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RJW100 

Cat. No. M28108
RJW100  Structure
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Quality Control & Documentation
Biological Activity

RJW100 is a potent liver receptor homolog 1 (LRH-1, NR5A2) and steroidogenic factor-1 (SF-1, NR5A1) agonist with pEC50s of 6.6 and 7.5, respectively. RJW100 also causes strong activation of the miR-200c (miRNA-200c, microRNA-200c) promoter.

Chemical Information
Molecular Weight 386.57
Formula C28H34O
CAS Number 1276664-20-0
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Suzanne G Mays, et al. Sci Rep. Enantiomer-specific activities of an LRH-1 and SF-1 dual agonist

[2] Suzanne G Mays, et al. J Biol Chem. Crystal Structures of the Nuclear Receptor, Liver Receptor Homolog 1, Bound to Synthetic Agonists

[3] Felipe de Jesus Cortez, et al. PLoS One. Disulfide-Trapping Identifies a New, Effective Chemical Probe for Activating the Nuclear Receptor Human LRH-1 (NR5A2)

[4] Yuxia Zhang, et al. Biochem Biophys Res Commun. Regulation of miR-200c by nuclear receptors PPARα, LRH-1 and SHP

[5] Richard J Whitby, et al. J Med Chem. Small molecule agonists of the orphan nuclear receptors steroidogenic factor-1 (SF-1, NR5A1) and liver receptor homologue-1 (LRH-1, NR5A2)

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Keywords: RJW100  supplier, MicroRNA (miRNA), inhibitors, activators


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