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Technical Data
| Formula | C18H18O3 |
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| Molecular Weight | 282.33 | CAS No. | 533884-09-2 | |
| Solubility (25°C)* | In vitro | DMSO | 57 mg/mL (201.89 mM) | |
| Ethanol | 57 mg/mL (201.89 mM) | |||
| Water | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Preparing Stock Solutions
Biological Activity
| Description | LY500307 is a potent, selective estrogen receptor β agonist with EC50 of 0.66 nM, 32-fold selectivity against estrogen receptor α. Phase 2. | ||
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| Targets |
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| In vitro | LY500307 shows potent binding affinity for both ERα (Ki 2.68 nM) and ERβ (Ki 0.19 nM), which exhibits 14-fold binding selectivity for the β isoform, generated using 3H-estradiol and recombinant, full-length, human ERs in a competitive binding assay. LY500307 shows full agonist function in both ERα and ERβ assays (>90% relative efficacy), displays potent inhibition toward ERβ with EC50 of 0.66 nM exhibiting 32 fold specificity for ERβ than for ERα which has EC50 of 19.4 nM measured using a transcription assay in the cotransfected human prostate cancer PC3/ER (α or β)-ERE cell line. LY500307/ERα and LY500307/ERβ X-ray cocrystal structures show significant differences in the manner in which LY500307 binds within the binding pockets. LY500307 displays a different orientation corresponding to a (ca. 180°) rotation on its bisphenol axis, and the A ring phenol of LY500307, while bound to histidine in both structures, locates to different sides of the imidazole functionality for this interaction explaining the observed selectivity of LY500307 for ERβ. [1] | ||
| In vivo | Oral administration of LY500307 (0.01-0.05 mg/kg) in CD-1 mice produces the reduction on prostate weights in a dose-response manner, has no effect on testes and SV weights in this dose range and no effect on T and DHT levels at up to 10 × the minimum efficacy dose (0.1 mg/kg), while the nonselective ER agonist diethylstilbestrol (DES) shows significant regression of prostate, testes, and SV and also lowering T and DHT. [1] | ||
| Features | Demonstrates significantly higher binding activity toward ERβ than ERα. |
Protocol (from reference)
| Animal Study:[1] |
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Selleck's Erteberel (LY500307) has been cited by 1 publication
| The Role of Estrogen and Estrogen Analogues in Friedreich’s Ataxia Cytoprotection. [Timothy E. Richardson, et al. University of North Texas, 2014, Health Science Center at Fort Worth ] |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.