linaclotide   Click here for help

GtoPdb Ligand ID: 5017

Synonyms: Constella® | Linzess® | MM-416775
Approved drug
linaclotide is an approved drug (FDA and EMA (2012))
Comment: Linaclotide represents a first-in-class, oral guanylate cyclase 2C activator [2]. It is a synthetic analogue of pathological heat-stable bacterial enterotoxins, and retains the same intrachain disulfide bond structure essential for biological activity.
Marketed formulations contain linaclotide acetate (PubChem CID 16158207). See also plecanatide, the second approved GC-C activator.
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Selectivity at catalytic receptors
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Target Sp. Type Action Value Parameter Concentration range (M) Reference
Guanylyl cyclase-C Primary target of this compound Hs Agonist Agonist 8.9 pKi - 2-3
pKi 8.9 (Ki 1.24x10-9 M) [2-3]
Description: Competitive-inhibition of [125I]-STa binding to T84 colorectal carcinoma cells
Guanylyl cyclase-C Rn Agonist Agonist 8.4 pKi - 2
pKi 8.4 (Ki 4.2x10-9 M) [2]
Description: Competitive-inhibition of [125I]-STa binding to rat intestinal mucosa