A peptide antagonist of the NK2 receptor
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GR83074 (trifluoroacetate salt)

Item No. 44017

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N2-[(1,1-dimethylethoxy)carbonyl]-L-arginyl-L-alanyl-D-tryptophyl-L-phenylalanyl-D-prolyl-L-prolyl-L-norleucinamide, trifluoroacetate salt
Synonyms
  • Boc-Arg-Ala-D-Trp-Phe-D-Pro-Pro-Nle-NH2
Molecular Formula
C50H72N12O9 • XCF3COOH
Formula Weight
985.2
Purity
≥95%
Formulation (Request formulation change)
A solid
Peptide Sequence
Boc-RAwFpPX-NH2 (X = norisoleucine)
Solubility(Learn about Variance in Solubility)
DMSO: Slightly soluble: 0.1-1 mg/mlWater: Slightly soluble: 0.1-1 mg/ml
SMILES
O=C(N1[C@H](CCC1)C(N2[C@@H](CCC2)C(N[C@H](C(N)=O)CCCC)=O)=O)[C@H](CC3=CC=CC=C3)NC([C@H](NC([C@H](C)NC([C@H](CCCNC(N)=N)NC(OC(C)(C)C)=O)=O)=O)CC4=CNC5=CC=CC=C45)=O.FC(F)(C(O)=O)F
InChi Code
InChI=1S/C50H72N12O9.C2HF3O2/c1-6-7-19-35(41(51)63)57-45(67)39-22-14-25-61(39)47(69)40-23-15-26-62(40)46(68)38(27-31-16-9-8-10-17-31)59-44(66)37(28-32-29-55-34-20-12-11-18-33(32)34)58-42(64)30(2)56-43(65)36(21-13-24-54-48(52)53)60-49(70)71-50(3,4)5;3-2(4,5)1(6)7/h8-12,16-18,20,29-30,35-40,55H,6-7,13-15,19,21-28H2,1-5H3,(H2,51,63)(H,56,65)(H,57,67)(H,58,64)(H,59,66)(H,60,70)(H4,52,53,54);(H,6,7)/t30-,35-,36-,37+,38-,39-,40+;/m0./s1
InChi Key
IRCAIGPCPMZDKO-FFWYJSDESA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $109

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    5 mg

    $491

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    10 mg

    $872

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    Product Description

    GR83074 is a peptide antagonist of the neurokinin-2 (NK2) receptor.1 It selectively inhibits neurokinin A-induced contractions in rat colon muscularis mucosae, which express NK2 receptors, over substance P-induced contractions in guinea pig ileum longitudinal smooth muscle strips, which express NK1 receptors (pKbs = 8.2 and 5.8, respectively). GR83074 (0.3 µmol/kg) inhibits neurokinin A-induced bronchoconstriction in guinea pigs.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. McElroy, A.B., Clegg, S.P., Deal, M.J., et al. Highly potent and selective heptapeptide antagonists of the neurokinin NK-2 receptor. J. Med. Chem. 35(14), 2582-2591 (1992).