LXR-623
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.
LXR-623是一种肝X受体激动剂,对LXR-α和LXR-β的IC50值分别为179 nM和24 nM[1].
LXR-623是LXR的部分激动剂,可以调节细胞胆固醇稳态相关基因的转录.作为LXR 的激动剂,LXR-623可以上调胆固醇转运体,从而促进胆固醇逆向转运.在啮齿动物中,口服给予LXR-623提升外周血细胞中的ABCA1和ABCG1转录水平.在人类中,LXR-623也显著增加PBMC\T细胞以及B细胞中的ABCA1和ABCG1.据发现,在动脉粥样硬化小鼠模型中,LXR-623上调肠ABCG5与ABCG8.在食蟹猴中,LXR-623上调全血中的ABCA1和ABCG1.此外,LXR-623可以降低脑中的β-淀粉样蛋白水平,有望用于治疗阿尔茨海默氏病[1,2].
参考文献：
[1] Katz A, Udata C, Ott E, et al. Safety, Pharmacokinetics, and Pharmacodynamics of Single Doses of LXR‐623, a Novel Liver X‐Receptor Agonist, in Healthy Participants. The Journal of Clinical Pharmacology, 2009, 49(6): 643-649.
[2] DiBlasio-Smith E A, Arai M, Quinet E M, et al. Discovery and implementation of transcriptional biomarkers of synthetic LXR agonists in peripheral blood cells. J Transl Med, 2008, 6: 59.
- 1. Jing Zeng, Daitze Wu, et al. "Activation of the liver X receptor pathway inhibits HBV replication in primary human hepatocytes." Hepatology. 2020 Dec;72(6):1935-1948. PMID: 32145089
- 2. Xu D, He H, et al. "SIRT2 plays a novel role on progesterone, estradiol and testosterone synthesis via PPARs/LXRα pathways in bovine ovarian granular cells." J Steroid Biochem Mol Biol. 2018 Aug 7. pii: S0960-0760(18)30023-2. PMID: 30009951
- 3. Xian X, Ding Y, et al. "LRP1 integrates murine macrophage cholesterol homeostasis and inflammatory responses in atherosclerosis."Elife. 2017 Nov 16;6. pii: e29292. PMID: 29144234
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 422.78 |
| Cas No. | 875787-07-8 |
| Formula | C21H12ClF5N2 |
| Solubility | insoluble in H2O; ≥15.49 mg/mL in EtOH with ultrasonic; ≥19.4 mg/mL in DMSO |
| Chemical Name | 2-[(2-chloro-4-fluorophenyl)methyl]-3-(4-fluorophenyl)-7-(trifluoromethyl)indazole |
| SDF | Download SDF |
| Canonical SMILES | C1=CC2=C(N(N=C2C(=C1)C(F)(F)F)CC3=C(C=C(C=C3)F)Cl)C4=CC=C(C=C4)F |
| 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。 |
| 细胞实验 [1]: | |
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细胞系 |
人外周血单核细胞 |
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溶解方法 |
该化合物在DMSO中的溶解度大于19.4 mg/mL。若获取更高浓度的溶液，可在37℃下孵育10分钟，随后在超声波浴中摇匀。-20℃以下可储存数月。 |
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反应条件 |
2 μM，18小时 |
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应用 |
LXR-623（2 μM，24小时或48小时）显著上调人PBMC中ABCA1、ABCG1和PLTP的mRNA表达。在PBMC、单核细胞、T细胞和B细胞中，2 μM LXR-623处理18小时导致ABCA1 mRNA水平增加约6倍。 |
| 动物实验 [1]: | |
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动物模型 |
C57/Bl6小鼠，正常雄性大鼠 |
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给药剂量 |
口服，50 mg/kg，30 mg/kg |
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应用 |
在大鼠中，口服LXR-623 (30 mg/kg)诱导外周血细胞中ABCA1和ABCG1基因表达。 |
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注意事项 |
由于实验环境的不同，实际溶解度可能与理论值略有不同，请测试室内所有化合物的溶解度。 |
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References: [1]. DiBlasio-Smith E A, Arai M, Quinet E M, et al. Discovery and implementation of transcriptional biomarkers of synthetic LXR agonists in peripheral blood cells[J]. Journal of translational medicine, 2008, 6(1): 59. |
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质量控制和MSDS
- 批次:
化学结构
相关生物数据
相关生物数据
