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Plecanatide acetate

  Cat. No.:  DC20012   Featured
Chemical Structure
1075732-84-1
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Field of application
Plecanatide acetate is a guanylate cyclase-C (GC-C) receptor agonist, binds and activates GC-C receptor, with an EC50 of 190 nM in T84 cells. Plecanatide acetate shows an-inflammatory activity in models of murine colitis.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1075732-84-1
SMILES: C(N[C@@H](CC(O)=O)C(N[C@@H](CCC(O)=O)C(N[C@@H](CS)C(N[C@@H](CCC(O)=O)C(N[C@@H](CC(C)C)C(N[C@@H](CS)C(N[C@@H](C(C)C)C(N[C@@H](CC(N)=O)C(N[C@@H](C(C)C)C(N[C@@H](C)C(N[C@@H](CS)C(N[C@@H]([C@H](O)C)C(NCC(N[C@@H](CS)C(N[C@@H](CC(C)C)C(O)=O)=O)=O)=O)=O)=O)=O)=O
Formula: C67H108N18O28S4
M.Wt: 1741.94
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: Plecanatide acetate is a guanylate cyclase-C (GC-C) receptor agonist, with an EC50 of 190 nM in T84 cells. Plecanatide acetate shows anti-inflammatory activity in models of murine colitis[1].
Target: EC50: 190 nM (guanylate cyclase-C receptor, T84 cells)[1]
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)[1] Dosage: 0.5 and 2.5 mg/kg Administration: P.O. for 7 days, with the first dose given the same day as TNBS Result: Effectively reduced colitis severity scores in BALB/c mice. Animal Model: BDF-1 mice (10-12 week old)[1] Dosage: 0.005-5 mg/kg Administration: P.O. once daily for 7 days Result: Effective at 0.005 mg/kg as sulfasalazine (80 mg/kg) to ameliorate DSS induced colitis in BDF-1 mice, but had no incremental effect on the amelioration of colitis at higher doses than 0.005 mg/kg. Plecanatide at 0.05 mg/kg per day was as effective as 80 mg/kg per day of sulfasalazine. Animal Model: TCRα-/- mice (sixteen week old)[1] Dosage: 0.5 or 2.5 mg/kg Administration: P.O. for 14 days Result: Reduced colitis scores in TCRα-/- mice.
In Vitro: Plecanatide acetate is a GC-C receptor agonist, binds and activates GC-C receptor, with an EC50 of 190 nM in T84 cells[1].
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.
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2018-0101
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