BMS-779788 (EXEL04286652)
(Synonyms: EXEL04286652; XL-652; BMS-788) 目录号 : GC31372
An LXR agonist
Cas No.:918348-67-1
Sample solution is provided at 25 µL, 10mM.
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BMS 779788 is a partial agonist of liver X receptor α (LXRα) and LXRβ (Kis = 68 and 14 nM, respectively, in a radioligand binding assay).1 It activates LXRα and LXRβ with EC50 values of 230 and 250 nM, respectively, in a transactivation assay. BMS 779788 increases expression of ATP-binding cassette transporter (ABCA1) in HeLa cells and isolated human and mouse whole blood (EC50s = 33, 1,200, and 120 nM, respectively). It also increases expression of Abca1 and Abcg2 in isolated mouse blood cells but does not increase plasma or hepatic triglycerides when administered at a dose of 10 mg/kg.
1.Kick, E., Martin, R., Xie, Y., et al.Liver X receptor (LXR) partial agonists: Biaryl pyrazoles and imidazoles displaying a preference for LXRβBioorg. Med. Chem. Lett.25(2)372-377(2015)
Animal experiment: | Monkeys: Male cynomolgus monkeys are used in the study. For a single-dose pharmacokinetic (PK)-pharmacodynamic (PD) study, 2 animals each are treated either with vehicle [0.5% carboxymethyl cellulose and 2% Tween 80 in purified water) or 1 mg/kg BMS-779788. For the 7 day PD study, 18 animals are randomized into 6 treatment groups (N=3/group; 3-6 kg) and received the following treatments at 7 AM daily for 7 days by oral gavage: vehicle, 10 mg/kg per day T0901317 and 0.3, 1, 3, or 10 mg/kg per day BMS-779788[1]. |
References: [1]. Kirchgessner TG, et al. Pharmacological characterization of a novel liver X receptor agonist with partial LXRα activity and a favorable window in nonhuman primates. J Pharmacol Exp Ther. 2015 Feb;352(2):305-14. | |
| Cas No. | 918348-67-1 | SDF | |
| 别名 | EXEL04286652; XL-652; BMS-788 | ||
| Canonical SMILES | OC(C)(C)C1=CN(C2=CC=C(C3=CC=CC(S(=O)(C)=O)=C3)C=C2)C(C(C)(C4=CC=CC=C4Cl)C)=N1 | ||
| 分子式 | C28H29ClN2O3S | 分子量 | 509.06 |
| 溶解度 | DMSO : ≥ 31 mg/mL (60.90 mM) | 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。 |
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| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9644 mL | 9.822 mL | 19.644 mL |
| 5 mM | 0.3929 mL | 1.9644 mL | 3.9288 mL |
| 10 mM | 0.1964 mL | 0.9822 mL | 1.9644 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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet