An NK2 receptor antagonist
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MEN10376

Item No. 31142

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-lysinamide
CAS Number
135306-85-3
Synonyms
  • DYWVWWK-NH2
  • Asp-Tyr-Trp-Val-Trp-Trp-Lys-NH2
Molecular Formula
C57H68N12O10
Formula Weight
1081.2
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:5): 0.16 mg/ml
λmax
222 nm
SMILES
OC(C[C@H](N)C(N[C@@H](CC1=CC=C(O)C=C1)C(N[C@H](CC2=CNC3=C2C=CC=C3)C(N[C@@H](C(C)C)C(N[C@H](CC4=CNC5=C4C=CC=C5)C(N[C@H](CC6=CNC7=C6C=CC=C7)C(N[C@@H](CCCCN)C(N)=O)=O)=O)=O)=O)=O)=O)=O
InChi Code
InChI=1S/C57H68N12O10/c1-31(2)50(69-56(78)48(26-35-30-63-43-16-8-5-13-39(35)43)67-53(75)45(23-32-18-20-36(70)21-19-32)65-52(74)40(59)27-49(71)72)57(79)68-47(25-34-29-62-42-15-7-4-12-38(34)42)55(77)66-46(24-33-28-61-41-14-6-3-11-37(33)41)54(76)64-44(51(60)73)17-9-10-22-58/h3-8,11-16,18-21,28-31,40,44-48,50,61-63,70H,9-10,17,22-27,58-59H2,1-2H3,(H2,60,73)(H,64,76)(H,65,74)(H,66,77)(H,67,75)(H,68,79)(H,69,78)(H,71,72)/t40-,44-,45-,46+,47+,48+,50-/m0/s1
InChi Key
QQHOFZNACVKNHK-SXVLBCBNSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $75

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    1 mg

    $134

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    5 mg

    $516

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    Product Description

    MEN10376 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 = 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.

    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).