GTx-007 (S-4) 是具有口服活性的、选择性的非甾体受体雄激素受体(AR)调节剂 (SARM) 和部分激动剂,Ki为4 nM。GTx-007 (S-4) 是具有较强活性的、具有组织选择性的 SARM。
生物活性 | GTx-007 (S-4) is an orally active and selective nonsteroidalandrogen receptor(AR)modulator (SARM) and a partial agonist, withKiof 4 nM. GTx-007 (S-4) is identified as SARMs with potent and tissue-selective in vivo pharmacological activity[1][2]. |
体内研究 (In Vivo) | GTx-007 (S-4) is only a partial agonist in the prostate and seminal vesicles, restoring them to 33.8 and 28.2% of intact animals, respectively[2]. GTx-007 significantly increased uterine expression ofWnt4andWnt7a[2].
Animal Model: | Female C57BL/6J mice[2]. | Dosage: | 0.5 mg/mouse. | Administration: | Seven daily subcutaneous injections. | Result: | Resulted in a highly heterogeneous pattern of AR expression in all compartments, with a significant increase of AR-positive cells in the luminal epithelium compared to VC. Had approximately ten glands per uterine cross-section within an endometrium, with a compact stroma, consistent with overall endogenous steroid depletion. Did not detect any impact of GTx-007 on body weight.
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : ≥ 100 mg/mL(226.57 mM) *"≥" means soluble, but saturation unknown. 配制储备液 1 mM | 2.2657 mL | 11.3286 mL | 22.6572 mL | 5 mM | 0.4531 mL | 2.2657 mL | 4.5314 mL | 10 mM | 0.2266 mL | 1.1329 mL | 2.2657 mL |
*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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (5.66 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.66 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (5.66 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.66 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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