2. Vitamin D Related/Nuclear Receptor
  3. Estrogen Receptor/ERR
  4. OP-1690

OP-1690 is a complete estrogen receptor (ERα) antagonist (CERAN), with pIC50 values of 7.5 and 7.9 in alkaline phosphatase (AP) activity assay and TR-FRET assay, respectively. OP-1690 modulates receptor function by inducing ERα tetramerization, effectively induces ERα degradation, inhibits target gene transcription, but exhibits low antiproliferative potency. OP-1690 can be used for breast cancer research.

For research use only. We do not sell to patients.

OP-1690

OP-1690 Chemical Structure

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OP-1690 Related Antibodies

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Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

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Description

OP-1690 is a complete estrogen receptor (ERα) antagonist (CERAN), with pIC50 values of 7.5 and 7.9 in alkaline phosphatase (AP) activity assay and TR-FRET assay, respectively. OP-1690 modulates receptor function by inducing ERα tetramerization, effectively induces ERα degradation, inhibits target gene transcription, but exhibits low antiproliferative potency. OP-1690 can be used for breast cancer research[1].

IC50 & Target[1]

ERα

7.5 (pIC50)

In Vitro

OP-1690 (7 d) inhibits the proliferation of MCF7 and CAMA-1 cells with pIC50 values of 6 and 5.9, respectively, which are lower than those of Fulvestrant (HY-13636) and RAD1901 (HY-19822).

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

OP-1690 Related Antibodies
Parmacokinetics
Species Dose Route Tmax Cmax T1/2 AUC0-last AUC0-∞ CL Vss F
Mice[1] 1 mg/kg i.v. 0.08 h 406 ng/mL 5.6 h 291 ng·h/mL 298 ng·h/mL 55.9 mL/min/kg 12.1 L/kg /
Mice[1] 5 mg/kg p.o. 0.25 h 4.95 ng/mL 2.8 h 9.19 ng·h/mL 10.6 ng·h/mL / / 0.7 %
Molecular Weight

541.07

Formula

C31H35ClF2N2O2
SMILES

FC1=CC=CC=C1C2(CCCC2)CN(CC3=CC=CC(O)=C3Cl)C4=CC=C(OC5CN(CCCF)C5)C=C4
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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OP-1690 Related Classifications

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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× = ×
C1   V1   C2   V2
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:

OP-1690OP1690OP 1690Estrogen Receptor/ERRERα ligand binding domainestrogen receptor-positive breast cancerestrogen receptor alphacomplete estrogen receptor antagonistestrogen receptor-positive breast cancersInhibitorinhibitorinhibit

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