erβ antagonist phtpp  (MedChemExpress)

Journal: Brain research

Article Title: Estrogen receptor α regulates the IKKs/NF-kB activity involved in the development of mechanical allodynia induced by REM sleep deprivation in rats.

doi: 10.1016/j.brainres.2024.149269

Figure Lengend Snippet: Fig. 3. ERα but not ERβ regulates BMS-345541-prevented REMSD-induced allodynia in female rats. A) Effect of intrathecal injection of BMS-345541 pretreatment (preTx BMS 10 µg) in the establishment of mechanical allodynia induced by REM sleep deprivation (REMSD) for two days in intact female rats (F), female rats with vehicle (Veh), rats treated with ICI (ICI+preTx BMS), rats treated with a selective ERα antagonist (MPP+preTx BMS) or rats treated with a selective ERβ antagonist (PHTPP+preTx BMS). B) Area under the curve (AUC) obtained from time course in A. C) Effect of intrathecal injection of BMS-345541 pretreatment (preTx BMS 10 µg) in the establishment of mechanical allodynia induced by REMSD in female rats with vehicle (Veh), non-ovariectomized female rats (F), ovariectomized rats (OVX) and ovariectomized rats in the presence of ERα agonist (OVX+PPT). D) Area under the curve obtained from time course in C. Data are expressed as the mean ± SEM (n = 6). *** p < 0.001 versus Veh group; # # # p < 0.001 versus intact female rats with pretreatment (F) by one-way ANOVA followed by the Tukey test.

Article Snippet: PHTPP [4-[2-fenil-5,7-bis(trifluorometil) pirazolo[1,5-a]-pirimidin-3-il]fenol], a selective ERβ antagonist (Cat. No SC-204191, Santa Cruz Biotecnology, Dallas, TX) and PPT(1,3,5-Tris (4-hydroxyphenyl)-4-propyl-1H-pyrazole), a selective ERα agonist (Cat. No. SC-297946, Santa Cruz Biotechnology, Dallas, TX) were dissolved in 1 % DMSO in saline.

Techniques: Injection

Journal: BMC Medicine

Article Title: NLRC5 exerts anti-endometriosis effects through inhibiting ERβ-mediated inflammatory response

doi: 10.1186/s12916-024-03571-0

Figure Lengend Snippet: ERβ promotes the development of endometriosis. A Immunohistochemical staining to detect the expression of ERβ in the epithelium and stroma of normal endometrial tissues and endometriosis patients (both in their eutopic and ectopic endometrium). Scale bar = 20 μm. B Experimental design flow chart for exploring the role and mechanism of ERβ in endometriosis female mice. C The gross morphology of representative mouse endometriosis lesions and lesion sections showed glandular and interstitial tissue by H & E staining, which was consistent with endometriosis. Scale bar = 100 μm. D – E Immunohistochemical and quantitative analyses of ERβ levels in the corn oil-treated C57BL/6 J mice with endometriosis and the ERβ agonist (ERB-041) or ERβ antagonist (PHTPP) of C57BL/6 J mice with endometriosis (both in their eutopic and ectopic endometrium). Scale bar = 20 μm. F Comparison of the size of ectopic lesions in the control group ( n = 3), that in the ERB-041 group ( n = 3), and that in the PHTPP group ( n = 3). Statistical analysis was performed using a one-way ANOVA followed by Tukey’s post hoc analysis. ** P ≤ 0.01, * P < 0.05. G The relative mRNA level of ERβ in hESCs was analyzed by qRT-PCR. H The protein expression of ERβ in hESCs was analyzed by western blotting. I – J The wound healing and transwell method was used to explore the impact of ERβ overexpression on the migration and invasive ability of hESCs in vitro. Scale bar = 100 μm. Statistical analysis was performed using a two-tailed Student’s t -test. * P < 0.05 compared with NC; ** P ≤ 0.01 compared with NC

Article Snippet: The mice model of endometriosis were randomly divided into seven groups: the control group, the ERβ activator (ERB-041, purchased from MedChem Express, USA) group, the ERβ antagonist (PHTPP, purchased from MedChem Express, USA) group, the NC group, the NC + ERB-041 group, the shNLRC5 group, and the shNLRC5 + ERB-041 group.

Techniques: Immunohistochemical staining, Staining, Expressing, Comparison, Control, Quantitative RT-PCR, Western Blot, Over Expression, Migration, In Vitro, Two Tailed Test

Journal: BMC Medicine

Article Title: NLRC5 exerts anti-endometriosis effects through inhibiting ERβ-mediated inflammatory response

doi: 10.1186/s12916-024-03571-0

Figure Lengend Snippet: ERβ promotes the development of endometriosis by activating inflammatory response. A – F Immunohistochemical and quantitative analyses of TNF-α, IL-6, and IL-10 levels in the corn oil-treated C57BL/6 J mice with endometriosis and ERB-041 or PHTPP of C57BL/6 J mice with endometriosis (both in their eutopic and ectopic endometrium). Scale bar = 20 μm. G A wound healing assay was used to explore the impact of LPS concentration on the migration ability of hESCs in vitro. Scale bar = 100 μm. Statistical analysis was performed using a one-way analysis of variance (ANOVA), followed by Tukey’s post hoc analysis. ** P ≤ 0.01, ns, non-significant. H ELISA analysis of TNF-α, IL-6, and IL-10 levels in the conditioned media harvested 48 h after plating hESCs with LPS. * P < 0.05 compared with control; ** P ≤ 0.01 compared with control. I ELISA analysis of TNF-α, IL-6, and IL-10 levels in the conditioned media harvested 48 h after plating hESCs. J – K Migration and invasive capabilities of hESCs in different groups, assessed by wound healing and transwell assays. Scale bar = 100 μm. Statistical analysis was performed using a one-way analysis of variance (ANOVA), followed by Tukey’s post hoc analysis. ** P ≤ 0.01, * P < 0.05, ns, non-significant

Article Snippet: The mice model of endometriosis were randomly divided into seven groups: the control group, the ERβ activator (ERB-041, purchased from MedChem Express, USA) group, the ERβ antagonist (PHTPP, purchased from MedChem Express, USA) group, the NC group, the NC + ERB-041 group, the shNLRC5 group, and the shNLRC5 + ERB-041 group.

Techniques: Immunohistochemical staining, Wound Healing Assay, Concentration Assay, Migration, In Vitro, Enzyme-linked Immunosorbent Assay, Control

Journal: BMC Medicine

Article Title: NLRC5 exerts anti-endometriosis effects through inhibiting ERβ-mediated inflammatory response

doi: 10.1186/s12916-024-03571-0

Figure Lengend Snippet: ERβ promoted NLRC5 expression in endometriosis. A – D Comparison of the expression levels of NLRC5 mRNA and protein in the eutopic and ectopic endometrial tissue of C57BL/6 J mice with endometriosis in the control group ( n = 3), that in the ERB-041 group ( n = 3), and that in the PHTPP group ( n = 3). E – F The relative mRNA and protein levels of NLRC5 in hESCs were analyzed by qRT-PCR and western blotting. Statistical analysis was performed using a one-way ANOVA followed by Tukey’s post hoc analysis. ** P ≤ 0.01, * P < 0.05, ns, non-significant

Article Snippet: The mice model of endometriosis were randomly divided into seven groups: the control group, the ERβ activator (ERB-041, purchased from MedChem Express, USA) group, the ERβ antagonist (PHTPP, purchased from MedChem Express, USA) group, the NC group, the NC + ERB-041 group, the shNLRC5 group, and the shNLRC5 + ERB-041 group.

Techniques: Expressing, Comparison, Control, Quantitative RT-PCR, Western Blot

Journal: eNeuro

Article Title: Local Synthesis of Estradiol in the Rostral Ventromedial Medulla Protects against Widespread Muscle Pain in Male Mice

doi: 10.1523/ENEURO.0332-24.2024

Figure Lengend Snippet: Pharmacological drugs utilized for RVM microinjection experiments

Article Snippet: PHTPP , ER-β antagonist , Tocris Bioscience , 2662 , 1 μM , 2% DMSO; 0.9% saline.

Techniques: Microinjection, Concentration Assay, Saline