| Identification | Back Directory | [Name]
Plecanatide acetate | [CAS]
1075732-84-1 | [Synonyms]
Plecanatide acetate
L-Leucine, L-asparaginyl-L-α-aspartyl-L-α-glutamyl-L-cysteinyl-L-α-glutamyl-L-leucyl-L-cysteinyl-L-valyl-L-asparaginyl-L-valyl-L-alanyl-L-cysteinyl-L-threonylglycyl-L-cysteinyl-, cyclic (4→12),(7→15)-bis(disulfide), acetate (1:1) | [Molecular Formula]
C67H108N18O28S4 | [MOL File]
1075732-84-1.mol | [Molecular Weight]
1741.94 |
| Hazard Information | Back Directory | [Uses]
Plecanatide acetate, an analogue of Uroguanylin, is an orally active guanylate cyclase-C (GC-C) receptor agonist. Plecanatide acetate activates GC-C receptors to stimulate cGMP synthesis with an EC50 of 190 nM in T84 cells assay. Plecanatide acetate can be used for the research of chronic idiopathic constipation, and it also shows anti-inflammatory activity in models of murine colitis[1][2][3]. | [in vivo]
Plecanatide (0.5 and 2.5 mg/kg, p.o.) ameliorates spontaneous and chemically induced colitis after treatment for 7 days in BALB/c mice, and 14 days in TCRα-/- mice[1].
Plecanatide (0.005-5 mg/kg, once daily for 7 days) also shows anti-inflammatory activity in dextran sulfate sodium (DSS) and trinitrobenzene sulfonic (TNBS)-induced colitis in BDF-1 mice[1]. | Animal Model: | Female BALB/c mice (2-4 month old) are induced colitis by TNBS[1] | | Dosage: | 0, 0.5 and 2.5 mg/kg | | Administration: | P.o. for 7 days | | Result: | Effectively reduced colitis severity scores as compared to vehicle treatment. |
| [References]
[1] Shailubhai K, et al. Plecanatide and dolcanatide, novel guanylate cyclase-C agonists, ameliorate gastrointestinal inflammation in experimental models of murine colitis. World J Gastrointest Pharmacol Ther. 2015 Nov 6;6(4):213-22. DOI:10.4292/wjgpt.v6.i4.213
[2] Rao SSC. Plecanatide: a new guanylate cyclase agonist for the treatment of chronic idiopathic constipation. Therap Adv Gastroenterol. 2018 Jun 8;11:1756284818777945. DOI:10.1177/1756284818777945
[3] Shailubhai K, et, al. Plecanatide, an oral guanylate cyclase C agonist acting locally in the gastrointestinal tract, is safe. Dig Dis Sci. 2013 Sep;58(9):2580-6. DOI:10.1007/s10620-013-2684-z |
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Biorbyt Ltd.
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