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Chemical Structure| 1161002-05-6 Chemical Structure| 1161002-05-6

Structure of G15
CAS No.: 1161002-05-6

Chemical Structure| 1161002-05-6

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G15 is a high-affinity and selective GPER receptor antagonist with Ki value of 20nM.

Synonyms: GRB-G15

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Product Details of G15

CAS No. :1161002-05-6
Formula : C19H16BrNO2
M.W : 370.24
SMILES Code : BrC1=C([C@@]2(NC3=CC=CC=C3[C@@]4(C=CC[C@]24[H])[H])[H])C=C5OCOC5=C1
Synonyms :
GRB-G15
MDL No. :MFCD16618401

Safety of G15

GHS Pictogram:
Signal Word:Danger
Hazard Statements:H302-H319-H332-H372-H400
Precautionary Statements:P260-P264-P270-P273-P280-P301+P312+P330-P304+P312-P305+P351+P338-P314-P337+P313-P391-P501
Class:9
UN#:3077
Packing Group:

Related Pathways of G15

GPCR

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Left ventricular apical myocytes 100 nM 1 hour G15 abolished the acute effects of E2 on cAMP, contraction and Ca2+ transient amplitudes, indicating that the acute effects of E2 were mediated by GPR30 via non-genomic signaling PMC6466778
H9c2 cardiomyocytes 10^-6 M 24 hours G15 inhibited the protective effects of both estradiol and G-1 on angiotensin II-induced cardiomyocyte hypertrophy PMC3307382
IEC-6 cells 10^-7 mol/L 48 hours or 96 hours To investigate the protective effect of G-1 on 5-FU-induced DNA damage, results showed that G-1 inhibited DNA damage by restoring ERK1/2 activity. PMC8557214

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6J mice Acute neuroinflammation model Intracerebroventricular injection 0.5 µg/µL Single injection To investigate the mediating role of GPER in SDG-mediated amelioration of neuroinflammation PMC11320852
C57BL/6 mice Chemotherapy-induced intestinal mucositis model Intraperitoneal injection 0.3 mg/kg/day Once daily for 5 days To investigate the effect of G15 on the protective role of G-1 in the CIM model, results showed that G15 abolished all the protective effects of G-1. PMC8557214

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.70mL

0.54mL

0.27mL

13.50mL

2.70mL

1.35mL

27.01mL

5.40mL

2.70mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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