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G-1 

Cat. No.: HY-107216 Purity: 99.20%
Handling Instructions

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

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

G-1 Chemical Structure

G-1 Chemical Structure

CAS No. : 881639-98-1

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 136 In-stock
Estimated Time of Arrival: December 31
1 mg USD 50 In-stock
Estimated Time of Arrival: December 31
5 mg USD 150 In-stock
Estimated Time of Arrival: December 31
10 mg USD 270 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Protocol

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  • References

Description

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

IC50 & Target

Ki: 11 nM (GPR30)[1]

In Vitro

G-1 is a nonsteroidal, high-affinity and selective agonist of GPR30 with a Ki 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].

In Vivo

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].

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

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

H2O : < 0.1 mg/mL (insoluble)

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

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

    Solubility: ≥ 2.5 mg/mL (6.06 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (6.06 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

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

*All of the co-solvents are provided by MCE.
References
Cell Assay
[2]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[3]

Four-week-old nu/nu-Forkhead box N1nu 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

412.28

Formula

C₂₁H₁₈BrNO₃

CAS No.

881639-98-1

SMILES

BrC1=C([[email protected]]2[[email protected]]3([H])[[email protected]](C=CC3)([H])C4=CC(C(C)=O)=CC=C4N2)C=C5C(OCO5)=C1

Shipping

Room temperature in continental US; may vary elsewhere

Purity: 99.20%

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Product Name:
G-1
Cat. No.:
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G-1

Cat. No.: HY-107216