G-15 |
| Catalog No.GC16618 |
G-15 es un antagonista del receptor de estrógeno acoplado a proteína G (GPER/GPR30) selectivo y de alta afinidad con una Ki de 20 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1161002-05-6
Sample solution is provided at 25 µL, 10mM.
G-15 is a selective antagonist of GPR30 with Ki value of 20 nM [1].
G protein-coupled receptor 30 (GPR30) is an integral membrane protein that localizes to the endoplasmic reticulum and with high affinity for estradiol and aldosterone. GPR30 participates in multiple intracellular signaling pathways [1].
G-15 is a selective GPR30 antagonist with Ki value of 20 nM, While displayed little binding to ERα or ERβ up to 10 μM. In SKBr3 breast cancer cells that expressed only GPR30, G-1 or estrogen significantly increased intracellular calcium concentrations, while G15 inhibited the response to G-1 or estrogen with IC50 value of 185 and 190 nM respectively in a dose-dependent way. In GPR30-transfected COS7 cells, G-15 inhibited both estrogen and G-1 activation of PI3K and accumulation of PIP3 [1]. In endometriotic cells, G-1 increased cell proliferation and Akt phosphorylation, while G-15 reversed this stimulation and inhibited cell proliferation and induced Akt dephosphorylation [2].
In intact rats and ovariectomized (OVX) rats treated with estradiol, G-15 impaired acquisition of delayed matching-to-position (DMP) T-maze task with a persistent turn. The result suggested that GPR30 played an crucial role in mediating the effects of estradiol on spatial learning [3].
References:
[1]. Dennis MK, Burai R, Ramesh C, et al. In vivo effects of a GPR30 antagonist. Nat Chem Biol, 2009, 5(6): 421-427.
[2]. G-protein-coupled estrogen receptor and the GPER-antagonist G-15 inhibits proliferation in endometriotic cells. Fertil Steril, 2013, 100(3): 770-776.
[3]. Hammond R, Nelson D, Kline E, et al. Chronic treatment with a GPR30 antagonist impairs acquisition of a spatial learning task in young female rats. Horm Behav, 2012, 62(4): 367-374.
| Cell experiment [1,2]: | |
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Cell lines |
Immortalized epithelial endometriotic cell line (11z) |
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Preparation method |
The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
10, 30, or 60 μM for 24, 48, or 72 hours |
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Applications |
G-1 (30 μM) led to Akt phosphorylation at serine 473 within 2 hours. Pretreatment with G-15 (60 μM) prevented this phosphorylation by G-1. Treatment with 10 μM G-1 for 72 hours significantly stimulated the cells with an increase of the relative proliferation. A subsequent 72-hour treatment with 30 μM G-15 significantly reversed this stimulation. Treatment with G-15 alone led to a decrease of the relative proliferation. G-15 dose-dependently inhibited G-1–mediated calcium mobilization in SKBr3 cells with IC50 of ～185 nM. G15 inhibited the G-1–mediated activation of PI(3)K in GPR30-transfected COS7 cells. |
| Animal experiment [3]: | |
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Animal models |
Ovariectomized female rats |
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Dosage form |
Subcutaneous injection, 5 μg/day, 10 μg/day |
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Application |
G-15 dose-dependently impaired DMP acquisition. G-15 specifically reduced the rate of acquisition. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Imesch P, Samartzis E P, Dedes K J, et al. Histone deacetylase inhibitors down-regulate G-protein-coupled estrogen receptor and the GPER-antagonist G-15 inhibits proliferation in endometriotic cells[J]. Fertility and sterility, 2013, 100(3): 770-776. [2]. Dennis M K, Burai R, Ramesh C, et al. In vivo effects of a GPR30 antagonist[J]. Nature chemical biology, 2009, 5(6): 421-427. [3]. Hammond R, Nelson D, Kline E, et al. Chronic treatment with a GPR30 antagonist impairs acquisition of a spatial learning task in young female rats[J]. Hormones and behavior, 2012, 62(4): 367-374. | |
| Cas No. | 1161002-05-6 | SDF | |
| Chemical Name | (3aR,4R,9bS)-4-(6-bromobenzo[d][1,3]dioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline | ||
| Canonical SMILES | BrC1=C(C=C2OCOC2=C1)[C@@H]3NC4=CC=CC=C4[C@@H]5[C@H]3CC=C5 | ||
| Formula | C19H16BrNO2 | M.Wt | 370.24 |
| Solubility | ≥ 37mg/mL in DMSO | Storage | -20°C, protect from light |
| 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 | 2.701 mL | 13.5048 mL | 27.0095 mL |
| 5 mM | 0.5402 mL | 2.701 mL | 5.4019 mL |
| 10 mM | 0.2701 mL | 1.3505 mL | 2.701 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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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: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 31 reference(s) in Google Scholar.)
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