Enclomiphene ((E)-Clomiphene) citrate 是一种有效的、可口服的非甾体雌激素受体 (estrogen receptor) 拮抗剂,具有抗雌激素作用。Enclomiphene citrate 可用于卵巢功能障碍、睾酮缺乏、男性性腺功能减退症和 type 2 型糖尿病的相关研究。
生物活性 | Enclomiphene ((E)-Clomiphene) citrate is a potent and orally active non-steroidalestrogen receptorantagonist, with antioestrogenic property. Enclomiphene citrate can be used for the research of ovarian dysfunction, testosterone deficiency, male hypogonadism and type 2 diabetes[1]. |
体外研究 (In Vitro) | Enclomiphene citrate (0-100 μM, 6 h) dose-dependently inhibits basal and gonadotrophin-stimulated small and large ovine luteal cell progesterone secretion[2]. Enclomiphene citrate (0-100 μg/mL, 24 h) dose-dependently inhibits fertilization rates, blastocyst formation rates, and degeneration rates in mouse oocytes[3]. Enclomiphene citrate (1 nM-10 μM, 6 h) dose-dependently decreases E2-induced inhibition of follicle stimulating hormone (FSH) secretion in primary sheep pituitary cells[4].
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体内研究 (In Vivo) | Enclomiphene citrate (subcutaneous injection, 0.25 and 0.5 mg/animal, daily) inhibits spermatogenesis and decreases serum luteinizing hormone (LH) and testosterone levels in intact or castrated rats[5]. Enclomiphene citrate (oral adminstration, 0.03-3 mg/kg, daily for 90 days) reductes body weight to sham levels, and reduced serum cholesterol[6].
Animal Model: | 21 days-old Charles River male rats[5] | Dosage: | 0.25 and 0.5 mg/animal, daily for 24 days. | Administration: | Subcutaneous injection | Result: | Decreased LH and testosterone levels in the serum. |
Animal Model: | OVX (ovariectomy) rat model[6] | Dosage: | 0.03, 1, and 3 mg/kg, daily for 90 days. | Administration: | Oral adminstration | Result: | Reducted body weight to sham levels, and reduced serum cholesterol. Showed dose-dependent effects on the proximal tibia with BMD and BMC approaching posttreatment Sham levels. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) |
溶解性数据 | In Vitro: DMSO : ≥ 50 mg/mL(83.60 mM) *"≥" means soluble, but saturation unknown. 配制储备液 1 mM | 1.6720 mL | 8.3601 mL | 16.7202 mL | 5 mM | 0.3344 mL | 1.6720 mL | 3.3440 mL | 10 mM | 0.1672 mL | 0.8360 mL | 1.6720 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 (sealed storage, away from moisture and light)。-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: ≥ 0.83 mg/mL (1.39 mM); Clear solution
此方案可获得 ≥ 0.83 mg/mL (1.39 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 8.3 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: ≥ 0.83 mg/mL (1.39 mM); Clear solution
此方案可获得 ≥ 0.83 mg/mL (1.39 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 8.3 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。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 0.83 mg/mL (1.39 mM); Clear solution
此方案可获得 ≥ 0.83 mg/mL (1.39 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 8.3 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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