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G-1

Catalog No. T15364   CAS 881639-98-1

G-1 is a nonsteroidal, high-affinity and selective GPR30 agonist (Ki: 11 nM).

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G-1 Chemical Structure
G-1, CAS 881639-98-1
Pack Size Availability Price/USD Quantity
1 mg In stock $ 43.00
5 mg In stock $ 80.00
10 mg In stock $ 126.00
25 mg In stock $ 223.00
50 mg In stock $ 369.00
100 mg In stock $ 531.00
1 mL * 10 mM (in DMSO) In stock $ 75.00
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Purity: 98.14%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description G-1 is a nonsteroidal, high-affinity and selective GPR30 agonist (Ki: 11 nM).
Targets&IC50 GPR30:(ki)11 nM
In vitro Treatment with G-1 (10 μM and 100 μM; 48 and 72 h) obviously reduces cell proliferation (P<0.001). At 72 h, the IC50 value for G-1 is calculated to be 20 μM. Cell cycle analysis of H295R cells after 24 h of G-1 treatment shows a cell cycle arrest in the G2 phase. Treatment of A549 cells with G-1(20 μM) reveals a significant increase in apoptosis, consistent with its antiproliferative effect (P<0.001)[2]. The presence of G-1 increases Bax expression while reduces Bcl-2[3].
In vivo After 14 days post-injury, the results display that the Basso mouse scale scores are obviously higher in the G-1 group compared with the other groups (P<0.05). G-1 administration produces a statistically significant induce in tumor volume from day 14 post-treatment. Grafted tumors harvested after a three-week treatment with G-1 show a significant decrease in tumor weight compare to vehicle-treated animals[3]. The number of caspase-3-positive cells in the cross-sections is counted, and G-1 group has fewer positive cells compared with the other groups (P<0.05), and there is no difference between the two groups (P>0.05)[1].
Molecular Weight 412.28
Formula C21H18BrNO3
CAS No. 881639-98-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 0.1 mg/mL (insoluble)

DMSO: 50 mg/mL (121.28 mM), sonification is recommended.

TargetMolReferences and Literature

1. Cheng Q, et al. G-1 exerts neuroprotective effects through G protein-coupled estrogen receptor 1 following spinal cord injury in mice. Biosci Rep. 2016 Aug 31;36(4). pii: e00373. 2. Kurt AH, et al. Oxidative/antioxidative enzyme-mediated antiproliferative and proapoptotic effects of the GPER1 agonist G-1 on lung cancer cells. Oncol Lett. 2015 Nov;10(5):3177-3182. 3. Chimento A, et al. GPER agonist G-1 decreases adrenocortical carcinoma (ACC) cell growth in vitro and in vivo. Oncotarget. 2015 Aug 7;6(22):19190-203.

Related compound libraries

This product is contained In the following compound libraries:
Nuclear Receptor Compound Library Covalent Inhibitor Library Anti-Cancer Compound Library Bioactive Compound Library Bioactive Compounds Library Max Anti-Ovarian Cancer Compound Library GPCR Compound Library Endocrinology-Hormone Compound Library

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Keywords

G-1 881639-98-1 Endocrinology/Hormones GPCR/G Protein Estrogen Receptor/ERR GPR Inhibitor inhibit G1 G 1 inhibitor

 

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