Erteberel (LY500307)

製品コードS1598 バッチS159802

印刷

化学情報

Synonyms

Erteberel

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₈H₁₈O₃

分子量

282.33

CAS No.

533884-09-2

Solubility (25°C)*

体外

DMSO

56 mg/mL (198.34 mM)

Ethanol

56 mg/mL (198.34 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

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 この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	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 この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	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.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	LY500307 is a potent, selective estrogen receptor β agonist with EC50 of 0.66 nM, 32-fold selectivity against estrogen receptor α. Phase 2.
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. Its cocrystal structures with ERα and ERβ show significant differences in the manner in which this compound 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. ^[1]
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. It 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. ^[1]
特徴	Demonstrates significantly higher binding activity toward ERβ than ERα.

プロトコル(参考用のみ)

キナーゼアッセイ	Cell-Based Transcriptional Assays
キナーゼアッセイ	Erteberel (LY500307) is evaluated in PC3 human prostatic adenocarcinoma cells transiently cotransfected with plasmid carrying either full length human ERα or full length human ERβ and a reporter plasmid using fugene 6 transfection reagent. Human ERα or human ERβ are constitutively expressed using plasmids containing the cytomegalovirus (CMV) promoter. Reporter plasmids for the ER CTF assays contain 3X human ERE plus the thymidine kinase (TK) promoter upstream of the luciferase reporter cDNA. Efficacy of this compound is determined relative to the reference molecule diethylstilbestrol. EC50 values are determined by computer fit to a concentration-response curve.
動物実験	動物モデル	CD-1 mice
	投薬量	0.01-0.05 mg/kg
	投与方法	Oral gavage daily

参考

https://pubmed.ncbi.nlm.nih.gov/17034120/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

The Role of Estrogen and Estrogen Analogues in Friedreich’s Ataxia Cytoprotection. [Timothy E. Richardson, et al. University of North Texas, 2014, Health Science Center at Fort Worth ]

The Role of Estrogen and Estrogen Analogues in Friedreich’s Ataxia Cytoprotection. [Timothy E. Richardson, et al. University of North Texas, 2014, Health Science Center at Fort Worth ]

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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