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AGN 194310

Cat. No. M10777
AGN 194310 Structure
Synonym:

VTP-194310

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Biological Activity

AGN 194310 (VTP-194310) is a highly affinity, potent, selective pan antagonist of retinoic acid receptors (RARs) against RARα, RARβ, RARγ Kd The values are 3 nM, 2 nM, and 5 nM, respectively.

Chemical Information
Molecular Weight 424.55
Formula C28H24O2S
CAS Number 229961-45-9
Solubility (25°C) DMSO ≥ 20 mg/mL
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] Thomas Lind, et al. PLoS One. Vitamin a is a negative regulator of osteoblast mineralization

[2] Eugenia Prus, et al. Leuk Lymphoma. Retinoic acid receptor antagonist inhibits CD38 antigen expression on human hematopoietic cells in vitro

[3] R G Keedwell, et al. Br J Cancer. An antagonist of retinoic acid receptors more effectively inhibits growth of human prostate cancer cells than normal prostate epithelium

[4] Liv M I Austenaa, et al. FASEB J. Vitamin A status significantly alters nuclear factor-kappaB activity assessed by in vivo imaging

[5] C R Walkley, et al. Leukemia. Retinoic acid receptor antagonism in vivo expands the numbers of precursor cells during granulopoiesis

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