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  3. G15

G15 

Cat. No.: HY-103449 Purity: >99.0%
Handling Instructions

G15 is a high affinity and selective G-protein-coupled estrogen receptor (GPER/GPR30) antagonist with a Ki of 20 nM.

For research use only. We do not sell to patients.

G15 Chemical Structure

G15 Chemical Structure

CAS No. : 1161002-05-6

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 94 In-stock
Estimated Time of Arrival: December 31
5 mg USD 85 In-stock
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10 mg USD 140 In-stock
Estimated Time of Arrival: December 31
50 mg USD 430 In-stock
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100 mg USD 740 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

G15 is a high affinity and selective G-protein-coupled estrogen receptor (GPER/GPR30) antagonist with a Ki of 20 nM[1][2].

IC50 & Target

Ki: 20 nM (GPER/GPR30)[2]

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.
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.
Clinical Trial
Molecular Weight

370.24

Formula

C₁₉H₁₆BrNO₂

CAS No.

1161002-05-6

SMILES

BrC1=C([[email protected]@H]2NC3=C(C=CC=C3)[[email protected]@]4([H])[[email protected]]2([H])CC=C4)C=C5OCOC5=C1

Shipping

Room temperature in continental US; may vary elsewhere

Storage

-20°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 41.67 mg/mL (112.55 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.62 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.62 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: >99.0%

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G15
Cat. No.:
HY-103449
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