| Identification | Back Directory | [Name]
2-Piperazinecarboxamide, N4-[N-(1-oxoheptyl)-L-cysteinyl-L-histidyl-L-phenylalanyl-D-alanylglycyl-L-arginyl-D-norleucyl-L-α-aspartyl-L-arginyl-L-isoleucyl-L-seryl-L-cysteinyl-L-tyrosyl]-5-[3-[(aminoiminomethyl)amino]propyl]-6-oxo-, cyclic (1→12)-disulfide, (2R,5S)- | [CAS]
952295-80-6 | [Synonyms]
PL-3994
(Hept-cyclo(Cys-His-Phe-D-Ala-Gly-Arg-D-nle-Asp-Arg-Ile-Ser-Cys)-Tyr-(Arg mimetic)-NH2)
2-Piperazinecarboxamide, N4-[N-(1-oxoheptyl)-L-cysteinyl-L-histidyl-L-phenylalanyl-D-alanylglycyl-L-arginyl-D-norleucyl-L-α-aspartyl-L-arginyl-L-isoleucyl-L-seryl-L-cysteinyl-L-tyrosyl]-5-[3-[(aminoiminomethyl)amino]propyl]-6-oxo-, cyclic (1→12)-disulfide, (2R,5S)- | [Molecular Formula]
C82H127N27O20S2 | [MOL File]
952295-80-6.mol | [Molecular Weight]
1875.19 |
| Hazard Information | Back Directory | [Uses]
PL-3994 is a natriuretic peptide receptor-A (NPR-A) agonist that is resistant to neutral endopeptidase and acts as a bronchodilator. PL-3994 produces concentration-dependent relaxation of pre-contracted guinea-pig trachea with an IC50 value of 42.7 nM[1]. | [in vivo]
Intratracheal PL-3994 (1-1000 mg/kg; i.t.; single dose) produces a dose-dependent inhibition of the bronchoconstrictor response evoked by aerosolized methacholine, without significant effect on cardiovascular parameters[1].
PL-3994 is resistant to degradation by human neutral endopeptidase (hNEP) (92% remaining after 2 h), whereas the natural ligands, ANP and CNP, are rapidly metabolized (≤1% remaining after 2 h)[1].
| Animal Model: | Guinea-pig model anaesthetized with urethane (1.75 g/kg, i.p.)[1] | | Dosage: | 1, 10, 100, 1000 mg/kg | | Administration: | Intrathecal; single dose | | Result: | Resulted a significant maximum inhibition of 43%, 63% and 70%, respectively, observed after 15-min pretreatment at doses of 10, 100 and 1000 mg/kg. |
| [References]
[1] Edelson JD, et al. In vitro and in vivo pharmacological profile of PL-3994, a novel cyclic peptide (Hept-cyclo(Cys-His-Phe-d-Ala-Gly-Arg-d-Nle-Asp-Arg-Ile-Ser-Cys)-Tyr-[Arg mimetic]-NH(2)) natriuretic peptide receptor-A agonist that is resistant to neutral endopeptidase and acts as a bronchodilator. Pulm Pharmacol Ther. 2013 Apr;26(2):229-38. DOI:10.1016/j.pupt.2012.11.001 |
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| Company Name: |
Biorbyt Ltd.
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+44 (0)1223 859 353 |
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http://www.biorbyt.com |
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