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Cat. No. Product Name CAS No. Information
PC-35286

GSK3179106

1627856-64-7

GSK3179106 (GSK-3179106, GSK 3179106) is a potent, selective, first-in-class and gut-restricted RET kinase inhibitor with IC50 of 0.4 and 11 nM in the biochemical assay and cellular assay respectively, 273-fold selectivity over KDR; possesses good kinase selectivity, only 26 out of a set of >300 recombinant kinases were found to be inhibited at 1 uM; GSK3179106 dosed orally at 10 mg/kg for 3.5 days BID reduced the visceromotor response to colorectal distension in comparison to rats given an acetic acid enema and dosed with vehicle, GSK3179106 has been developed for the treatment of IBS in a clinical setting.

Irritable Bowel Syndrome

Phase 1 Clinical

PC-43351

LX-1031

945976-76-1 LX-1031 is a potent, orally active tryptophan 5-hydroxylase (TPH) inhibitor with potency of 10-100 nM, reduces 5-HT synthesis peripherally; dose-dependently reduces expression of 5-HT in the duodenum, jejunum and ileum, but had no effect on brain 5-HT levels, significantly reduces urinary 5-hydroxyindoleacetic acid (5-HIAA) in vivo; exhibits potential for illnesses characterized by excess 5-HT, such as diarrhea-predominant irritable bowel syndrome (IBS-D) and carcinoid diarrhea.

Irritable Bowel Syndrome

Phase 2 Discontinued

PC-43209

Etrasimod

1206123-37-6 Etrasimod (APD334) is a potent, selective, centrally available S1P1 receptor antagonist with β-arrestin EC50 of 6.1 nM, internalizes human S1P1 in CHO cells expressing HA tagged S1P1 with IC50 of 1.88 nM; produces robust lymphocyte lowering effect (IC50=0.1 uM in mice), shows effectivity in mouse experimental autoimmune encephalomyelitis (EAE) model of MS and a rat collagen induced arthritis (CIA) model, orally active.

Irritable Bowel Syndrome

Phase 2 Clinical

PC-61902

Semapimod

352513-83-8 Semapimod (CNI 1493;AXD-455) is a tetravalent guanylhydrazone that acts as a selective inhibitor of cytokine-inducible arginine transport and NO production, inhibits TLR4 signaling (IC50=0.3 uM) by targeting the TLR chaperone gp96; does not inhibit EDRF activity, inhibits nitric oxide synthesis by inflammatory macrophages; prevents the development of carrageenan-induced footpad inflammation, and conferred protection against lethal LPS challenge in mice.

Irritable Bowel Syndrome

Phase 2 Clinical

PC-61901

Semapimod hydrochloride

164301-51-3 Semapimod (CNI 1493;AXD-455) is a tetravalent guanylhydrazone that acts as a selective inhibitor of cytokine-inducible arginine transport and NO production, inhibits TLR4 signaling (IC50=0.3 uM) by targeting the TLR chaperone gp96; does not inhibit EDRF activity, inhibits nitric oxide synthesis by inflammatory macrophages; prevents the development of carrageenan-induced footpad inflammation, and conferred protection against lethal LPS challenge in mice.

Irritable Bowel Syndrome

Phase 2 Clinical

PC-61269

Pexacerfont

459856-18-9 A potent, selective and orally active CRF1 receptor antagonist with IC50 of 6.1 nM, >1,000-fold selectivity over CRF-binding protein and biogenic amine receptors; demonstrates oral effectivity in rat models of anxiety, possesses good pharmacokinetic profile in vivo.

Irritable Bowel Syndrome

Phase 2 Discontinued

PC-61221

MKC-733

194093-42-0 A potent, selective, orally active 5-HT3 receptor agonist with high affinity for canine intestinal smooth muscle 5-HT3 receptors; dose dependently stimulates contraction and basal electrolyte secretion in the isolated guinea pig colon, effects that are antagonized by the selective 5-HT3 antagonist ondansetron, also accelerates gastric emptying in some animal models.

Irritable Bowel Syndrome

Phase 2 Discontinued

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