| Identification | Back Directory | [Name]
Plecanatide | [CAS]
467426-54-6 | [Synonyms]
Trulance
Pukanatide
ATCH(1-39)
Prikanatide
Plecanatide
Plecanatide impurity
Plecanatide USP/EP/BP
Plecanatide Impurtiy
ASN-ASP-GLU-CYS-GLU-LEU-CYS-VAL-ASN-VAL-ALA-CYS-THR-GLY-CYS-LEU(DISULFIDE BOND CYS1&CYS3,CYS2&CYS4)
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)
(4S)-4-[(2S)-2-[(2S)-2-amino-3-carbamoylpropanamido]-3-carboxypropanamido]-4-{[(1R,4S,7S,10S,13S,16R,19S,22S,25R,32S,38R)-10-(carbamoylmethyl)-38-{[(1S)-1-carboxy-3-methylbutyl]carbamoyl}-22-(2-carboxyethyl)-32-[(1R)-1-hydroxyethyl]-4-methyl-19-(2-methylpropyl)-3,6,9,12,15,18,21,24,30,33,36-undecaoxo-7,13-bis(propan-2-yl)-27,28,40,41-tetrathia-2,5,8,11,14,17,20,23,31,34,37-undecaazabicyclo[14.13.13]dotetracontan-25-yl]carbamoyl}butanoic acid | [Molecular Formula]
C65H104N18O26S4 | [MDL Number]
MFCD33029246 | [MOL File]
467426-54-6.mol | [Molecular Weight]
1681.89 |
| Chemical Properties | Back Directory | [Boiling point ]
2120.0±65.0 °C(Predicted) | [density ]
1.47±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
3.61±0.21(Predicted) | [color ]
White to off-white | [InChIKey]
NSPHQWLKCGGCQR-DLJDZFDSSA-N |
| Hazard Information | Back Directory | [Uses]
Plecanatide is used in the treatment of chronic idiopathic constipation and irritable bowel syndrome with constipation. It works as a laxative by drawing water in to the gastrointestinal tract thereby softening stool and encouraging its natural passage. | [Enzyme inhibitor]
This uroguanylin analogue (FW = 1681.90 g/mol; CAS 467426-54-6), also
known by the codename SP-304, binds to and activates guanylate cyclase-C
(GC-C) receptors (EC50 ≈ 0.3 μM) expressed on the epithelial cells lining
the gastrointestinal mucosa, stimulating cyclic GMP production, which in
turn sequentially activates protein kinase G-II and the chloride channel
known as the Cystic Fibrosis Transmembrane-conductance Regulator
(CFTR) to regulate ion and fluid transport, to promote epithelial cell
homeostasis, and to maintain barrier function in the GI mucosa. Plecanatide
is a hexadecapeptide that is structurally identical to uroguanylin, except for
an glutamate substitution at position-3. Oral treatment with plecanatide at a
dose range between 0.05-2.5 mg/kg per day is as effective as once-daily
treatment with 5-amino salicylic acid (100 mg/kg) or sulfasalazine (80
mg/kg). Amelioration of colitis by the treatment with plecanatide or
dolcanatide was not dose-dependent, most likely due to saturation of
available GC-C receptors. |
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