A peptide NK1 receptor agonist
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GR73632 (acetate)

Item No. 43047

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(5-amino-1-oxopentyl)-L-phenylalanyl-L-phenylalanyl-L-prolyl-N-methyl-L-leucyl-L-methioninamide, acetate
Synonyms
  • Deamino-Orn-Phe-Phe-Pro-N(Me)Leu-Met-NH2
Molecular Formula
C40H59N7O6S • XC2H4O2
Formula Weight
766.0
Purity
≥98%
Formulation (Request formulation change)
A solid
Peptide Sequence
XFFPZM-NH2 (X = Deamino ornithine, Z = N-methyl leucine)
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥ 10 mg/mlEthanol: Soluble: ≥ 10 mg/mlPBS (pH 7.2): Slightly soluble: 0.1-1 mg/ml
SMILES
O=C([C@H](CC1=CC=CC=C1)NC([C@H](CC2=CC=CC=C2)NC(CCCCN)=O)=O)N3[C@H](C(N(C)[C@@H](CC(C)C)C(N[C@@H](CCSC)C(N)=O)=O)=O)CCC3.CC(O)=O
InChi Code
InChI=1S/C40H59N7O6S.C2H4O2/c1-27(2)24-34(38(51)44-30(36(42)49)20-23-54-4)46(3)40(53)33-18-13-22-47(33)39(52)32(26-29-16-9-6-10-17-29)45-37(50)31(25-28-14-7-5-8-15-28)43-35(48)19-11-12-21-41;1-2(3)4/h5-10,14-17,27,30-34H,11-13,18-26,41H2,1-4H3,(H2,42,49)(H,43,48)(H,44,51)(H,45,50);1H3,(H,3,4)/t30-,31-,32-,33-,34-;/m0./s1
InChi Key
JPTHKLGOFVAHTM-DYORFFRXSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

    5 mg

    $160

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    10 mg

    $256

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    25 mg

    $599

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    Product Description

    GR73632 is a peptide neurokinin-1 (NK1) receptor agonist.1 It potentiates electrically induced contractions in isolated guinea pig vas deferens (EC50 = 2 nM). Intradermal administration of GR73632 (30 nmol/animal) increases scratching behavior in gerbils.2 It induces foot tapping behavior in gerbils when intracerebroventricularly administered at a dose of 3 pmol.3 GR73632 (5 mg/kg) induces emesis in shrews.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hall, J.M., and Morton, I.K.M. Novel ligands confirm NK-1 receptor-mediated modulation of neurotransmission in the guinea pig vas deferens preparation. Ann. N. Y. Acad. Sci. 632, 404-406 (1991).

    2. Trower, M.K., Fisher, A., Upton, N., et al. Neurokinin-1 receptor antagonist orvepitant is an effective inhibitor of itch-associated response in a Mongolian gerbil model of scratching behaviour. Exp. Dermatol. 23(11), 858-860 (2014).

    3. Di Fabio, R., Alvaro, G., Griffante, C., et al. Discovery and biological characterization of (2R,4S)-1'-acetyl-N-{(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethyl}-2-(4-fluoro-2-methylphenyl)-N-methyl-4,4'-bipiperidine-1-carboxamide as a new potent and selective neurokinin 1 (NK1) receptor antagonist clinical candidate. J. Med. Chem. 54(4), 1071-1079 (2011).

    4. Zhong, W., Chebolu, S., and Darmani, N.A. Intracellular emetic signaling cascades by which the selective neurokinin type 1 receptor (NK1R) agonist GR73632 evokes vomiting in the least shrew (Cryptotis parva). Neurochem. Int. 122, 106-119 (2019).