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)

  • GC31008 structure
    GC31008Dienestrol
    CAS: 84-17-3
    纯度: >98.00%

    Dienestrol(Restrol) is a synthetic, non-steroidal estrogen. It is an estrogen receptor agonist.

  • GC31565 structure
    GC31565NNC45-0781
    CAS: 207277-66-5

    NNC45-0781是一种组织选择性的雌激素(estrogen)部分激动剂。

  • GC31589 structure
    GC31589MK-6913 (Tetrahydrofluoroene 52)
    CAS: 1398510-92-3

    MK-6913 (Tetrahydrofluoroene 52) (Tetrahydrofluoroene 52) 是一种有效的选择性雌激素受体 β；激动剂。

  • GC31746 structure
    GC31746Gestrinone (R 2323)
    CAS: 16320-04-0
    纯度: >99.50%

    An androgen and progesterone receptor ligand used to treat endometriosis

  • GC32406 structure
    GC32406H3B-6545
    CAS: 2052130-80-8
    纯度: >99.50%

    H3B-6545是一种口服有效的选择性雌激素受体共价拮抗剂(SERCA)。

  • GC32445 structure
    GC32445Nitromifene (CI628)
    CAS: 10448-84-7

    Nitromifene (CI628) 是雌激素受体 (ER) 的拮抗剂。

  • GC32696 structure
    GC32696Elacestrant dihydrochloride (RAD1901 dihydrochloride)
    CAS: 1349723-93-8
    纯度: >99.50%

    Elacestrant (RAD1901) Dihydrochloride is an orally available selective estrogen receptor degrader (SERD) with IC50 of 48 nM and 870 nM for ERα and ERβ, respectively.

  • GC32782 structure
    GC32782Brilanestrant (ARN-810)
    CAS: 1365888-06-7
    纯度: >99.50%

    A selective estrogen receptor degrader

  • GC32920 structure
    GC32920GDC-0927 (SRN-927)
    CAS: 1642297-01-5
    纯度: >99.50%

    GDC-0927 (SRN-927) (SRN-927) 是一种有效的、非甾体、口服生物可利用的选择性雌激素受体拮抗剂。

  • GC33011 structure
    GC33011BHPI
    CAS: 56632-39-4
    纯度: >98.00%

    An ERα antagonist

  • GC33025 structure
    GC33025Elacestrant (RAD1901)
    CAS: 722533-56-4

    Elacestrant (RAD1901) (RAD1901) 是一种口服选择性雌激素受体降解剂 (SERD)，对 ERα 的 IC50 分别为 48 和 870 nM；和ERβ，分别。

  • GC33193 structure
    GC33193GDC-0927 Racemate (SRN-927 Racemate)
    CAS: 1443983-36-5

    GDC-0927 Racemate (SRN-927 Racemate) (SRN-927 Racemate) 是一种雌激素受体降解剂，有效抑制 ER-α；活性，IC50为0.2 nM，用于ER相关疾病的研究。

  • GC33262 structure
    GC33262H3B-5942
    CAS: 2052128-15-9
    纯度: >99.00%

    A selective estrogen receptor covalent antagonist

  • GC33349 structure
    GC33349E3 ligase Ligand 5
    CAS: 1264754-13-3
    纯度: >98.00%

    PROTAC ERRa ligand 1是雌激素相关受体a(ERRa)拮抗剂，对ERRa和 ERRy的IC 50 分别为0.04和 2.8μM。

  • GC33378 structure
    GC33378H3B-6545 Hydrochloride
    CAS: 2052132-51-9
    纯度: >99.00%

    H3B-6545Hydrochloride是一种口服有效的选择性雌激素受体共价拮抗剂(SERCA)。

  • GC33381 structure
    GC33381Arzoxifene hydrochloride (LY 353381 HCl)
    CAS: 182133-27-3

    Arzoxifene (LY353381) hydrochloride 是一种选择性雌激素受体调节剂，在乳腺和子宫组织中是一种有效的雌激素拮抗剂，同时作为雌激素激动剂来维持骨密度和降低血清胆固醇。

  • GC33402 structure
    GC33402Idoxifene (CB7432)
    CAS: 116057-75-1

    Idoxifene (CB7432) (CB7432) 是一种新型的组织特异性选择性雌激素受体调节剂 (SERM)。

  • GC34006 structure
    GC34006Equilin (7-Dehydroestrone)
    CAS: 474-86-2
    纯度: >99.00%

    Equilin (7-Dehydroestrone) (7-Dehydroestrone) 是一大类雌激素物质的重要成员，在化学上与二甲双胍 (oestrone) 相关。

  • GC34151 structure
    GC34151PAC
    CAS: 2158322-33-7
    纯度: >98.00%

    PAC是由抗体通过linker与PROTAC偶联而组成的。PAC的详细信息请参考专利文献WO2017201449A1中的化合物PAC1。与PROTAC(无Ab)相比，PAC更加显著降低雌激素受体-α(ERα)水平。

  • GC34153 structure
    GC34153Pipendoxifene hydrochloride
    CAS: 245124-69-0
    纯度: >99.00%

    Pipendoxifenehydrochloride是一种选择性的雌激素受体调节剂(SERMs)。

  • GC34293 structure
    GC34293Elacestrant S enantiomer (RAD1901 S enantiomer)

    ElacestrantSenantiomer是elacestrant的低活性对映体。Elacestrant(RAD1901)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870nM。

  • GC34294 structure
    GC34294Elacestrant S enantiomer dihydrochloride (RAD1901 S enantiomer dihydrochloride)

    ElacestrantSenantiomerdihydrochloride是elacestrant的低活性对映体。Elacestrant(RAD1901)dihydrochloride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870nM。

  • GC34341 structure
    GC34341PROTAC ERα Degrader-1
    CAS: 2417369-94-7

    PROTACERαDegrader-1包含泛素E3连接酶结合基团，linker和靶蛋白结合基团。PROTACERαDegrader-1的详细信息请参考专利文献WO2017201449A1中的化合物P1。PROTACERαDegrader-1降低雌激素受体-α(ERα)水平。

  • GC34733 structure
    GC34733PROTAC ER Degrader-2
    CAS: 1351169-29-3
    纯度: >98.00%

    PROTACERDegrader-2是合成PAC的中间体。PAC是由抗体通过linker与PROTAC偶联而组成的。PAC的详细信息请参考专利文献WO2017201449A1中的化合物LP2。与PROTAC(无Ab)相比，PAC更加显著降低雌激素受体-α(ERα)水平。