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Erteberel (LY500307) Estrogen/progestogen Receptor agonist

Name: Erteberel (LY500307)
Brand: Selleck Chemicals
SKU: S1598
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S1598

Erteberel (LY500307) is a potent, selective estrogen receptor β agonist with EC50 of 0.66 nM, demonstrating 32-fold selectivity against estrogen receptor α. It is currently in Phase 2.

Chemical Structure

Molecular Weight: 282.33

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Quality Control

Batch: Purity: 99.39%

99.39

Related Targets	Adrenergic Receptor GPR Androgen Receptor Glucocorticoid Receptor ACE RAAS Progesterone Receptor Opioid Receptor PGES THR
Other Estrogen/progestogen Receptor Inhibitors	Elacestrant (RAD1901) Dihydrochloride MPP dihydrochloride Cholesterol Endoxifen HCl G15 Chrysin Licochalcone A AZD9496 PHTPP Liquiritigenin

Solubility

In vitro
Batch:

DMSO : 57 mg/mL (201.89 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 57 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection 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.
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.	2.800mg/ml (9.92mM)	Taking the 1 mL working solution as an example, add 50 μL of 56 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 clarify; 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.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.450mg/ml (1.59mM)	Taking the 1 mL working solution as an example, add 50 μL of 9 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. 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.

Chemical Information, Storage & Stability

Molecular Weight	282.33	Formula	C₁₈H₁₈O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	533884-09-2	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent

Mechanism of Action

Features	Demonstrates significantly higher binding activity toward ERβ than ERα.
Targets/IC₅₀/Ki	ERβ 0.66 nM(EC50)
In vitro	Erteberel (LY500307) shows potent binding affinity for both ERα (K_i 2.68 nM) and ERβ (K_i 0.19 nM), which exhibits 14-fold binding selectivity for the β isoform, generated using 3H-estradiol and recombinant, full-length, human ERs in a competitive binding assay. It shows full agonist function in both ERα and ERβ assays (>90% relative efficacy), displays potent inhibition toward ERβ with EC50 of 0.66 nM exhibiting 32 fold specificity for ERβ than for ERα which has EC50 of 19.4 nM measured using a transcription assay in the cotransfected human prostate cancer PC3/ER (α or β)-ERE cell line. The cocrystal structures of this compound with ERα and ERβ show significant differences in the manner in which it binds within the binding pockets. It displays a different orientation corresponding to a (ca. 180°) rotation on its bisphenol axis, and the A ring phenol, while bound to histidine in both structures, locates to different sides of the imidazole functionality for this interaction explaining the observed selectivity for ERβ.
In vivo	Oral administration of Erteberel (LY500307) (0.01-0.05 mg/kg) in CD-1 mice produces the reduction on prostate weights in a dose-response manner, has no effect on testes and SV weights in this dose range and no effect on T and DHT levels at up to 10 × the minimum efficacy dose (0.1 mg/kg), while the nonselective ER agonist diethylstilbestrol (DES) shows significant regression of prostate, testes, and SV and also lowering T and DHT.
References	[1] https://pubmed.ncbi.nlm.nih.gov/17034120/

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If your product S1598 is chiral isoform or not?

Answer:
It is a chiral isoform. The chiral part is from the raw material.

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