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Cat. No. M13345
LE135  Structure
Size Price Availability Quantity
5mg USD 280  USD280 In stock
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Quality Control & Documentation
Biological Activity

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.

Chemical Information
Molecular Weight 438.56
Formula C29H30N2O2
CAS Number 155877-83-1
Solubility (25°C) DMSO ≥ 40 mg/mL
Storage 2-8°C
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.


[1] 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

[2] Shijin Yin, et al. Br J Pharmacol. LE135, a retinoid acid receptor antagonist, produces pain through direct activation of TRP channels

[3] 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

[4] Zhen Li, et al. J Cell Biochem. The role of retinoic acid receptor inhibitor LE135 on the osteochondral differentiation of human bone marrow mesenchymal stem cells

[5] H Umemiya, et al. Yakugaku Zasshi. [Retinoid antagonists]

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Keywords: LE135 supplier, RAR/RXR, inhibitors, activators

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