G-1 is a nonsteroidal, high-affinity and selective agonist of GPR30 with a K_i of 11 nM.

Ki: 11 nM (GPR30)^[1]

G-1 is a nonsteroidal, high-affinity and selective agonist of GPR30 with a K_i of 11 nM^[1]. Treatment with G-1 (10 μM and 100 μM) for 48 and 72 h significantly decreases cell proliferation (P<0.001). At 72 h, the IC₅₀ value for G-1 is calculated to be 20 μM. Treatment of A549 cells with G-1 at a concentration of 20 μM reveals a significant increase in apoptosis, consistent with its antiproliferative effect (P<0.001)^[2]. Cell cycle analysis of H295R cells after 24 h of G-1 treatment demonstrates a cell cycle arrest in the G₂ phase. The presence of G-1 increases Bax expression while decreases Bcl-2^[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

The results at 14 days post-injury show that the Basso mouse scale (BMS) scores are significantly higher in the G-1 group compared with the other groups (P<0.05). The number of caspase-3-positive cells in the cross sections is counted, and G-1 group has fewer positive cells compare with the other groups (P<0.05), and there is no difference between the two groups (P>0.05)^[1]. G-1 administration produces a statistically significant decrease in tumor volume from day 14 post treatment. Grafted tumors harvested after three-week treatment with G-1 show a significant decrease in tumor weight compare to vehicle treated animals^[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

412.28

C₂₁H₁₈BrNO₃

881639-98-1

Room temperature in continental US; may vary elsewhere.

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

In Vitro: 

DMSO : 50 mg/mL (121.28 mM; Need ultrasonic)

*

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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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 (6.06 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (6.06 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-CD in saline)

  Solubility: 2.5 mg/mL (6.06 mM); Suspended solution; Need ultrasonic

  此方案可获得 2.5 mg/mL (6.06 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 μL 20% 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 (6.06 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (6.06 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。

• [1]. Cheng Q, et al. G-1 exerts neuroprotective effects through G protein-coupled estrogen receptor 1 following spinal cord injury in mice. Biosci Rep. 2016 Aug 31;36(4). pii: e00373.

  [2]. Kurt AH, et al. Oxidative/antioxidative enzyme-mediated antiproliferative and proapoptotic effects of the GPER1 agonist G-1 on lung cancer cells. Oncol Lett. 2015 Nov;10(5):3177-3182.

  [3]. Chimento A, et al. GPER agonist G-1 decreases adrenocortical carcinoma (ACC) cell growth in vitro and in vivo. Oncotarget. 2015 Aug 7;6(22):19190-203.

A549 human lung cancer cells are treated with various concentrations (10 nM, 100 nM, 1 μM, 10 μM and 100 μM) of G-1 in 96-well plates and incubated for 48 or 72 h. Following incubation, MTT solution is added to each well at a concentration of 0.5 mg/mL, and incubated for 4 h at 37°C. At the end of this period, 100 µL DMSO solvent is added to each well. The absorbance values [optical density (OD)] at 570 nm of the solution in each well are read using a spectrophotometer^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Four-week-old nu/nu-Forkhead box N1^nu female mice are used in this study. H295R cells, 6×10⁶, suspended in 100 μL PBS, are combined with 30 μL of Matrigel (4 mg/mL) and injected subcutaneously in the shoulder of each animal. Mice are treated 21 days after cell injection, when tumors have reached an average volume of about 200 mm³. Animals are randomly assigned to be treated with vehicle or G-1 at a concentration of 2 mg/kg/daily. Drug tolerability is assessed in tumor-bearing mice in terms of: a) lethal toxicity, i.e. any death in treated mice occurring before any death in control mice; b) body weight loss percentage=100-[(body weight on day x/body weight on day 1)×100], where x represents a day during the treatment period. Animals are sacrificed by cervical dislocation 42 days after cell injection^[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

• [1]. Cheng Q, et al. G-1 exerts neuroprotective effects through G protein-coupled estrogen receptor 1 following spinal cord injury in mice. Biosci Rep. 2016 Aug 31;36(4). pii: e00373.

  [2]. Kurt AH, et al. Oxidative/antioxidative enzyme-mediated antiproliferative and proapoptotic effects of the GPER1 agonist G-1 on lung cancer cells. Oncol Lett. 2015 Nov;10(5):3177-3182.

  [3]. Chimento A, et al. GPER agonist G-1 decreases adrenocortical carcinoma (ACC) cell growth in vitro and in vivo. Oncotarget. 2015 Aug 7;6(22):19190-203.