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Erteberel (LY500307)

现货
Catalog No.
B1518
ERβ激动剂
组合的产品项目
规格价格库存 数量
5mg
¥ 3,500.00
现货
50mg
¥ 15,000.00
现货

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Background

Erteberel (LY500307) is a potent and selective ERβ (estrogen receptor beta) agonist (EC50 = 0.66 nM). [1]

Estrogen receptors are nuclear hormone receptors that act as a ligand-activated transcription factor. It regulates gene expression, cell proliferation and differentiation in target tissues and involved in breast cancer, endometrial cancer and osteoporosis etc. [1]

In transcription assay of cotransfected human prostate cancer cell line, Erteberel showed potency (EC50 = 0.66 nM), selectivity (32-fold) and full agonist function (>90% relative efficacy) to ERβ than to ERα. [1]

In mouse model, prostate wet weight of CD-1 mice were measured following oral daily doses of Erteberel for 7 days. Results showed reduction on prostate weight in a dose-dependent manner (0.01 mg/kg – 0.05 mg/kg), and no effect on testes/seminal vesicle weight and androgens testosterone/dihydrotestosterone circulating level. [1]

Reference:
[1] Norman BH, Dodge JA, Richardson TI, Borromeo PS, Lugar CW, Jones SA, Chen K, Wang Y, Durst GL, Barr RJ, Montrose-Rafizadeh C, Osborne HE, Amos RM, Guo S, Boodhoo A, Krishnan V.  Benzopyrans are selective estrogen receptor beta agonists with novel activity in models of benign prostatic hyperplasia.  J Med Chem. 2006 Oct 19;49(21):6155-7. 

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt282.33
Cas No.533884-09-2
FormulaC18H18O3
Solubility≥14.1mg/mL in DMSO
Chemical Name(3aS,4R,9bR)-4-(4-hydroxyphenyl)-1,2,3,3a,4,9b-hexahydrocyclopenta[c]chromen-8-ol
SDFDownload SDF
Canonical SMILESC1CC2C(C1)C3=C(C=CC(=C3)O)OC2C4=CC=C(C=C4)O
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

激酶实验 [1]:

雌激素受体(ER)结合实验

竞争结合实验在缓冲液(50mM Hepes, pH 7.5, 1.5mM EDTA, 150mM NaCl, 10% glycerol, 1mg/ml ovalbumin和5mM DTT)中进行测定,每孔含有0.025 μCi、3HEstradiol、10 ng雌激素alpha或beta受体。加入竞争性结合化合物(10个不同浓度)。在含有1μM的17-β Estradiol中进行非特异性结合物的测定。结合反应体系(140 μl)在室温孵育4小时,加入70 μl预冷DCC缓冲液 (含50 ml 实验缓冲液、0.75g charcoal和0.25g dextran). 培养板在4℃振荡器上混匀8分钟、随后在4℃、3,000 rpm离心10分钟。120μl等份的混合物转移到另一块96孔白色平底板,并加入175μl闪烁液,将培养板密封并且轻微震荡,5小时后在仪器上读板,计算IC50和10μM的抑制率。测定结合于ERα和ER beta 受体的3H-雌二醇KD值,结合实验的化合物的IC50值被转化为Ki 。

细胞实验:

细胞系

人前列腺癌细胞株(PC-3细胞)

溶解方法

该化合物在DMSO中的溶解度> 10 mM。若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。

反应时间

N/A

应用

Erteberel显示出潜在的、特异性地结合ERβ的活性,其EC50值为0.66 nM [1]。

动物实验:

动物模型

雄性和雌性大鼠生殖模型和大鼠及兔胚胎发育模型

剂量

0.03-10 mg/kg/天给药大鼠、或1-25 mg/kg/天给药兔、口服给药、处理2或10周

应用

使用LY500307药物处理雄性大鼠生殖模型(药物剂量1 mg/kg/天)、雌性大鼠生殖模型及其胚胎发育模型(药物剂量0.3 mg/kg/天)和兔胚胎发育模型(药物剂量25 mg/kg/天)均未观察到药物不良反应 [2]。

注意事项

请于室内测试所有化合物的溶解度。实际溶解度和理论值可能略有不同,这是由实验系统的误差引起的,属于正常现象。

References:

1. Norman, B. H., Dodge, J. A., Richardson, T. I., Borromeo, P. S., Lugar, C. W., Jones, S. A., Chen, K., Wang, Y., Durst, G. L., Barr, R. J., Montrose-Rafizadeh, C., Osborne, H. E., Amos, R. M., Guo, S., Boodhoo, A. and Krishnan, V. (2006) Benzopyrans are selective estrogen receptor beta agonists with novel activity in models of benign prostatic hyperplasia. J Med Chem. 49, 6155-6157

2. Hilbish, K. G., Breslin, W. J., Johnson, J. T. and Sloter, E. D. (2013) Fertility and developmental toxicity assessment in rats and rabbits with LY500307, a selective estrogen receptor beta (ERbeta) agonist. Birth Defects Res B Dev Reprod Toxicol. 98, 400-415

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