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In vitro: Linaclotide inhibits in vitro [125I]-STa binding to intestinal mucosal membranes from wt mice in a concentration-dependent manner. In contrast, [125I]-STa binding to these membranes from GC-C null mice is significantly decreased. After incubation in vitro in jejunal fluid for 30 min, linaclotide is completely degraded. Linaclotide acts on guanylate cyclase-C receptors on the luminal membrane to increase chloride and bicarbonate secretions into the intestine and inhibit the absorption of sodium ions, thus increasing the secretion of water into the lumen and improving defecation; the drug is minimally absorbed into the systemic circulation.
In vivo: Pharmacokinetic analysis shows very low oral bioavailability (0.10%). In intestinal secretion and transit models, linaclotide exhibits significant pharmacological effects in wt, but not in GC-C null mice: induction of increased fluid secretion into surgically ligated jejunal loops is accompanied by the secretion of elevated levels of cyclic guanosine-3',5-monophosphate and accelerated gastrointestinal transit. Linaclotide significantly increases weekly spontaneous bowel movements and complete spontaneous bowel movements (CSBMs) while reducing abdominal pain in patients with chronic constipation.
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| Animal models | female CD-1 mice |
| Formulation | |
| Dosages | 8 mg/kg |
| Administration | i.v. |
| Molecular Weight | 1526.74 |
| Formula | C59H79N15O21S6 |
| CAS Number | 851199-59-2 |
| Solubility (25°C) | DMSO 30 mg/mL Water 9 mg/mL (adjust pH to 2 with HCl) |
| Storage | -20°C, dry, sealed |
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MCUF-651 is an orally active guanylyl cyclase A receptor (GC-A) positive allosteric modulator (PAM) (KD: 397 nM ). |
| Zagociguat
Zagociguat is the stimulator of soluble guanylate cyclase. |
| 2-Chloro-ATP
2-Chloro-ATP is a soluble guanylate cyclase inhibitor that increases intracellular calcium concentration at low concentrations through a mechanism independent of inositol phosphate production. |
| CFM 1571 hydrochloride
CFM 1571 hydrochloride is the stimulator of the nitric oxide receptor, soluble guanylate cyclase (sGC) with an EC50 and IC50 of 5.49 μM and 2.84 μM, respectively. |
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