TargetMol

Acolbifene

Product Code:
 
TAR-T10239
Product Group:
 
Inhibitors and Activators
Supplier:
 
TargetMol
Regulatory Status:
 
RUO
Shipping:
 
cool pack
Storage:
 
-20℃
1 / 1
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TAR-T10239-50mg50mgEnquire
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TAR-T10239-1mg1mg£132.00
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TAR-T10239-1mL1 mL * 10 mM (in DMSO)£230.00
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Further Information

Bioactivity:
Acolbifene is a selective antagonist of estrogen receptors with IC50s of 2 nM and 0.4 nM for estradiol-induced transcriptional activity of ERα and ERβ. Acolbifene shows an anticarcinogenic property.
CAS:
182167-02-8
Formula:
C29H31NO4
Molecular Weight:
457.56
Pathway:
Endocrinology/Hormones
Purity:
0.98
SMILES:
CC1=C([C@@H](OC=2C1=CC=C(O)C2)C3=CC=C(OCCN4CCCCC4)C=C3)C5=CC=C(O)C=C5
Target:
Estrogen Receptor/ERR

References

1. A Tremblay, et al. EM-800, a novel antiestrogen, acts as a pure antagonist of the transcriptional functions of estrogen receptors alpha and beta. Endocrinology. 1998 Jan;139(1):111-8. 2. Christian Lemieux, et al. The selective estrogen receptor modulator acolbifene reduces cholesterolemia independently of its anorectic action in control and cholesterol-fed rats. J Nutr. 2005 Sep;135(9):2225-9. 3. F Labrie, et al. EM-652 (SCH 57068), a third generation SERM acting as pure antiestrogen in the mammary gland and endometrium. J Steroid Biochem Mol Biol. Apr-Jun 1999;69(1-6):51-84. 4. Sylvain Gauthier, et al. Synthesis and structure-activity relationships of analogs of EM-652 (acolbifene), a pure selective estrogen receptor modulator. Study of nitrogen substitution. J Enzyme Inhib Med Chem. 2005 Apr;20(2):165-77. 5. Wang T, et al. Recent advances in selective estrogen receptor modulators for breast cancer. Mini Rev Med Chem. 2009 Sep;9(10):1191-201.