GlpBio

Estrogen Receptor/ERR

Estrogen Receptor/ERR(雌激素受体/ERR)

Estrogen receptors are a group of proteins found inside cells. They are receptors that are activated by the hormone estrogen (17β-estradiol). Two classes of estrogen receptor exist: ER, which is a member of the nuclear hormone family of intracellular receptors, and GPER (GPR30), which is a member of the rhodopsin-like family of G protein-coupled receptors. The ER's helix 12 domain plays a crucial role in determining interactions with coactivators and corepressors and, therefore, the respective agonist or antagonist effect of the ligand. Different ligands may differ in their affinity for alpha and beta isoforms of the estrogen receptor: estradiol binds equally well to both receptors, estrone, and raloxifene bind preferentially to the alpha receptor, estriol, and genistein to the beta receptor. Estrogen and its receptors are essential for sexual development and reproductive function, but also play a role in other tissues such as bone. Estrogen receptors are also involved in pathological processes including breast cancer, endometrial cancer, and osteoporosis. Alternative promoter usage and alternative splicing result in dozens of transcript variants, but the full-length nature of many of these variants has not been determined.

Estrogen Receptor/ERR 相关产品(169)

  • GC39707 structure
    GC39707Droloxifene
    CAS: 82413-20-5
    纯度: >99.50%

    A selective estrogen receptor modulator

  • GC39747 structure
    GC39747(E/Z)-GSK5182
    CAS: 2699724-40-6
    纯度: >98.50%

    (E/Z)-GSK5182 是 (E)-GSK5182 和 (Z)-GSK5182 的消旋体。GSK5182 是一种高效选择性，具有口服活性的 ERRγ 反向激动剂，其 IC50 值为 79 nM。GSK5182 还能增加肝癌细胞中 reactive oxyen species (ROS) 的产生。

  • GC40643 structure
    GC40643(R)-Equol
    CAS: 221054-79-1
    纯度: >99.00%

    An estrogen receptor α agonist

  • GC40753 structure
    GC40753α-Zearalanol
    CAS: 26538-44-3
    纯度: >98.00%

    α-Zearalenol(α-玉米赤烯醇)是一种对雌激素受体 (ER) 具有高亲和力的霉菌毒素, α-Zearalenol 是 zearalenone (ZEN) 的衍生物,由于其异种雌激素效应可引起动物的生殖障碍。

  • GC41153 structure
    GC41153Tibolone
    CAS: 5630-53-5
    纯度: >98.00%

    Tibolone是一种合成类固醇，具有弱雌激素、孕激素及雄激素活性。

  • GC44686 structure
    GC44686Prochloraz
    CAS: 67747-09-5
    纯度: >98.00%

    An imidazole antifungal

  • GC44804 structure
    GC44804Raloxifene 4'-Glucuronide
    CAS: 182507-22-8
    纯度: >98.00%

    A metabolite of raloxifene

  • GC44805 structure
    GC44805Raloxifene 6-Glucuronide
    CAS: 174264-50-7
    纯度: >90.00%

    A metabolite of raloxifene

  • GC45968 structure
    GC45968(±)-Liquiritigenin
    CAS: 69097-97-8
    纯度: >95.00%

    A flavonoid with anticancer activity

  • GC48124 structure
    GC48124Tamoxifen-d5
    CAS: 157698-32-3
    纯度: >99.00%

    An internal standard for the quantification of tamoxifen

  • GC48613 structure
    GC48613Ospemifene-d4
    纯度: >99.00%

    An internal standard for the quantification of ospemifene

  • GC60806 structure
    GC60806Enclomiphene D4 hydrochloride

    EnclomipheneD4hydrochloride((E)-ClomipheneD4hydrochloride;trans-ClomipheneD4hydrochloride;EnclomifeneD4hydrochloride)是Enclomiphene的氘代标记物。EnclomipheneD4hydrochloride((E)-ClomipheneD4hydrochloride;trans-ClomipheneD4hydrochloride;EnclomifeneD4hydrochloride) 是一种有效、可口服的 oestrogenreceptor 拮抗剂，具有抗雌激素作用。

  • GC60815 structure
    GC60815Estradiol dipropionate
    CAS: 113-38-2
    纯度: >98.00%

    Estradiol dipropionate (17-Beta-Estradiol-3,17-Dipropionate) is a semisynthetic, steroidal estrogen which has been used in hormone therapy for menopausal symptoms and low estrogen levels in women and in the treatment of gynecological disorders.

  • GC60816 structure
    GC60816Estrogen receptor modulator 1
    CAS: 63676-22-2

    Estrogen receptor modulator 1 (compound 18) is an orally active and selective estrogen receptor modulator (SERM) with pIC50 of 0.46. Estrogen receptor modulator 1 exhibits potential anti-tumor activity.

  • GC61390 structure
    GC61390Zuclomiphene citrate
    CAS: 7619-53-6

    Zuclomiphenecitrate是柠檬酸克罗米芬的顺式异构体。Zuclomiphenecitrate具有抗雌激素的作用，比反式异构体更能抑制黄体生成激素(LH)的分泌。Zuclomiphenecitrate也是一种口服活性降胆固醇剂。

  • GC61391 structure
    GC61391Zuclomiphene D4 citrate

    ZuclomipheneD4citrate是Zuclomiphenecitrate的氘代物。Zuclomiphenecitrate具有抗雌激素的作用，比反式异构体更能抑制黄体生成激素(LH)的分泌。Zuclomiphenecitrate也是一种口服活性降胆固醇剂。

  • GC61488 structure
    GC61488(Rac)-Acolbifene
    CAS: 151533-34-5
    纯度: >99.50%

    (Rac)-Acolbifene(EM-343;(Rac)-EM-652)是EM652(estrogenreceptor拮抗剂)的外消旋形式，具有抗雌激素和雌激素活性。(Rac)-Acolbifene(EM-343;(Rac)-EM-652)含哌啶环，具有良好的药理作用，RBA=380。

  • GC61514 structure
    GC61514Acolbifene hydrochloride
    CAS: 252555-01-4
    纯度: >98.00%

    A selective estrogen receptor modulator

  • GC61817 structure
    GC61817GPR30 agonist-1
    CAS: 415919-74-3
    纯度: >98.50%

    GPR30 agonist-1 是一种 G 蛋白偶联受体 30 (GPR30) 激动剂。GPR30 agonist-1 发挥血管舒张作用。

  • GC62307 structure
    GC62307PROTAC ERRα Degrader-3
    CAS: 2306388-65-6
    纯度: >98.00%

    PROTAC ERRα Degrader-3 是一种基于 PROTAC 的强效选择性 ERRα 降解剂。PROTAC ERRα Degrader-3 能够在 30 nM 的浓度下将 ERRα 蛋白特异性降解 >80%。PROTAC ERRα Degrader-3 对 ERRβ 和 ERRγ 蛋白无活性。

  • GC62379 structure
    GC62379Elacestrant (S enantiomer)
    CAS: 2309762-29-4

    Elacestrant S enantiomer (RAD1901 S enantiomer) 是 Elacestrant 的低活性对映体。Elacestrant 是有选择性和口服活性的雌激素受体 (ER) 的降解剂，对 ERα 和 ERβ 的 IC50 值分别为 48 和 870 nM。

  • GC62484 structure
    GC62484FLTX1
    CAS: 1481401-71-1
    纯度: >99.50%

    FLTX1 是一种荧光他莫昔芬 (Tamoxifen) 衍生物，可以在透化和非透化条件下特异性标记细胞内 Tamoxifen 结合位点 (雌激素受体)。FLTX1 在乳腺癌细胞中表现出 Tamoxifen 有效的抗雌激素特性。FLTX1 缺乏对子宫的雌激素激动作用。

  • GC62723 structure
    GC62723ARV-471
    CAS: 2229711-68-4
    纯度: >99.50%

    ARV-471 是一种口服生物可利用的雌激素受体靶向（ER靶向）PROTAC, 用于治疗局部晚期或转移性ER+/HER2-乳腺癌患者。

  • GC63185 structure
    GC63185Segetalin B
    CAS: 164991-89-3
    纯度: >99.50%

    Segetalin B 是可从 Vaccaria segetalis 分离得到的环五肽、具有类雌激素的活性。