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VDR agonist 2

Cat. No. M43610
VDR agonist 2 Structure
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Biological Activity

VDR agonist 2 is a VDR (vitamin D receptor) agonist that can effectively inhibit TGF-β1-induced activation of hepatic stellate cells (HSC).

Chemical Information
Molecular Weight 366.37
Formula C20H21F3O3
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
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] Bálint Rehó et al. J Biol Chem. Agonist-controlled competition of RAR and VDR nuclear receptors for heterodimerization with RXR is manifested in their DNA binding

[2] Anna A Brożyna et al. Int J Mol Sci. Vitamin D Signaling in Psoriasis: Pathogenesis and Therapy

[3] Siqing Jiang et al. J Steroid Biochem Mol Biol. Vitamin D/VDR attenuate cisplatin-induced AKI by down-regulating NLRP3/Caspase-1/GSDMD pyroptosis pathway

[4] Zhaoxin Hu et al. Cell Death Dis. VDR activation attenuate cisplatin induced AKI by inhibiting ferroptosis

[5] Sylvia Christakos et al. Physiol Rev. Vitamin D: Metabolism, Molecular Mechanism of Action, and Pleiotropic Effects

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