LX-1031

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

LX-1031 是一种有效的口服活性色氨酸 5-羟化酶 (TPH) 抑制剂，效力为 10-100 nM。

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.

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With oral administration of LX-1031 in mice, the average 5-HT reductions in the jejunum relative to control are appr 33, 51, and 66% with the 15, 45 and 135 mg/kg/day doses respectively. In a preliminary report, the effects of LX-1031, 100 mg/kg daily, on 5-HT levels in jejunal mucosa are reversible within 2 days of discontinuation in mice. LX-1031 dose-dependently reduces expression of 5-HT in the duodenum, jejunum and ileum, but has no effect on brain 5-HT levels in preclinical assay.

LX1031 | LX 1031

Metabolic Enzyme/Protease

TPH

TPH

Other Indications

Irritable Bowel Syndrome

945976-76-1

538.5177

C28H25F3N4O4

>98% (HPLC)

DMSO: ≥ 34 mg/mL

N[C@@H](CC1=CC=C(C2=NC(N)=NC(O[C@H](C3=CC=C(C4=CC=CC(OC)=C4)C=C3)C(F)(F)F)=C2)C=C1)C(O)=O

L-Phenylalanine, 4-[2-amino-6-[(1R)-2,2,2-trifluoro-1-(3'-methoxy[1,1'-biphenyl]-4-yl)ethoxy]-4-pyrimidinyl]-

(-20℃)

With Ice Pack

≥ 2 years