G-1 |
| Catalog No.GC12766 |
G-1 is a selective and potent agonist of GPR30 with EC50 value about 2 nM.
Products are for research use only. Not for human use. We do not sell to patients.
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]: | |
|
Cell lines |
A549 human lung cancer cells |
|
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. |
|
Reaction Conditions |
0.01-100 µM for 48 and 72 h |
|
Applications |
Treatment with G-1 (10-5 and 10-4 M) for 48 and 72 h significantly decreased cell proliferation. |
| Animal experiment [2]: | |
|
Animal models |
SJL mice (5-7 weeks old) |
|
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. |
|
Dosage form |
50 mg/kg/day for 21 days |
|
Applications |
G-1 administration significantly reduced the severity of actively induced experimental allergic encephalomyelitis (EAE) but not the incidence of disease. |
|
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 | |
| Chemical Name | 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 | ||
| Formula | C21H18BrNO3 | M.Wt | 412.28 |
| Solubility | 1mg/ml in ethanol; 20mg/ml in DMSO; 30mg/ml in DMF | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 37 reference(s) in Google Scholar.)
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