G-1
目录号 : GC12766
G-1 is a selective and potent agonist of GPR30 with EC50 value about 2 nM.
Cas No.:881639-98-1
Sample solution is provided at 25 µL, 10mM.
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G-1 is a selective and potent agonist of GPR30 with EC50 value about 2 nM [1].
G-1 treatment (10-5 and 10-4 M) for 48 and 72 h significantly decreased A549 cell proliferation, at 72 h, the IC50 value for G-1 was calculated to be 2×10-5 M [2]. G-1 treatment at a concentration of 2×10-5 M had no significant effect on CAT activity but led to a significant increase in SOD activity, GPx activity and NO level [2]. G-1 inhibited TNF-α and IL-6 release on primary human macrophages derived from monocytes treated with GM-CSF over 6 days. The agonist inhibited the induction of both cytokines with IC50 values of 209 nM and 317 nM, respectively [3]. G-1 was also able to inhibit LPS induction of TNF-α in a mouse macrophage cell line, RAW 264.7 [3].
G-1 (50 mg/kg/day, 21 days) administration significantly reduced the severity of actively induced experimental allergic encephalomyelitis (EAE). G-1 treatment reduced the qualitative degree of inflammation in the lumbar spinal cord. G-1 treatment reduced the fraction of CNS-infiltrating macrophages (CD45hiCD11b+) in three individually analyzed mice [3]. G-1 could exert protective effects on motoneurons. The intraperitoneal injection of the GPR30 agonist G-1 for 14 days induces neuroprotective effects similar with the same dose of E2 [4].
References:
[1]. Bologa C G, Revankar C M, Young S M, et al. Virtual and biomolecular screening converge on a selective agonist for GPR30[J]. Nature chemical biology, 2006, 2(4): 207-212.
[2]. Kurt A H, Çelik A, Kelleci B M. Oxidative/antioxidative enzyme-mediated antiproliferative and proapoptotic effects of the GPER1 agonist G-1 on lung cancer cells[J]. Oncology Letters, 2015, 10(5): 3177-3182.
[3]. Blasko E, Haskell C A, Leung S, et al. Beneficial role of the GPR30 agonist G-1 in an animal model of multiple sclerosis[J]. Journal of neuroimmunology, 2009, 214(1-2): 67-77.
[4]. Cheng Q, Meng J, Wang X, et al. G-1 exerts neuroprotective effects through G protein-coupled estrogen receptor 1 following spinal cord injury in mice[J]. Bioscience Reports, 2016, 36(4).
| Cell experiment [1]: | |
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Cell lines |
A549 human lung cancer cells |
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Preparation Method |
A549 human lung cancer cells were treated with various concentrations (10-8, 10-7, 10-6, 10-5 and 10-4 M) of 17β-estradiol and G-1 in 96-well plates and incubated for 48 or 72 h. Following incubation, MTT solution (Sigma-Aldrich) was added to each well at a concentration of 0.5 mg/ml, and incubated for 4 h at 37°C. |
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Reaction Conditions |
0.01-100 µM for 48 and 72 h |
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Applications |
Treatment with G-1 (10-5 and 10-4 M) for 48 and 72 h significantly decreased cell proliferation. |
| Animal experiment [2]: | |
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Animal models |
SJL mice (5-7 weeks old) |
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Preparation Method |
SJL mice were immunized s.c. with 50 µg PLP139-151 and CFA (400 µg Mycobacterium tuberculosis). Mice were treated with 50 mg/kg/day G-1 daily for 21 days beginning at the day of disease induction. Control mice were similarly treated with vehicle (5% Dimethyl sulfoxide (DMSO), 95% Polyethylene glycol (PEG)-300. |
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Dosage form |
50 mg/kg/day for 21 days |
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Applications |
G-1 administration significantly reduced the severity of actively induced experimental allergic encephalomyelitis (EAE) but not the incidence of disease. |
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References: [1]: Kurt A H, Çelik A, Kelleci B M. Oxidative/antioxidative enzyme-mediated antiproliferative and proapoptotic effects of the GPER1 agonist G-1 on lung cancer cells[J]. Oncology Letters, 2015, 10(5): 3177-3182. | |
| Cas No. | 881639-98-1 | SDF | |
| 化学名 | rel-1-[4-(6-bromo-1,3-benzodioxol-5-yl)-3aR,4S,5,9bS-tetrahydro-3H-cyclopenta[c]quinolin-8-yl]-ethanone | ||
| Canonical SMILES | CC(C1=CC([C@@](C=CC2)([H])[C@@]2([H])[C@H](C3=CC(OCO4)=C4C=C3Br)N5)=C5C=C1)=O | ||
| 分子式 | C21H18BrNO3 | 分子量 | 412.28 |
| 溶解度 | 1mg/ml in ethanol; 20mg/ml in DMSO; 30mg/ml in DMF | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4255 mL | 12.1277 mL | 24.2554 mL |
| 5 mM | 0.4851 mL | 2.4255 mL | 4.8511 mL |
| 10 mM | 0.2426 mL | 1.2128 mL | 2.4255 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet