2. Vitamin D Related/Nuclear Receptor
  3. Estrogen Receptor/ERR
  4. OSU-ERβ-12

OSU-ERβ-12 is a selective, orally active and brain-penetrant ERβ agonist with an EC50 of 78.3 nM and a Ki of 2.02 nM. OSU-ERβ-12 shows more than 200-fold selectivity for ERβ over ERα. OSU-ERβ-12 potently binds to ERβ, reducing the expression of pro-fibrotic genes mediated by TGF-β, which contributes to the reduction of liver fibrosis. OSU-ERβ-12 can be used for the study of fibrotic liver disease, non-alcoholic fatty liver disease (NAFLD), neuroinflammation.

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OSU-ERβ-12

OSU-ERβ-12 Chemical Structure

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OSU-ERβ-12 Related Antibodies

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Description

OSU-ERβ-12 is a selective, orally active and brain-penetrant ERβ agonist with an EC50 of 78.3 nM and a Ki of 2.02 nM. OSU-ERβ-12 shows more than 200-fold selectivity for ERβ over ERα. OSU-ERβ-12 potently binds to ERβ, reducing the expression of pro-fibrotic genes mediated by TGF-β, which contributes to the reduction of liver fibrosis. OSU-ERβ-12 can be used for the study of fibrotic liver disease, non-alcoholic fatty liver disease (NAFLD), neuroinflammation[1][2][3].

IC50 & Target[1]

ERβ

78.3 nM (EC50)

ERα

>10,000 nM (EC50)

hERβ

2.0 nM (Ki)

hERα

6.6 nM (Ki)

In Vitro

OSU-ERβ-12 (1 μM; 18 h; HEK-293 cells) is highly selective for hERβ[1].
OSU-ERβ-12 (10 μM - 30 μM; 60 min; Human liver microsomes) is highly stable in human liver microsomes[1].
OSU-ERβ-12 (2 μM; 6 h; Mouse, rat, monkey, and human plasma) has high plasma protein binding in multiple species[1].
OSU-ERβ-12 (30 μM; 5 min; Chinese hamster ovary cells expressing hERG potassium channels) does not inhibit hERG potassium channels[1].
OSU-ERβ-12 (24 hours; Human HCC cell (HepG2) and human HSC (LX-2) co-culture) reduces the TGF-β-mediated expression of pro-fibrotic genes (MCP-1, TGF-β, COL1A1) in the co-culture system[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

OSU-ERβ-12 Related Antibodies
Parmacokinetics
Species Dose Route Cmax AUCall T1/2 F
Mice[1] 10 mg/kg p.o. 11.4 μM 73.7 μM/L·h 7.0 h 53.8 %
Mice[1] 10 mg/kg s.c. 41.5 μM 145 μM/L·h 11.3 h 100 %
Mice[1] 10 mg/kg i.v. 75.6 μM 137 μM/L·h 5.4 h /
In Vivo

OSU-ERβ-12 (10 mg/kg, 100 mg/kg; Oral gavage; once daily; 4 weeks) reduces liver fibrosis in CCl4-induced fibrosis mice[1][3].
OSU-ERβ-12 (20 mg/kg, 50 mg/kg; oral gavage; 6 consecutive days) increases plasma and brain concentrations and uterine mass in 67NR murine mammary nonmetastatic tumor model[2].
OSU-ERβ-12 (50 mg/kg; 6 days; Hippocampus, frontal cortex, and hypothalamus of ovariectomized (OVX) mice) increases IL-6 expression in the hypothalamus, primarily driven by the tumor-bearing mice[2].
OSU-ERβ-12 (50 mg/kg; 6 days; Hypothalamus, hippocampus, and frontal cortex of ovariectomized (OVX) mice) increases the expression of Gper1 and Cyp19a1 in the frontal cortex of sham surgery mice but not in tumor-bearing mice[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6N mice (22.2 g; 8-week-old) bearing CCl4-induced hepatic fibrosis[1]
Dosage: 10 mg/kg, 100 mg/kg
Administration: Oral gavage; once daily; 4 weeks
Result: Significantly reduced CCl4-induced liver fibrosis in mice at both non-selective (100 mg/kg). 
Animal Model: Balb/c (female, 8-9-week-old, nulliparous, ovariectomized)[2]
Dosage: 20 mg/kg, 50 mg/kg
Administration: oral gavage; 6 consecutive days
Result: Increased plasma and brain concentrations in a dose-dependent manner and increased uterine mass six hours after the final treatment.
Animal Model: Balb/c (female, 8-9-week-old, nulliparous, ovariectomized)[2]
Dosage: 50 mg/kg
Administration: oral gavage; 6 consecutive days
Result: Did not effectively reduce neuroinflammation and increased IL-6 expression in the hippocampus and frontal cortex in tumor-free mice. In tumor-bearing mice, it increased hypothalamic IL-6 expression and partially ameliorated the reduction in hypothalamic expression of Esr1, Esr2, and Gper1.
Molecular Weight

352.43

Formula

C25H20O2
SMILES

OC(C=C1)=CC=C1C2345C678C9%10%11C%12%13%14C962C%123%15C%13%16%17C%10%14%18([C@@H](O)CCCCCC)C%117%19C%18%16%20C%1984C%17%15%205
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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OSU-ERβ-12 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

OSU-ERβ-12Estrogen Receptor/ERRhERGoff-target interactionsagonistNASHERβestrogen receptor betaERβ agonistOSU-ER\u03b2-12Carborane-basedpharmacokineticshuman liver microsome stabilityHepaticCYPER\u03b2-selectiveFibrosisfunctional activityInhibitorinhibitorinhibit

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