LG-120753
LG-120753 is an orally active nonsteroidal progesterone receptor (PR) antagonist, with an IC50 of 38 nM against hPR-B, a Ki of 19 nM against hPR-A, an IC50 of 227 nM against hAR, and IC50 values greater than 1000 nM against hGR, hER and hMR. LG-120753 blocks the action of progesterone, binds to and antagonizes hPR-A, and shows limited cross-reactivity with other steroid receptors. LG-120753 blocks blastocyst implantation, prevents the establishment of pregnancy, exhibits dose-dependent antiprogestogenic activity in vivo, and induces reversible antifertility effects.
For research use only. We do not sell to patients.
- CAS No.: 179894-84-9
- Formula: C19H18N2
- Molecular Weight:274.36
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:unspecified strain (female, virgin)[1]
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Dosage:0.1 mg/mouse; 0.5 mg/mouse; 1.0 mg/mouse; 2.5 mg/mouse; 5.0 mg/mouse
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Administration:p.o.; daily; 3 days
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Result:Reduced pregnancy rate to 83.3% at 0.1 mg/mouse.
Reduced pregnancy rate to 83.3% at 0.5 mg/mouse.
Reduced pregnancy rate to 66.7% at 1.0 mg/mouse.
Reduced pregnancy rate to 50% at 2.5 mg/mouse.
Reduced pregnancy rate to 0% at 5.0 mg/mouse.
Restored pregnancy rate to 100% when co-administered with steroidal progestin R5020.
Chemical Information
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CAS No. 179894-84-9
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Molecular Weight 274.36
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Formula C19H18N2
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SMILES
N#CC1=CC=CC(C2=CC=C3NC(C)(C)C=C(C)C3=C2)=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Trophoblast Invasion Assay
The trophoblast invasion assay is commonly based on the Matrigel-coated Transwell invasion system, in which invasive cells migrate through a reconstituted basement membrane matrix toward a chemoattractant gradient, thereby modeling extracellular matrix (ECM) penetration and invasive behavior in vitro. The readout is typically the number of cells that traverse the Matrigel barrier and attach to the lower surface of a porous membrane, reflecting invasive capacity through ECM-like substrates and basement membrane components. This system was originally developed to quantify invasive cell behavior using Matrigel as a basement membrane analog in a Boyden chamber format.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)