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AGN194204

Cat. No. M21366
AGN194204 Structure
Synonym:

IRX4204; NRX194204; VTP 194204

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Quality Control & Documentation
Biological Activity

AGN194204 (IRX4204) is inactive against RAR and is an orally active and selective RXR agonist with Kd values of 0.4 nM, 3.6 nM and 3.8 nM for RXRα, RXRβ and RXRγ, respectively, and EC50s of 0.2 nM, 0.8 nM and 0.08 nM. AGN194204 has anti-inflammatory and anti-cancer effects.

Chemical Information
Molecular Weight 352.51
Formula C24H32O2
CAS Number 220619-73-8
Solubility (25°C) N/A
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] Reuven Rasooly, et al. J Immunol. Retinoid x receptor agonists increase bcl2a1 expression and decrease apoptosis of naive T lymphocytes

[2] Xiangquan Li, et al. J Biol Chem. Distinct mechanisms of glucose lowering by specific agonists for peroxisomal proliferator activated receptor gamma and retinoic acid X receptors

[3] Sivaprakasam Balasubramanian, et al. Carcinogenesis. Suppression of human pancreatic cancer cell proliferation by AGN194204, an RXR-selective retinoid

[4] Paolo E Macchia, et al. Am J Physiol Endocrinol Metab. RXR receptor agonist suppression of thyroid function: central effects in the absence of thyroid hormone receptor

[5] Charles B Stephensen, et al. J Immunol. Vitamin A enhances in vitro Th2 development via retinoid X receptor pathway

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Keywords: AGN194204, IRX4204; NRX194204; VTP 194204 supplier, RAR/RXR, inhibitors, activators


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