| 中文名称: | RAD-140 | ||||
|---|---|---|---|---|---|
| 英文名称: | RAD140 | ||||
| 别名: | 2-氯-4-[[(1R,2S)-1-[5-(4-氰基苯基)-1,3,4-恶二唑-2-基]-2-羟基丙基]氨基]-3-甲基苯甲腈;2-氯-4-(((1R,2S)-1-(5-(4-氰苯基)-1,3,4-恶二唑-2-基)-2-羟丙基)氨基)-3-甲基苯甲腈;2-氯-4-[[(1R,2S)-1-[5-(4-氰基苯基)-1,3,4-恶二唑-2-基]-2-羟丙基]氨基]-3-甲基苄腈 RAD140;Testolone;OralSARMSMuscleBuildingRad140/TestoloneForIncreasingMuscleMass;2-Chloro-4-[[(1R,2S)-1-[5-(4-cyanophenyl)-1,3,4-oxadiazol-2-yl]-2-hydroxypropyl]amino]-3-methylbenzonitrile;CS-2554 | ||||
| CAS No: | 1182367-47-0 | 分子式: | C20H16ClN5O2 | 分子量: | 393.83 |
| CAS No: | 1182367-47-0 | ||||
| 分子式: | C20H16ClN5O2 | ||||
| 分子量: | 393.83 | ||||
熔点：
179-183℃
沸点：
687.7±65.0 °C(Predicted)
密度：
1.41±0.1 g/cm3(Predicted)
包装规格：
25mg 100mg 500mg 1g in glass bottle
产品简介：
一种选择性雄激素受体调节剂，研究证明能改善瘦体重和身体功能，会增加肌腱力量,促进韧带健康、骨密度增长。
溶解性：
DMSO :≥ 100 mg/mL(253.92 mM)
储备液保存：
-80°C, 2 years
-20°C, 1 year
-20°C, 1 year
体内实验：
1、请依序添加每种溶剂：10% DMSO→40% PEG300→5% Tween-80→45% Saline
Solubility: ≥ 2.5 mg/mL (6.35 mM); 澄清溶液
此方案可获得 ≥ 2.5 mg/mL（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；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 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-CD in Saline)
Solubility: 2.5 mg/mL (6.35 mM); 悬浊液; 超声助溶
此方案可获得 2.5 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。
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 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。
3、请依序添加每种溶剂：10% DMSO→90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.35 mM); 澄清溶液
此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
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 μL玉米油中，混合均匀。
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
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。
Solubility: ≥ 2.5 mg/mL (6.35 mM); 澄清溶液
此方案可获得 ≥ 2.5 mg/mL（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；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 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-CD in Saline)
Solubility: 2.5 mg/mL (6.35 mM); 悬浊液; 超声助溶
此方案可获得 2.5 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。
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 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。
3、请依序添加每种溶剂：10% DMSO→90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.35 mM); 澄清溶液
此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
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 μL玉米油中，混合均匀。
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
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。
靶点：
Ki: 7 nM (Androgen receptor)
体外研究：
Vosilasarm (0-300 nM; pretreated for 1 hour) increases neuron viability against Aβ in a concentration-dependent manner.
Vosilasarm (100 nM; 1 hour) protects cultured neurons against apoptotic insults. Vosilasarm shows protective profiles of significantly protecting against neuronal death induced by Aβ and AAII, but not H2O2.
Vosilasarm (100 nM; 15 minutes) induces a significant increase in levels of phosphorylated but not total ERK in neuronal cultures.
Vosilasarm (100 nM; 1 hour) protects cultured neurons against apoptotic insults. Vosilasarm shows protective profiles of significantly protecting against neuronal death induced by Aβ and AAII, but not H2O2.
Vosilasarm (100 nM; 15 minutes) induces a significant increase in levels of phosphorylated but not total ERK in neuronal cultures.
体内研究：
The stability of Vosilasarm is high (t1/2 > 2 h) in incubations with rat, monkey, and human microsomes, and Vosilasarm also has good bioavailability in rats (F = 27-63%) and monkeys (65-75%).
In castrated immature rats, Vosilasarm (0.03-0.3 mg/kg; for 11 days) stimulates the levator ani bulbocavernosus muscle weight and prostate weight.
A high dose of Vosilasarm (10 mg/kg, p.o.) actually antagonizes the effect of testosterone propionate (TP) at 1 mg/kg on the seminal vesicles but adds to the effect of TP on the levator ani muscle. The effective dose for achieving antagonism by Vosilasarm is 0.3-1 mg/kg (p.o.) for 1 mg/kg TP (s.c.). In the young castrate male rat model, Vosilasarm appears to be a potent and complete androgen agonist on the levator ani, but a weaker, partial antagonist on the seminal vesicle and possibly the prostate.
Vosilasarm is neuroprotective in vivo using the rat kainate lesion model. In experiments with gonadectomized, adult male rats, Vosilasarm is shown to exhibit peripheral tissue-specific androgen action that largely spared prostate, neural efficacy as demonstrated by activation of androgenic gene regulation effects, and neuroprotection of hippocampal neurons against cell death caused by systemic administration of the excitotoxin kainate.
In castrated immature rats, Vosilasarm (0.03-0.3 mg/kg; for 11 days) stimulates the levator ani bulbocavernosus muscle weight and prostate weight.
A high dose of Vosilasarm (10 mg/kg, p.o.) actually antagonizes the effect of testosterone propionate (TP) at 1 mg/kg on the seminal vesicles but adds to the effect of TP on the levator ani muscle. The effective dose for achieving antagonism by Vosilasarm is 0.3-1 mg/kg (p.o.) for 1 mg/kg TP (s.c.). In the young castrate male rat model, Vosilasarm appears to be a potent and complete androgen agonist on the levator ani, but a weaker, partial antagonist on the seminal vesicle and possibly the prostate.
Vosilasarm is neuroprotective in vivo using the rat kainate lesion model. In experiments with gonadectomized, adult male rats, Vosilasarm is shown to exhibit peripheral tissue-specific androgen action that largely spared prostate, neural efficacy as demonstrated by activation of androgenic gene regulation effects, and neuroprotection of hippocampal neurons against cell death caused by systemic administration of the excitotoxin kainate.
注意事项：
1、为了您的安全和健康，请穿实验服并戴一次性手套操作。
2、以上信息仅做参考交流之用。
2、以上信息仅做参考交流之用。
保存条件：
-20°C
UN码：
HazardClass：
危害声明：
安全说明：
搜索质检报告(COA)
参考文献 & 客户发表文献
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
