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Dolcanatide

Cat. No. M31364
Dolcanatide Structure
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Biological Activity

Dolcanatide is an orally active uridine analog that is also a guanylate cyclase C (GC-C) agonist with anti-inflammatory activity and may be used in studies related to inflammatory bowel disease.

Chemical Information
Molecular Weight 1681.89
Formula C65H104N18O26S4
CAS Number 1092457-65-2
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] David S Weinberg, et al. Cancer Biol Ther. Phase I double-blind, placebo-controlled trial of dolcanatide (SP-333) 27 mg to explore colorectal bioactivity in healthy volunteers

[2] Jeffrey A Rappaport, et al. Front Oncol. The Guanylate Cyclase C-cGMP Signaling Axis Opposes Intestinal Epithelial Injury and Neoplasia

[3] Illona-Marie Boulete, et al. World J Gastroenterol. Oral treatment with plecanatide or dolcanatide attenuates visceral hypersensitivity via activation of guanylate cyclase-C in rat models

[4] Kunwar Shailubhai, et al. World J Gastrointest Pharmacol Ther. Plecanatide and dolcanatide, novel guanylate cyclase-C agonists, ameliorate gastrointestinal inflammation in experimental models of murine colitis

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