Plecanatide

Modify Date: 2024-01-02 11:50:12

Plecanatide Structure
Plecanatide structure
Common Name Plecanatide
CAS Number 467426-54-6 Molecular Weight 1681.886
Density 1.5±0.1 g/cm3 Boiling Point 2120.0±65.0 °C at 760 mmHg
Molecular Formula C65H104N18O26S4 Melting Point N/A
MSDS N/A Flash Point 1235.9±34.3 °C

 Use of Plecanatide


Plecanatide, an analogue of uroguanylin, is an orally active guanylate cyclase-C (GC-C) receptor agonist, with an EC50 of 190 nM in T84 cells. Plecanatide 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].

 Names

Name Plecanatide
Synonym More Synonyms

 Plecanatide Biological Activity

Description Plecanatide, an analogue of uroguanylin, is an orally active guanylate cyclase-C (GC-C) receptor agonist, with an EC50 of 190 nM in T84 cells. Plecanatide 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].
Related Catalog
Target

EC50: 190 nM (guanylate cyclase-C)[1]

In Vitro 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].
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.

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

[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.

 Chemical & Physical Properties

Density 1.5±0.1 g/cm3
Boiling Point 2120.0±65.0 °C at 760 mmHg
Molecular Formula C65H104N18O26S4
Molecular Weight 1681.886
Flash Point 1235.9±34.3 °C
Exact Mass 1680.625244
LogP -4.45
Vapour Pressure 0.0±0.6 mmHg at 25°C
Index of Refraction 1.631
Storage condition -20°C

 Safety Information

Hazard Codes Xn

 Synonyms

L-Asparaginyl-L-α-aspartyl-N-{(1R,4S,7S,10S,13S,16R,19S,22S,25R,32S,38R)-10-(2-amino-2-oxoethyl)-22-(2-carboxyethyl)-38-{[(1S)-1-carboxy-3-methylbutyl]carbamoyl}-32-[(1R)-1-hydroxyethyl]-19-isobut yl-7,13-diisopropyl-4-methyl-3,6,9,12,15,18,21,24,30,33,36-undecaoxo-27,28,40,41-tetrathia-2,5,8,11,14,17,20,23,31,34,37-undecaazabicyclo[14.13.13]dotetracont-25-yl}-L-α-glutamine
L-α-Glutamine, L-asparaginyl-L-α-aspartyl-N-[(1R,4S,7S,10S,13S,16R,19S,22S,25R,32S,38R)-10-(2-amino-2-oxoethyl)-22-(2-carboxyethyl)-38-[[[(1S)-1-carboxy-3-methylbutyl]amino]carbonyl]-32-[(1R)- 1-hydroxyethyl]-4-methyl-7,13-bis(1-methylethyl)-19-(2-methylpropyl)-3,6,9,12,15,18,21,24,30,33,36-undecaoxo-27,28,40,41-tetrathia-2,5,8,11,14,17,20,23,31,34,37-undecaazabicyclo[14.13.13]dotetracont-2 5-yl]-
Plecanatide