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1092457-65-2

1092457-65-2 Structure

1092457-65-2 Structure
IdentificationBack Directory
[Name]

D-Leucine, D-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)
[CAS]

1092457-65-2
[Synonyms]

Dolcanatide
D-Leucine, D-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)
[Molecular Formula]

C65H104N18O26S4
[MOL File]

1092457-65-2.mol
[Molecular Weight]

1681.89
Chemical PropertiesBack 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
[Sequence]

{d-Asn}--Asp-Glu-Cys-Glu-Leu-Cys-Val-Asn-Val-Ala-Cys-Thr-Gly-Cys-{d-Leu} (Disulfide bridge: Cys4-Cys12; Cys7-Cys15)
Hazard InformationBack Directory
[Uses]

Dolcanatide is an orally active GC-C (guanylate cyclase-C) agonist. Dolcanatide shows laxative, anti-nociceptive and anti-inflammatory activity. Dolcanatide can be used in inflammatory bowel disease research[1][2].
[in vivo]

Dolcanatide (oral administration; 0.01 and 0.05 mg/kg; once) alleviates TNBS-induced rectal allodynia in rats[1].
Dolcanatide (oral administration; 0.01 and 0.05 mg/kg; once) alleviates stress-induced colorectal hypersensitivity (CRD) in rats[1].

Animal Model:TNBS-induced rectal allodynia in rats[1]
Dosage:0.01 and 0.05 mg/kg
Administration:Oral administration; 0.01 and 0.05 mg/kg; once
Result:Attenuated the TNBS-induced increase in the number of abdominal contractions (distending pressures up to 60 mmHg).
Animal Model:Stress-induced visceral hypersensitivity in Wistar rats[1]
Dosage:0.01 and 0.05 mg/kg
Administration:Oral administration; 0.01 and 0.05 mg/kg; once
Result:Resulted in a significant reduction in the rate of PRS (partial restraint stress)-induced abdominal contractions with increasing CRD (colorectal distension) pressures.
[References]

[1] Boulete IM, et al. Oral treatment with plecanatide or dolcanatide attenuates visceral hypersensitivity via activation of guanylate cyclase-C in rat models. World J Gastroenterol. 2018 May 7;24(17):1888-1900. DOI:10.3748/wjg.v24.i17.1888
[2] 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
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