LY500307 Inhibitor CAS No. 533884-09-2

Cat. No.	Name	Size	Price
KI0501	LY500307	5 mg	$332
	LY500307	10 mg	$624
	LY500307	50 mg	$1896
	LY500307	200 mg	$4830

Chemical Characteristic

Product Name	LY500307
Synonyms	Erteberel, SERBA-1
CAS No.	533884-09-2
Molecular Weight	282.33
Formula	C₁₈H₁₈O₃
Chemical Name	(3aS,4R,9bR)-1,2,3,3a,4,9b-Hexahydro-4-(4-hydroxyphenyl)cyclopenta[c][1]benzopyran-8-ol
Smiles	[C@@H]1([C@@H]2[C@H](c3c(O1)ccc(c3)O)CCC2)c1ccc(cc1)O
Chemical Structure

Biological activities

LY500307 is a potent, selective estrogen receptor (ER) β agonist.^[1] The EC50 of LY500307 is 0.66 nM. LY500307 potently binds both ERα and ERβ with Ki of 2.68 and 0.19 nM, respectively. LY500307 inhibits ERα with an EC50 of 19.4 nM measured using a transcription assay in the cotransfected human prostate cancer PC3/ER (α or β)-ERE cell line. Therefore, LY500307 exhibits 32 fold specificity for ERβ than for ERα. LY500307 binds to histidine. LY500307 locates to different sides of the imidazole functionality for this interaction explaining the observed selectivity of LY500307 for ERβ.^[2] In vitro, LY500307 induces apoptosis in both prostate epithelial and stromal cell lines. In a mouse model, oral administration of LY500307 for 14 days reduces prostate weight without any significant change in circulating testosterone concentrations or seminal vesicle/testes weights.^[1] LY500307 (0.01-0.05 mg/kg) reduces prostate weights in a dose-response manner in CD-1 mice.^[2]

Protocols

LY500307 is dissolved in the solution containing 1% carbxymethyl cellulose and 0.25% Tween 80.^[2]

References

[1] Gravas S, et al. Investigational therapies targeted to the treatment of benign prostatic hyperplasia. Expert Opin Investig Drugs. 2013, 22(3): 357-368. [2] Norman BH, et al. Benzopyrans are selective estrogen receptor beta agonists with novel activity in models of benign prostatic hyperplasia. J Med Chem. 2006, 49(21): 6155-6157.

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