
- LX1606
- Telotristat
LX-1031TPH inhibitor |
Sample solution is provided at 25 µL, 10mM.
































Quality Control & MSDS
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- Purity = 99.50%
- COA (Certificate Of Analysis)
- HPLC (Retest)
- NMR (Nuclear Magnetic Resonance)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure

Description | LX-1031 is an oral, small molecule inhibitor of tryptophan 5-hydroxylase (TPH). | |||||
Targets | TPH | |||||
IC50 |

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Cas No. | 945976-76-1 | SDF | Download SDF |
Synonyms | LX1031; LX 1031 | ||
Chemical Name | (2S)-2-amino-3-[4-[2-amino-6-[(1R)-2,2,2-trifluoro-1-[4-(3-methoxyphenyl)phenyl]ethoxy]pyrimidin-4-yl]phenyl]propanoic acid | ||
Canonical SMILES | COC1=CC=CC(=C1)C2=CC=C(C=C2)C(C(F)(F)F)OC3=NC(=NC(=C3)C4=CC=C(C=C4)CC(C(=O)O)N)N | ||
Formula | C28H25F3N4O4 | M.Wt | 538.52 |
Solubility | ≥26.9 mg/mL in DMSO, <2.45 mg/ml="" in="" etoh,="">2.45><2.55 mg/ml="" in="" h2o="">2.55> | Storage | Store at -20°C |
Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. |
Tryptophan hydroxylase (TPH) is a key enzyme in the synthesis of serotonin. Serotonin plays important physiological roles both peripherally and centrally. LX-1031 is a heterocyclic substituted phenylalanine analog, an oral small molecule tryptophan hydroxylase (TPH) inhibitor that reduces synthesis of serotonin (5-HT) peripherally and is being developed for conditions characterized by excess 5-HT expression such as diarrhea-predominant irritable bowel syndrome (IBS-D) and, possibly, carcinoid diarrhea.
In vitro: LX-1031 inhibits TPH1 at its concentration of 10-8–10-7 mol L-1 range [1].
In vivo: With oral administration of LX-1031 in mice, the 5-HT reductions in the jejunum relative to control were ~33%, 51%, and 66% with the 15, 45 and 135 mg/kg/day doses, respectively; the effect of 5 mg/kg/day on GI 5-HT content was not significantly different from control [2].
Clinical trial: In double-blind studies (doses of LX-1031 ranging from 250 to 1000 mg q.i.d.), average 5HIAA reductions of 33% were noted. In phase I studies, 54 healthy volunteers received the drug for up to 14 days while the diet was strictly controlled to avoid 5-HT-rich foods. Twenty four hour urine collections were obtained. Significant reductions in urinary 5-HIAA persisted over the duration of exposure [3].
References:[1] Camilleri M. LX-1031, a tryptophan 5-hydroxylase inhibitor, and its potential in chronic diarrhea associated with increased serotonin. Neurogastroenterol Motil. 2011;23(3):193-200. [2] Brown PM, Jackson JI, Frazier KS, Turner CA, Shi ZC, Liu Q. From mouse knockout to investigational drug: LX1031, a novel potential treatment for irritable bowel syndrome. Am J Gastroenterol 2007; 102: S961 (Abstract).[3] Freiman J, Jackson J, Frazier KS, Yang QM, Liu Q, Brown P. LX1031: inhibition of 5-HT synthesis as a new target in the management of irritable bowel syndrome (IBS). Neurogastroenterol Motil 2009; 21: 250.
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看我的回答:
抗原(antigen, Ag)是一类能诱导免疫系统发生免疫应答,并能与免疫应答的产物(抗体或效应细胞)发生特异性结合的物质。抗原具有免疫原性和反应原性两种性质。
免疫原性是指抗原刺激机体后,机体免疫系统能形成抗体或致敏T淋巴细胞的特异性免疫反应。
反应原性是指产生的抗体或致敏T淋巴细胞能与抗原进行特异性结合的免疫反应。
既具免疫原性又具反应原性的抗原称免疫原。某种物质之所以能成为一个良好的免疫原,是因为它有特异的化学结构,这就是抗原决定簇。抗原决定簇可以与相应的淋巴细胞表面的受体蛋白结合引起免疫应答。一个抗原决定簇只能激活一种淋巴细胞(对于B细胞)只刺激产生一种类型抗体。一个抗原可以有一个或多个抗原决定簇。抗原功能性决定簇的总数称抗原结合价。抗原决定簇少,抗体与抗原结合就少,往往就见不到反应。天然抗原或复杂的半抗原决定簇往往多达几十个,因此可以与很多抗体分子交互结合。
有些分子本身没有免疫原性,不能引起免疫反应,但是如果把它们和某些载体分子,如蛋白质分子结合起来就有了免疫原性,就能使动物对这一复合分子产生特异的抗体。这种本身无免疫原性,但有反应原性,一旦把它与载体结合就有了免疫原性的物质,就称半抗原或不完全抗原。如寡糖,类脂和一些简单的化学物质等。吗啡就是一种半抗原,把它与蛋白分子结合起来,就可以使动物体产生相应抗体,此抗体可作为检测是否吸毒的试剂。
抗原相对分子量一般都在10X103以上,而在4X103以下者一般无免疫原性。在一定相对分子量范围内,分子量大者免疫原性强,这是因为:
1、相对分子量大,表面抗原决定簇就多,而淋巴细胞要求一定数量抗原决定簇刺激才能活化;
2、大分子化学结构稳定,在水中呈胶体,不易被机体破坏或排除,这样在体内存留时间就长,有利于持续刺激淋巴细胞。核酸本身免疫原性很低,但只要有5个核苷酸与蛋白质分子载体连接,就能刺激机体产生抗体。
抗原可分外源性抗原和内源性抗原两类,前者如细菌、病毒、花粉、各种毒素以及小型动植物;后者主要为机体从未接触过的物质或构象发生改变的自身成分,如变性的IgG重链、晶状体物质、精子、脑组织等。
抗体是人或动物受抗原物质(如细菌或其毒素、病毒等)刺激后,由浆细胞合成和分泌的一种特异性蛋白质。抗体是人体抵抗感染的一种重要武器。19世纪末,德国科学家Behring发明了用含白喉抗毒素的动物血清注射给白喉患儿,使其治愈。此后医学家们用含有不同抗体的动物血清或人血清来治疗或预防多种传染病。由于Behring开创了抗体治疗传染病的方法,对防治传染病作出了卓越贡献,本世纪初荣获诺贝尔医学奖。但传统的人工生产抗体的方法是将抗原物质(如细菌或其毒素等)注射给动物(如马、羊等),使动物产生针对该抗原物质的抗体。人们抽取免疫动物的血液,分离出含抗体的血清。这种体内生产抗体的传统方法有许多缺点。例如所获得的抗体不纯,不能连续生产,动物饲养与管理工作繁重等,故长期以来医学家们一直在探索在试管内(即体外)生产抗体的方法, 1976年英国剑桥大学两位科学家Milstein和Koh1er将小鼠骨髓瘤细胞与免疫小鼠的脾细胞杂交。小鼠骨髓瘤细胞能在体外无限增殖传代并能分泌无抗体活性的球蛋白;免疫小鼠脾细胞能产生针对某种抗原的抗体,但不能在体外无限增殖。将两者融合成一种杂交瘤细胞,后者继承了两个亲代细胞的特点,既可在体外无限增殖,又可产生针对某种抗原的抗休。一个杂交瘤细胞在体外不断增殖所形成的细胞集团,被称之为克隆。在同一克隆中所有的细胞产生相同的抗体,此抗体称之为单克隆抗体(简称McAb)。它是单一特异性的高纯度的抗体,可在体外连续大量生产。McAb在临床医学及基础医学领域发挥了巨大作用,给某些难治疾病的诊断、防治带来了新的希望。如针对某种肿瘤细胞的McAb与毒素、抗癌药物或放射性物质结合成复合物(医学上称为生物导弹),将此复合物注射到病人体内,可定向杀伤McAb所针对的肿瘤细胞,而对其它正常细胞则无作用,这是任何其它抗癌治疗方法办不到的。因此,单克隆抗体技术被誉为现代生物科学的一项革命性突破,是当今四大生物工程技术之一。由于Milstein和kohler的杰出贡献,1984年他俩共同获取了诺贝尔医学奖。

