LE 135A retinoic acid receptor antagonist

LE 135 (CAS 155877-83-1)

LE 135 | CAS 155877-83-1 is rated 5.0 out of 5 by 1.
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Synonym: LE-135
Application: A retinoic acid receptor antagonist
CAS Number: 155877-83-1
Purity: ≥97%
Molecular Weight: 438.57
Molecular Formula: C29H30N2O2
* Refer to Certificate of Analysis for lot specific data (including water content).
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LE 135 is a retinoic acid receptor antagonist which displays moderate selectivity for RARβ over RARα Additionally, LE 135 is highly selective over RARγ and RXRα This compound also Inhibits human HL-60 leukemia cell differentiation induced by the retinoid Am80.


References

1. Eyrolles, L., et al. 1994. J. Med. Chem. 37: 1508-1517. PMID: 8182710
2. Umemiya, H., et al. 1997. J. Med. Chem. 40: 4222-4234. PMID: 9435893
3. Li, Y., et al. 1999. J. Biol. Chem. 274: 15360-15366. PMID: 10336422

Physical State :
Solid
Solubility :
Soluble in DMSO (100 mM).
Storage :
Store at 4° C
Melting Point :
249.57° C (Predicted)
Boiling Point :
601.34° C at 760 mmHg (Predicted)
Density :
1.18 g/cm3 (Predicted)
Refractive Index :
n20D 1.63 (Predicted)
IC50 :
HL-60 leukemia cell differentiation induced by Am80: IC50 = 150 nM (human)
Ki Data :
RARβ: Ki= 0.22 µM; RARα : Ki= 1.4 µM
pK Values :
pKa: 3.02 (Predicted), pKb: 4.1 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
10410894
MDL Number :
MFCD06798318
SMILES :
CC1(CCC(C2=CC3=C(C=C21)N=C(C4=CC=CC=C4N3C)C5=CC=C(C=C5)C(=O)O)(C)C)C

Download SDS (MSDS)

Certificate of Analysis

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LE 135  Product Citations

See how others have used LE 135. Click on the entry to view the PubMed entry .

Citations 1 to 1 of 1 total

PMID: # 24308840  Yin, S. et al. 2014. Br. J. Pharmacol. 171: 1510-20.

Citations 1 to 1 of 1 total
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Rated 5 out of 5 by from Yin Yin, S. et al. (PubMed 24308840) found that LE 135, a retinoid acid receptor antagonist, produces pain through direct activation of TRP channels. -SCBT Publication Review
Date published: 2015-04-28
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