LE135 is an effective RAR antagonist, which can selectively bind RARα (Ki is 1.4 μM) and RARβ (Ki is 220 nM), and has a higher affinity for RARβ. The LE135 is highly selective for RARγ, RXRα, RXRβ and RXRγ. LE135 is also a vitamin A acid receptor antagonist.
|Solubility (25°C)||DMSO ≥ 40 mg/mL|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
 Solvig Diederichs, et al. Cell Physiol Biochem. Regulating chondrogenesis of human mesenchymal stromal cells with a retinoic Acid receptor-Beta inhibitor: differential sensitivity of chondral versus osteochondral development
 Sally E Henderson, et al. Am J Vet Res. Chondrogenic effects of exogenous retinoic acid or a retinoic acid receptor antagonist (LE135) on equine chondrocytes and bone marrow-derived mesenchymal stem cells in monolayer culture
|Related RAR/RXR Products|
KCL-286 is an orally active retinoic acid receptor-beta (RAR-beta) agonist for studies related to spinal cord injury.
XS-060 is a potent anticancer agent and RXRα antagonist.
BPA-B9 is a RXRα ligand and antagonist targeting the pRXRα-PLK1 interaction.
|ER 50891 quarterhydrate
ER 50891 quarterhydrate is a potent antagonist of retinoic acid receptor α(RARα).
4-Hydroxyretinoic acid (4-HRA) is a naturally occurring retinoid derivative with diverse biological effects.
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