D-tryptophyl-D-tryptophyl-L-argininamide, acetate
Synonyms
  • Asp-Tyr-D-Trp-Val-D-Trp-D-Trp-Arg-NH2
  • [Tyr5,D-Trp6,8,9,Arg10]-Neurokinin A (4-10)
  • [Tyr5,D-Trp6,8,9,Arg10]-NKA (4-10)
Molecular Formula
C57H68N14O10 • XC2H4O2
Formula Weight
1109.3
Purity
≥98%
Formulation
A solid
Peptide Sequence
DYwVwwR-NH2
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥10 mg/mlEthanol: Slightly soluble: 0.1-1 mg/ml
SMILES
N=C(N)NCCC[C@@H](C(N)=O)NC([C@@H](CC1=CNC2=CC=CC=C12)NC([C@H](NC([C@H](C(C)C)NC([C@H](NC([C@@H](NC([C@@H](N)CC(O)=O)=O)CC3=CC=C(C=C3)O)=O)CC4=CNC5=CC=CC=C45)=O)=O)CC6=CNC7=CC=CC=C67)=O)=O.OC(C)=O
InChi Code
InChI=1S/C57H68N14O10.C2H4O2/c1-30(2)49(71-55(80)47(25-34-29-65-42-15-8-5-12-38(34)42)69-52(77)44(22-31-17-19-35(72)20-18-31)67-51(76)39(58)26-48(73)74)56(81)70-46(24-33-28-64-41-14-7-4-11-37(33)41)54(79)68-45(23-32-27-63-40-13-6-3-10-36(32)40)53(78)66-43(50(59)75)16-9-21-62-57(60)61;1-2(3)4/h3-8,10-15,17-20,27-30,39,43-47,49,63-65,72H,9,16,21-26,58H2,1-2H3,(H2,59,75)(H,66,78)(H,67,76)(H,68,79)(H,69,77)(H,70,81)(H,71,80)(H,73,74)(H4,60,61,62);1H3,(H,3,4)/t39-,43-,44-,45+,46+,47+,49-;/m0./s1
InChi Key
GEMMXXJOYQNYLE-GZOXVFSSSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    5 mg

    $79

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    10 mg

    $126

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    25 mg

    $257

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    50 mg

    $395

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    Product Description

    MEN10207 is a peptide neurokinin-2 (NK2) receptor antagonist.1 It inhibits contractions induced by neurokinin A (NKA) in endothelium-deprived isolated rabbit pulmonary artery (pA2 = 7.89), 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 = 5.9 using NKA as an agonist) and NK1 receptors in isolated guinea pig ileum (pA2 = 5.52 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, MEN10207 (1 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. However, MEN10207 also induces bladder motility in anesthetized rats and bronchoconstriction in anesthetized guinea pigs when administered alone.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Maggi, C.A., Giuliani, S., Ballati, L., et al. In vivo evidence for tachykininergic transmission using a new NK-2 receptor-selective antagonist, MEN 10,376. J. Pharmacol. Exp. Ther. 257(3), 1172-1178 (1991).