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G-1 (LNS 8801) Estrogen/progestogen Receptor antagonist

Name: G-1 (LNS 8801)
Brand: Selleck Chemicals
SKU: S0851
Rating: 5 (1 reviews)

Cat.No.S0851

G-1 (LNS 8801) is a nonsteroidal and selective agonist of G protein-coupled receptor 30 (GPR30, G protein-coupled estrogen receptor 1, GPER) with Ki of 11 nM.

Chemical Structure

Molecular Weight: 412.28

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Quality Control

Batch: S085101 DMSO]82 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.55%

Cited in Nature Medicine for its top-tier quality
COA
SDS
Datasheet

99.55

Related Targets	CXCR Hedgehog/Smoothened PKA Adrenergic Receptor AChR 5-HT Receptor Histamine Receptor Dopamine Receptor Ras KRas
Other Estrogen/progestogen Receptor Inhibitors	Elacestrant (RAD1901) Dihydrochloride Vepdegestrant (ARV-471) MPP dihydrochloride Kaempferol Cholesterol G15 Endoxifen HCl Licochalcone A Chrysin Pregnenolone

Chemical Information, Storage & Stability

Molecular Weight	412.28	Formula	C₂₁H₁₈BrNO₃	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	881639-98-1	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent

Solubility

In vitro
Batch:

DMSO : 82 mg/mL (198.89 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (12.13mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	GPR30 (Cell-free assay) 11 nM(Ki)
References	[1] https://pubmed.ncbi.nlm.nih.gov/27407175/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06351488	Not yet recruiting	Kidney Transplant Patients Eligible for a Solid Biopsy	Assistance Publique - Hôpitaux de Paris\|CGenetix\|Institut National de la Santé Et de la Recherche Médicale France	June 10 2024	--
NCT06217458	Not yet recruiting	DCIS\|Breast Carcinoma in Situ\|Calcification	Clinical Hospital Center Rijeka	March 1 2024	Not Applicable
NCT06178146	Recruiting	IrAE	Jun Wang\|Qianfoshan Hospital	September 1 2023	Phase 4

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Handling Instructions

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