GLPG0492
目录号 : GC30086
A selective androgen receptor modulator
Cas No.:1215085-92-9
Sample solution is provided at 25 µL, 10mM.
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GLPG0492 is a selective androgen receptor modulator (SARM).1 It activates the androgen receptor in a transactivation assay (EC50 = 12 nM in HeLa cells expressing the human receptor). GLPG0492 (10 mg/kg per day) increases levator ani muscle weight, a marker of anabolic activity, but has no effect on ventral prostate weight, a marker of androgenic activity, in castrated rats. It increases twitch tension in isolated diaphragm strips, as well as increases the total distance run in a treadmill test and decreases gastrocnemius muscle fibrosis in the exercised-mdx mouse model of muscular dystrophy when administered at a dose of 30 mg/kg.2 GLPG0492 also reverses immobilization-induced muscle atrophy in a mouse model of hindlimb immobilization.3
1.Nique, F., Hebbe, S., Triballeau, N., et al.Identification of a 4-(hydroxymethyl)diarylhydantoin as a selective androgen receptor modulatorJ. Med. Chem.55(19)8236-8247(2012) 2.Cozzoli, A., Capogrosso, R.F., Sblendorio, V.T., et al.GLPG0492, a novel selective androgen receptor modulator, improves muscle performance in the exercised-mdx mouse model of muscular dystrophyPharmacol. Res.729-24(2013) 3.Blanqué, R., Lepescheux, L., Auberval, M., et al.Characterization of GLPG0492, a selective androgen receptor modulator, in a mouse model of hindlimb immobilizationBMC Musculoskelet. Disord.15:291(2014)
| Cas No. | 1215085-92-9 | SDF | |
| Canonical SMILES | N#CC1=CC=C(N(C(N(C)[C@]2(CO)C3=CC=CC=C3)=O)C2=O)C=C1C(F)(F)F | ||
| 分子式 | C19H14F3N3O3 | 分子量 | 389.33 |
| 溶解度 | DMSO : ≥ 50 mg/mL (128.43 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 | 2.5685 mL | 12.8426 mL | 25.6852 mL |
| 5 mM | 0.5137 mL | 2.5685 mL | 5.137 mL |
| 10 mM | 0.2569 mL | 1.2843 mL | 2.5685 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