LP533401 hcl
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.
LP533401 hcl是Tph-1的抑制剂[1].
色氨酸羟化酶-1(Tph-1)是色氨酸羟化酶的同功酶,是肠道和肺源性血清素生物合成的起始酶.Tph-1主要表达在肠和肺中[2].
LP533401 hcl是Tph-1的抑制剂.在表达Tph1的大鼠RBL2H3细胞中,1 μM的LP533401完全抑制血清素的生成.LP533401通过与残基Tyr235和Phe241相互作用,减少70％的重组野生型TPH-1的活性[1].
在啮齿类动物中,口服给药LP533401无法透过血脑屏障.在小鼠中,250 mg/kg 的LP533401剂量依赖性地降低血清中30％的血清素浓度.在切除卵巢的雌性C57BL6/J小鼠中,10\100和250 mg/kg剂量的LP533401处理 28天,增加骨质量和骨形成参数,如骨钙素血清浓度\成骨细胞数目和骨形成率.此外,LP533401剂量依赖性地降低血清中血清素浓度,但并没有影响大脑血清素的含量.在切除卵巢的雌性大鼠中,LP533401完全恢复了卵巢切除引发的骨质疏松[1].在SM22-5-HTT+转基因小鼠中,平滑肌细胞过表达5-HT转运体(5-HTT),具有自发发展的肺动脉高压(PH),250 mg/kg的LP533401持续给药21天,显著降低肺和血液中的5-HT水平\血管Ki67阳性细胞\远端肺动脉血管\右心室(RV)肥大和右心室收缩压[2].
参考文献：
[1]. Yadav VK, Balaji S, Suresh PS, et al. Pharmacological inhibition of gut-derived serotonin synthesis is a potential bone anabolic treatment for osteoporosis. Nat Med, 2010, 16(3): 308-312.
[2]. Abid S, Houssaini A, Chevarin C, et al. Inhibition of gut- and lung-derived serotonin attenuates pulmonary hypertension in mice. Am J Physiol Lung Cell Mol Physiol, 2012, 303(6): L500-508.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 562.94 |
| Cas No. | 1040526-12-2 |
| Formula | C27H23ClF4N4O3 |
| Solubility | ≥56.3 mg/mL in DMSO; insoluble in H2O; ≥19.4 mg/mL in EtOH |
| Chemical Name | (2S)-2-amino-3-(4-(2-imino-6-(2,2,2-trifluoro-1-(3'-fluoro-[1,1'-biphenyl]-4-yl)ethoxy)-2,3-dihydropyrimidin-4-yl)phenyl)propanoic acid hydrochloride |
| SDF | Download SDF |
| Canonical SMILES | FC1=CC=CC(C2=CC=C(C(OC(C=C(N3)C4=CC=C(C[C@@](N)([H])C(O)=O)C=C4)=NC3=N)([H])C(F)(F)F)C=C2)=C1.Cl |
| 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。 |
质量控制和MSDS
- 批次:
化学结构
