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Picture of (2R)-2-[[(2R)-2-[[(2R)-2-amino-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]-N-[(2R)-5-(diaminomethylideneamino)-1-oxo-1-(pyridin-4-ylmethylamino)pentan-2-yl]hexanamide

(2R)-2-[[(2R)-2-[[(2R)-2-amino-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]-N-[(2R)-5-(diaminomethylideneamino)-1-oxo-1-(pyridin-4-ylmethylamino)pentan-2-yl]hexanamide

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Origin: China

Cas No: 228546-92-7

Specification: 99%min

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Supply Ability: 100 mt/month

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    CAS No.: 228546-92-7 Formula: C36H49N9O4 Molecular Weight: 671.83200

    Description

    CR665 (H-D-Phe-D-Phe-D-Nle-D-Arg-NH-4-Picolyl), also known by the previous developmental code names FE-200665 and JNJ-38488502, is an all D-amino acid peptide that acts as a peripherally restricted κ-opioid receptor agonist. The selectivity for FE 200665 is 1/16,900/84,600 for the human κ, μ, and δ opioid receptors, respectively. The dose of FE 200665 required to produce motor impairment (measure of CNS penetration) was 548 times higher than the dose required for antinociceptive activity. It is being developed for use by Cara Therapeutics under the code name CR665.
    A small, double blind study was done in healthy humans to determine the analgesic effects. CR665 was dosed at 0.36mg/kg I.V., and was compared to 15mg oxycodone orally. CR665 had analgesic effects on visceral pain, but produced a hyperalgesic response in a skin pinch test.

    Basic Info

    Chemical Name (2R)-2-[[(2R)-2-[[(2R)-2-amino-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]-N-[(2R)-5-(diaminomethylideneamino)-1-oxo-1-(pyridin-4-ylmethylamino)pentan-2-yl]hexanamide
    Synonyms

    CR665;
    D-Argininamide,D-phenylalanyl-D-phenylalanyl-D-norleucyl-N-(4-pyridinylmethyl);
    UNII-3BX9UG06GG;

    CAS No. 228546-92-7
    Molecular Formula C36H49N9O4
    Molecular Weight 671.83200
    PSA 231.17000
    LogP 6.67080

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