LX-1031
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
色氨酸羟化酶（TPH）是血清素合成的关键酶。血清素在外周以及中枢均发挥着重要的生理作用。LX-1031，一种杂环取代的苯丙氨酸类似物，是口服的色氨酸羟化酶（TPH）小分子抑制剂，可以减少外周血清素（5-HT）合成，被研发用于5-HT过度表达相关疾病，如腹泻型肠易激综合征（IBS-D）和良性肿瘤腹泻。
体外：在10-8 ~ 10-7 mol L-1的浓度范围内，LX-1031抑制TPH1[1]。
体内：以15、45和135 mg/kg/day的剂量，口服给予小鼠LX-1031，实验组的空肠5-HT与对照组的相比，分别减少了~33%、51%和66%。胃肠道5-HT含量在5 mg/kg/day LX-1031组和对照组中没有显著差异[2]。
临床试验：在双盲研究（LX-1031剂量为250 ~ 1000 mg q.i.d.）中，5HIAA平均减少了33%。在I期临床试验中，54例健康志愿者接受长达14天的药物治疗，同时，其饮食严格受控（剔除富含5-HT的食物）。收集24小时的尿液。LX-1031显著地持续减少尿液中的5-HIAA[3]。
参考文献：
[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.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 538.52 |
| Cas No. | 945976-76-1 |
| Formula | C28H25F3N4O4 |
| Synonyms | LX1031; LX 1031 |
| Solubility | ≥26.93 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O |
| 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 |
| SDF | Download SDF |
| 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 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| Description | LX-1031是口服的5色氨酸羟化酶（TPH）小分子抑制剂。 | |||||
| 靶点 | TPH | |||||
| IC50 | ||||||
质量控制和MSDS
- 批次:
化学结构
