03/01/13 LY500307 (Erteberel) Datasheet | Buy LY500307 (Erteberel) from supplier Selleckchem.com

LY500307 (Erteberel) Datasheet

Technical Data LY500307 (Erteberel) Chemical Structure

DMSO 57 mg/mL Molecular Weight (MW) 282.33 Solubility (25°C) Water <1 mg/mL Formula C H O 18 18 3 Ethanol 57 mg/mL

2 years -20°C Powder CAS No. 533884-09-2 Return Policy Storage 2 weeks 4°C in DMSO Selleck Chemicals wishes you the best Synonyms N/A 6 months -80°C in DMSO possible online shopping experience with our 365 day unconditional Return Policy. If you are not satisfied with your Biological Activity purchase, either for protocol related or product related problems, you may Description LY500307 (SERBA-1) is a potent, selective receptor β agonist with EC50 of 0.66 nM. return any item(s) within 365 days from Targets β the original purchase date. Please see the following instructions when you [1] IC50 0.66 nM (EC50) return products.

LY500307 shows potent binding affinity for both ERα (Ki 2.68 nM) and ERβ (Ki 0.19 nM), which exhibits 1. All requests for returns should be 14-fold binding selectivity for the β isoform, generated using 3H- and recombinant, full-length, communicated to Selleck Chemicals human ERs in a competitive binding assay. LY500307 shows full agonist function in both ERα and prior to shipping. Any items returned to ERβ assays (>90% relative efficacy), displays potent inhibition toward ERβ with EC50 of 0.66 nM Selleck Chemicals should be in the exhibiting 32 fold specificity for ERβ than for ERα which has EC50 of 19.4 nM measured using a original packaging and in the same In vitro transcription assay in the cotransfected human prostate cancer PC3/ER (α or β)-ERE cell line. condition as originally purchased. LY500307/ERα and LY500307/ERβ X-ray cocrystal structures show significant differences in the 2. When returning purchased goods, manner in which LY500307 binds within the binding pockets. LY500307 displays a different orientation please inform us of the purchase order corresponding to a (ca. 180°) rotation on its bisphenol axis, and the A ring phenol of LY500307, while number or package tracking number. bound to histidine in both structures, locates to different sides of the imidazole functionality for this 3. Return shipping is absolutely FREE. interaction explaining the observed selectivity of LY500307 for ERβ. [1] 4. This offer is only valid for products purchased directly from Selleck and its Oral administration of LY500307 (0.01-0.05 mg/kg) in CD-1 mice produces the reduction on prostate authorized distributors. weights in a dose-response manner, has no effect on testes and SV weights in this dose range and no 5. Once your return request is received In vivo effect on T and DHT levels at up to 10× the minimum efficacy dose (0.1 mg/kg), while the nonselective and approved, your refund will be ER agonist (DES) shows significant regression of prostate, testes, and SV and also processed or automatically applied to lowering T and DHT. [1] your credit card within 7 days. Please note that depending on your credit card The phase II study to evaluate daily oral doses of LY500307 for 24 weeks in men with lower urinary tract company, it may take additional 2-10 Clinical Trials symptoms (LUTS) and prostatic enlargement secondary to benign prostatic hyperplasia (BPH) has business days for us to post the refund been terminated due to insufficient efficacy. to your account. Features LY500307 shows significantly higher binding activity toward ERβ than ERα. Toll Free:

Protocol (Only for Reference) (877) 796-6397 Kinase Assay: [1] -- USA and Canada only -- PC3 human prostatic adenocarcinoma cells are transiently cotransfected with plasmid carrying either full Fax: length human ERα or full length human ERβ and a reporter plasmid using fugene 6 transfection reagent. Cell-Based +1-713-796-9816 Human ERα or human ERβ are constitutively expressed using plasmids containing the cytomegalovirus Transcriptional (CMV) promoter. Reporter plasmids for the ER CTF assays contain 3X human ERE plus the thymidine Assays kinase (TK) promoter upstream of the luciferase reporter cDNA. Efficacy is determined relative to the Orders: reference molecule diethylstilbestrol. EC50 values are determined by computer fit to a concentration- +1-832-582-8158 response curve. [email protected]

Animal Study:[1] Tech Support: Animal Models CD-1 mice +1-832-582-8158 Formulation Dissolved in the solution containing 1% carbxymethyl cellulose and 0.25% Tween 80. Ext:3 Monday–Friday Doses 0.01-0.05 mg/kg 9:00 AM–5:00 PM (Central Time)

Administration Oral gavage daily [email protected] We will contact you within one business day References [1] Norman BH, et al. J Med Chem, 2006, 49(21), 6155-6157. Website:

www.selleckchem.com PLEASE KEEP THE PRODUCT UNDER -20°C FOR LONG-TERM STORAGE.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE

Specific storage and handling information for each product is indicated on the product datasheet. Most Selleck products are stable under the recommended conditions. Products are sometimes shipped at a temperature that differs from the recommended storage temperature. Many products are stable in the short-term at temperatures that differ from that required for long-term storage. We ensure that the product is www.selleckchem.com/datasheet/LY500307-DataSheet.html 1/2 03/01/13 LY500307 (Erteberel) Datasheet | Buy LY500307 (Erteberel) from supplier Selleckchem.com

shipped under conditions that will maintain the quality, but save your shipping charges by using the most economical storage conditions for an overnight shipment. Upon receipt of the product, follow the storage recommendations on the product datasheet.

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