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Bexarotene | Retinoid RXR agonist

CAS:
153559-49-0
Catalog Number:
10-2121
Activity:
Retinoid RXR agonist
Alternate Names:
LGD-1069, SR-11247
Chemical Name:
4-[1-(5,6,7,8-Tetrahydro-3,5,5,8,8-pentamethyl-2-naphthalenyl)ethenyl]benzoic acid
Molecular Weight:
348.49
Molecular Formula:
C24H28O2
Solubility:
Soluble in DMSO (up to 60 mg/ml) or in Ethanol (up to 10 mg/ml with warming).
Physical Properties:
White solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 1 week.
Shipping Code:
RT

Bexarotene (153559-49-0) is a highly potent and selective retinoid X receptor (RXR) agonist (EC50=28, 25, 20 nM for RXRα, β, γ respectively).1 Clinically useful antineoplastic agent for cutaneous T-cell lymphoma2 Causes complete regression of mammary carcinoma3. Bexarotene significantly increases clearance of soluble β-amyloid in a mouse Alzheimer’s model and increases cognitive ability.4 Reverses apoE4-driven brain pathology and behavioral deficits in vivo.5

References/Citations:

1) Boehm et al. (1995), Design and synthesis of potent retinoid X receptor selective ligands that induce apoptosis in leukemia cells; J. Med. Chem., 38 3146
2) Gniadecki et al. (2007), The optimal use of bexarotene in cutaneous T-cell lymphoma; Br. J. Dermatol., 157 433
3) Bischoff et al. (1998), Beyond tamoxifen: the retinoid X receptor-selective ligand LGD1069 (TARGRETIN) causes complete regression of mammary carcinoma; Cancer Res., 58 479
4) Cramer et al. (2012), ApoE-directed therapeutics rapidly clear β-amyloid and reverse deficits in AD mouse models; Science, 335 1503
5) Boehm-Cagan and Michaelson (2014), Reversal of apoE4-driven brain pathology and behavioral deficits by bexarotene; J. Neurosci., 34 7293

Bexarotene | Retinoid RXR agonist is also available in the Cellular Metabolism Library.
CAS:
153559-49-0
Catalog Number:
10-2121
Activity:
Retinoid RXR agonist
Alternate Names:
LGD-1069, SR-11247
Chemical Name:
4-[1-(5,6,7,8-Tetrahydro-3,5,5,8,8-pentamethyl-2-naphthalenyl)ethenyl]benzoic acid
Molecular Weight:
348.49
Molecular Formula:
C24H28O2
Solubility:
Soluble in DMSO (up to 60 mg/ml) or in Ethanol (up to 10 mg/ml with warming).
Physical Properties:
White solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 1 week.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

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