Plecanatide acetate 

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].

EC50: 190 nM (guanylate cyclase-C receptor, T84 cells)^[1]

Plecanatide (1 nM-10 μM) activates GC-C receptor to stimulate cGMP synthesis in a dose-dependent manner with EC₅₀ of 190 nM in T84 cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

1741.94

C₆₇H₁₀₈N₁₈O₂₈S₄

1075732-84-1

Solid

White to off-white

Asn-Asp-Glu-Cys-Glu-Leu-Cys-Val-Asn-Val-Ala-Cys-Thr-Gly-Cys-Leu (Disulfide bridge: Cys4-Cys12; Cys7-Cys15)

NDECELCVNVACTGCL (Disulfide bridge: Cys4-Cys12; Cys7-Cys15)

NC(C[C@H](N)C(N[C@@H](CC(O)=O)C(N[C@@H](CCC(O)=O)C(N[C@@H]1C(N[C@H](C(N[C@H](C(N[C@]2([H])C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@@](C(N[C@@](C(NCC(N[C@@H](CSSC2)C(N[C@H](C(O)=O)CC(C)C)=O)=O)=O)([H])[C@H](O)C)=O)([H])CSSC1)=O)C)=O)C(C)C)=O)CC(N)=O)=O)C(C)C)=O)=O)CC(C)C)=O)CCC(O)=O)=O)=O)=O)=O)=O.CC(O)=O

Room temperature in continental US; may vary elsewhere.

Sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [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.  [Content Brief]

  [2]. Rao SSC. Plecanatide: a new guanylate cyclase agonist for the treatment of chronic idiopathic constipation. Therap Adv Gastroenterol. 2018 Jun 8;11:1756284818777945.  [Content Brief]

  [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.  [Content Brief]