An NK2 receptor agonist
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[Lys5,MeLeu9,Nle10]-Neurokinin A (4-10) (trifluoroacetate salt)

Item No. 43051

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
L-α-aspartyl-L-lysyl-L-phenylalanyl-L-valylglycyl-N-methyl-L-leucyl-L-norleucinamide, trifluoroacetate salt
Synonyms
  • Asp-Lys-Phe-Val-Gly-methyl-Leu-Nle-NH2
  • LMN-NKA
Molecular Formula
C39H65N9O9 • XCF3COOH
Formula Weight
804.0
Purity
≥98%
Formulation (Request formulation change)
A solid
Peptide Sequence
DKFVG-methyl-LX-NH2 (X = Norleucine)
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥ 10 mg/mlEthanol: Sparingly soluble: 1-10 mg/mlPBS (pH 7.2): Soluble: ≥ 10 mg/ml
SMILES
OC(C[C@H](N)C(N[C@@H](CCCCN)C(N[C@H](C(N[C@@H](C(C)C)C(NCC(N(C)[C@@H](CC(C)C)C(N[C@H](C(N)=O)CCCC)=O)=O)=O)=O)CC1=CC=CC=C1)=O)=O)=O.O=C(O)C(F)(F)F
InChi Code
InChI=1S/C39H65N9O9.C2HF3O2/c1-7-8-16-27(34(42)52)44-38(56)30(19-23(2)3)48(6)31(49)22-43-39(57)33(24(4)5)47-37(55)29(20-25-14-10-9-11-15-25)46-36(54)28(17-12-13-18-40)45-35(53)26(41)21-32(50)51;3-2(4,5)1(6)7/h9-11,14-15,23-24,26-30,33H,7-8,12-13,16-22,40-41H2,1-6H3,(H2,42,52)(H,43,57)(H,44,56)(H,45,53)(H,46,54)(H,47,55)(H,50,51);(H,6,7)/t26-,27-,28-,29-,30-,33-;/m0./s1
InChi Key
SCQLNJRFZWBCEM-WVHCJTCASA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $87

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    10 mg

    $165

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    25 mg

    $392

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    50 mg

    $740

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    Product Description

    [Lys5,MeLeu9,Nle10]-Neurokinin A (4-10) is a neurokinin-2 (NK2) receptor agonist and derivative of neurokinin A (Item No. 24221).1 It binds to NK2 receptors in isolated human colon circular muscle membranes in a radioligand binding assay (IC50 = 0.87 nM). [Lys5,MeLeu9,Nle10]-Neurokinin A (4-10) induces contraction of isolated rat bladder and fundus strips (EC50s = 10 and 117 nM, respectively), effects that can be inhibited by the NK2 receptor antagonists SR48968 and MEN10627.2 It also induces contraction of uterine horns isolated from rats in proestrus/estrus and diestrus/metestrus (EC50s = 25.12 and 51.29 nM, respectively).3 [Lys5,MeLeu9,Nle10]-Neurokinin A (4-10) induces urination and defecation in conscious dogs but also induces emesis and hypotension at similar doses.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Warner, F.J., Comis, A., Miller, R.C., et al. Characterization of the [125I]-neurokinin A binding site in the circular muscle of human colon. Br. J. Pharmacol. 127(5), 1105-1110 (1999).

    2. Matuszek, M.A., Zeng, X.-P., Strigas, J., et al. An investigation of tachykinin NK2 receptor subtypes in the rat. Eur. J. Pharmacol. 352(1), 103-109 (1998).

    3. Moodley, N., Lau, W.A.K., Pennefather, J.N., et al. NK2 receptors mediate tachykinin-induced contractions of rat uterus during the oestrous cycle. Eur. J. Pharmacol. 376(1-2), 53-60 (1999).

    4. Rupniak, N.M.J., Katofiasc, M., Walz, A., et al. [Lys5,MeLeu9,Nle10]-NKA(4-10) Elicits NK2 receptor-mediated micturition and defecation, and NK1 receptor-mediated emesis and hypotension, in conscious dogs. J. Pharmacol. Exp. Ther. 366(1), 136-144 (2018).