LXR-623
(Synonyms: 2-[(2-氯-4-氟苯基)甲基]-3-(4-氟苯基)-7-(三氟甲基)-2H-吲唑,WAY 252623) 目录号 : GC13954
An LXR modulator
Cas No.:875787-07-8
Sample solution is provided at 25 µL, 10mM.
LXR-623 is an agonist of liver X-receptor with IC50 values of 179nM and 24nM for LXR-α and LXR-β, respectively [1].
LXR-623 is a partial agonist of LXR which regulates the transcription of genes involved in cellular cholesterol homeostasis. As the LXR agonist, LXR-623 is used to enhance reverse cholesterol transport through up-regulating cholesterol transporters. To rodents, orally dosed LXR-623 increases the transcription level of ABCA1 and ABCG1 in peripheral blood cells. To human, LXR-623 also significantly increases ABCA1 and ABCG1 both in PBMC cells and in T- and B-cells. In addition, in mouse model of atherosclerosis, LXR-623 is found to up-regulate intestinal ABCG5 and ABCG8. In cynomolgus monkeys, LXR-623 up-regulates ABCA1 and ABCG1 in whole blood. Besides that, LXR-623 is proposed to be used in treatment of Alzheimer’s disease since it can lower the level of amyloid-βin brain [1, 2].
References:
[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.
| Cell experiment [1]: | |
|
Cell lines |
Human peripheral blood mononuclear cells |
|
Preparation method |
The solubility of this compound in DMSO is >19.4mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
|
Reacting condition |
2 μM, 18 hours |
|
Applications |
LXR-623 (2 μM for either 24 or 48 hours) treatment significantly upregulated mRNA for ABCA1, ABCG1, and PLTP in human PBMC. In PBMC, monocytes, T cells, and B cells, treatment with 2 μM LXR-623 for 18 hours resulted in approximately 6 fold induction of ABCA1 mRNA levels. |
| Animal experiment [1]: | |
|
Animal models |
C57/Bl6 mice, Normal male rats |
|
Dosage form |
Oral administration, 50 mg/kg, 30 mg/kg |
|
Application |
Oral administration of LXR-623 (30 mg/kg) induced ABCA1 and ABCG1 gene expression in rodent peripheral blood cells in vivo. |
|
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
|
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. | |
| Cas No. | 875787-07-8 | SDF | |
| 别名 | 2-[(2-氯-4-氟苯基)甲基]-3-(4-氟苯基)-7-(三氟甲基)-2H-吲唑,WAY 252623 | ||
| 化学名 | 2-[(2-chloro-4-fluorophenyl)methyl]-3-(4-fluorophenyl)-7-(trifluoromethyl)indazole | ||
| 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 | ||
| 分子式 | C21H12ClF5N2 | 分子量 | 422.78 |
| 溶解度 | ≥ 19.4mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.3653 mL | 11.8265 mL | 23.653 mL |
| 5 mM | 0.4731 mL | 2.3653 mL | 4.7306 mL |
| 10 mM | 0.2365 mL | 1.1826 mL | 2.3653 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet