LY2452473是一种选择性雄激素受体（AR）调节剂（SARM）。
Cas No.:1029692-15-6
Sample solution is provided at 25 µL, 10mM.
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LY2452473 is a selective androgen receptor modulator (SARM)[1-2]. LY2452473 can be used in research related to prostate cancer and hypogonadism-associated conditions[3-4].
In vitro, PC12 cells were treated with LY2452473 (0.1nM-10µM) for 12 hours. LY2452473 dose-dependently and highly selectively antagonized AR activity and inhibited the MAPK signaling pathway. Additionally, LY2452473 activated the cAMP signaling pathway[5].
References:
[1] Mazzarino M, Di Costanzo L, Comunità F, et al. UHPLC-HRMS Method for the Simultaneous Screening of 235 Drugs in Capillary Blood for Doping Control Purpose: Comparative Evaluation of Volumetric and Non-volumetric Dried Blood Spotting Devices. ACS Omega. 2022 Aug 29;7(36):31845-31868
[2] Stacchini C, Botrè F, Comunità F, et al. Simultaneous detection of different chemical classes of selective androgen receptor modulators in urine by liquid chromatography-mass spectrometry-based techniques. J Pharm Biomed Anal. 2021 Feb 20;195:113849.
[3] Piper T, Heimbach S, Adamczewski M, et al. An in vitro assay approach to investigate the potential impact of different doping agents on the steroid profile. Drug Test Anal. 2021 May;13(5):916-928.
[4] Karatt TK, Sathiq MA, Laya S, et al. Metabolic study of selective androgen receptor modulator LY2452473 in thoroughbred horses for doping control. Rapid Commun Mass Spectrom. 2023 May 15;37(9):e9491.
[5] Popović L, Brankatschk B, Palladino G, et al. Polypharmacological profiling across protein target families and cellular pathways using the multiplexed cell-based assay platform safetyProfiler reveals efficacy, potency and side effects of drugs. Biomed Pharmacother. 2024 Nov;180:117523.
LY2452473是一种选择性雄激素受体（AR）调节剂（SARM） [1-2]。LY2452473可用于前列腺癌和与性腺功能减退相关疾病的研究[3-4]。
在体外，LY2452473（0.1nM-10μM）处理PC12细胞12小时。LY2452473可剂量依赖性地、高选择性地拮抗Ar的活性和抑制MAPK信号通路，LY2452473可激活cAMP信号通路[5]。
| Cell experiment [1]: | |
Cell lines | PC12 cells (rat pheochromocytoma cell line) |
Preparation Method | Cells were cultured in medium supplemented with 10% fetal bovine serum (FBS). Cells were treated with the LY2452473 (0.1nM-10μM) for 12h. |
Reaction Conditions | 0.1nM-10μM; 12h. |
Applications | LY2452473 dose-dependently antagonized AR activity and MAPK signaling pathway. LY2452473 activated the cAMP signaling pathway. |
References: | |
| Cas No. | 1029692-15-6 | SDF | |
| Canonical SMILES | O=C(N[C@@H]1CC(N(C2=C3C=C(C=C2)C#N)CC4=NC=CC=C4)=C3C1)OC(C)C | ||
| 分子式 | C22H22N4O2 | 分子量 | 374.44 |
| 溶解度 | DMSO : 62.5 mg/mL (166.92 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 | 2.6707 mL | 13.3533 mL | 26.7065 mL |
| 5 mM | 534.1 μL | 2.6707 mL | 5.3413 mL |
| 10 mM | 267.1 μL | 1.3353 mL | 2.6707 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
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- Purity: >98.00% Appearance: A solid
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