G15 是一种高亲和力和选择性 G 蛋白偶联雌激素受体(GPER/GPR30)拮抗剂，Ki值为 20 nM。
| 生物活性 | G15 is a high affinity and selectiveG-protein-coupledestrogen receptor(GPER/GPR30)antagonist with aKiof 20 nM[1][2]. |
| IC50& Target | Ki: 20 nM (GPER/GPR30)[2] |
体外研究
(In Vitro) | G15 (0.1-10 μM; 2 days) inhibits GPER-mediated proliferation stimulated by 17β-estradiol (E2) in A549 and H1793 cell lines[1].
G15 (1 μM; 48 hours) inhibits the response of GPER stimulated by E2 and G1 in A549 and H1793 cell lines[1].
Cell Proliferation Assay[1] | Cell Line: | A549, H1793 cell lines | | Concentration: | 0.1, 1, 10 μM (combination with 10 nM E2) | | Incubation Time: | 2 days | | Result: | Inhibited GPER-mediated proliferation stimulated by E2. |
Western Blot Analysis[1] | Cell Line: | A549, H1793 cell lines | | Concentration: | 1 μM (combination with 10 nM E2 and 10 nM G1) | | Incubation Time: | 48 hours | | Result: | Inhibited the response of GPER stimulated by E2 and G1. |
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体内研究
(In Vivo) | G15 (1.46 mg/kg; i.h.; twice a week for 14 weeks) decreases the number of tumor nodules and tumor index increased by the E2 or G1 group in urethane-induced adenocarcinoma mice[1].
| Animal Model: | Four-week-old female Kunming mice (Urethane-induced adenocarcinoma)[1] | | Dosage: | 1.46 mg/kg (combination with E2, 0.09 mg/kg and fulvestrant (Ful), 2.4 mg/kg) | | Administration: | Subcutaneous injection; twice a week for 14 weeks | | Result: | The number of tumor nodules decreased in the E2+Ful+G15 group. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | -20°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| 溶解性数据 | In Vitro: DMSO : 41.67 mg/mL(112.55 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.7010 mL | 13.5048 mL | 27.0095 mL | | 5 mM | 0.5402 mL | 2.7010 mL | 5.4019 mL | | 10 mM | 0.2701 mL | 1.3505 mL | 2.7010 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 (protect from 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: ≥ 2.08 mg/mL (5.62 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.62 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 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%corn oil Solubility: ≥ 2.08 mg/mL (5.62 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.62 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 20.8 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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