Vosilasarm (RAD140) is a potent, orally active, nonsteroidal selectiveandrogen receptormodulator (SARM) with aK_iof 7 nM. Vosilasarm shows good selectivity over other steroid hormone nuclear receptors^[1].

Ki: 7 nM (Androgen receptor)^[1]

Vosilasarm (0-300 nM; pretreated for 1 hour) increases neuron viability against Aβ in a concentration-dependent manner^[2].
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^[2].
Vosilasarm (100 nM; 15 minutes) induces a significant increase in levels of phosphorylated but not total ERK in neuronal cultures^[2].

The stability of Vosilasarm is high (t_1/2>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%)^[1].
In castrated immature rats, Vosilasarm (0.03-0.3 mg/kg; for 11 days) stimulates the levator ani bulbocavernosus muscle weight and prostate weight^[1].
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^[1].
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^[2].

393.83

Solid

C₂₀H₁₆ClN₅O₂

1182367-47-0

Room temperature in continental US; may vary elsewhere.

DMSO : ≥ 100 mg/mL(253.92 mM)

*"≥" means soluble, but saturation unknown.

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。

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 (6.35 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (6.35 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。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液
• 2.

  请依序添加每种溶剂： 10% DMSO    90% (20%SBE-β-CDin saline)

  Solubility: 2.5 mg/mL (6.35 mM); Suspended solution; Need ultrasonic

  此方案可获得 2.5 mg/mL (6.35 mM) 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 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
• 3.

  请依序添加每种溶剂： 10% DMSO    90%corn oil

  Solubility: ≥ 2.5 mg/mL (6.35 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (6.35 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  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。