A peptide agonist of the NK2 receptor
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GR64349 (acetate)

Item No. 42915

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(S)-4-(((S)-1-(((S)-1-(((S)-1-(((R)-1-((S)-1-(((S)-1-amino-4-(methylthio)-1-oxobutan-2-yl)amino)-4-methyl-1-oxopentan-2-yl)-2-oxopyrrolidin-3-yl)amino)-3-methyl-1-oxobutan-2-yl)amino)-1-oxo-3-phenylpropan-2-yl)amino)-3-hydroxy-1-oxopropan-2-yl)amino)-3-((S)-2,6-diaminohexanamido)-4-oxobutanoic acid
Synonyms
  • Lys-Asp-Ser-Phe-Val-[R-γ-Lac]-Leu-Met-NH2
  • [Lys3,Gly8-R-Lac-Leu9]NKA (3-10)
  • [Lys3,Gly8-R-γ-lactam-Leu9]NKA (3-10)
  • [Lys3,Gly8-R-Lac-Leu9]Neurokinin A (3-10)
Molecular Formula
C42H68N10O11S • C2H4O2
Formula Weight
981.2
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly Soluble: 0.1-1 mg/mlWater: Slightly Soluble: 0.1-1 mg/ml
SMILES
CSCC[C@@H](C(N)=O)NC([C@@H](N1C([C@@H](CC1)NC([C@H](C(C)C)NC([C@@H](NC([C@H](CO)NC([C@H](CC(O)=O)NC([C@@H](N)CCCCN)=O)=O)=O)CC2=CC=CC=C2)=O)=O)=O)CC(C)C)=O.CC(O)=O
InChi Code
InChI=1S/C42H68N10O11S.C2H4O2/c1-23(2)19-32(40(61)46-27(35(45)56)15-18-64-5)52-17-14-28(42(52)63)47-41(62)34(24(3)4)51-38(59)29(20-25-11-7-6-8-12-25)49-39(60)31(22-53)50-37(58)30(21-33(54)55)48-36(57)26(44)13-9-10-16-43;1-2(3)4/h6-8,11-12,23-24,26-32,34,53H,9-10,13-22,43-44H2,1-5H3,(H2,45,56)(H,46,61)(H,47,62)(H,48,57)(H,49,60)(H,50,58)(H,51,59)(H,54,55);1H3,(H,3,4)/t26-,27-,28+,29-,30-,31-,32-,34-;/m0./s1
InChi Key
FRPLQMAKGLULNS-GHUJIWMPSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Certificates of Analysis & Batch Specific Data

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    1 mg

    $347

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    5 mg

    $867

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    Product Description

    GR64349 is a peptide agonist of the neurokinin-2 (NK2) receptor.1 It selectively induces contractions in isolated rat colon muscularis mucosae, which endogenously express NK2 receptors, over isolated guinea pig ileum longitudinal smooth muscle and everted rat portal vein, which endogenously express NK1 and NK3 receptors, respectively (EC50s = 3.7, 4,237, and 1,177 nM, respectively). GR64349 also induces contractions in isolated guinea pig trachea in a concentration-dependent manner.2 In vivo, GR64349 (1.1 nmol/animal) induces contralateral rotations in rats when infused into the substantia nigra.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Deal, M.J., Hagan, R.M., Ireland, S.J., et al. Conformationally constrained tachykinin analogues: Potent and highly selective neurokinin NK-2 receptor agonists. J. Med. Chem. 35(22), 4195-4204 (1992).

    2. Beresford, I.J., Sheldrick, R.L., Ball, D.I., et al. GR159897, a potent non-peptide antagonist at tachykinin NK2 receptors. Eur. J. Pharmacol. 272(2-3), 241-248 (1995).

    3. Elliott, P.J., Mason, G.S., Stephens-Smith, M., et al. Behavioural and biochemical responses following activation of midbrain dopamine pathways by receptor selective neurokinin agonists. Neuropeptides 19(2), 119-126 (1991).