G-1

SKU: orb1308286

Description

G-1 is a nonsteroidal, high-affinity, and selective agonist for GPR30 (GPER), with a Ki value of 11 nM. This compound is employed in both in vitro and in vivo research to study GPER-mediated signaling in fields such as oncology, cardiology, endocrinology, and neuroscience, as documented in scientific literature.

Research Area

Metabolism Research, Pharmacology & Drug Discovery

Images & Validation

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Key Properties

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CAS Number	881639-98-1
MW	412.28
Formula	C₂₁H₁₈BrNO₃
SMILES	[H][C@@]12CC=C[C@]1([H])c1cc(ccc1N[C@@H]2c1cc2OCOc2cc1Br)C(C)=O
Target	GPR\|\|\|Estrogen Receptor/ERR
Solubility	DMSO:120 mg/mL (291.06 mM);H2O:< 0.1 mg/mL (insoluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.85 mM)

Bioactivity

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Target IC50	GPR30:(ki)11 nM
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. 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).
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). The presence of G-1 increases Bax expression while reduces Bcl-2.

Storage & Handling

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Storage	-20°C
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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ERR, G 1, Estrogen Receptor/ERR, EstrogenReceptor, Estrogen Receptor, GPR30, G1, G-1, inhibit, Inhibitor

Quality Guarantee

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Compound Identifiers

PubChem CID

16112908 ↗

Key Properties

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No computed properties available.

Protocol Information

Find More Protocols

Applications:	ELISA, IHC, WB
Reactivity:	Human
Species/Host:	Rabbit
Clonality:	Polyclonal
Conjugation:	Unconjugated

Reactivity:	Human
Dynamic Range:	3.13-200ng/mL
Sensitivity:	1.88 ng/mL

Applications:	ELISA, IF, IHC, WB
Reactivity:	Human, Mouse, Rat
Clonality:	Polyclonal
Conjugation:	Unconjugated

Applications:	ELISA, SBR
Reactivity:	Plant
Species/Host:	Mouse
Clonality:	Monoclonal
Conjugation:	Unconjugated

G-1

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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