In Vivo (Add solvents to the product individually and in order.)
Homogeneous suspension
CMC-NA
≥5mg/ml
Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO
40%PEG300
5%Tween80
50%ddH2O
Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.
2.800mg/ml
(9.92mM)
Taking the 1 mL working solution as an example, add 50 μL of 56 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution
5% DMSO
95% Corn oil
Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.
0.450mg/ml
(1.59mM)
Taking the 1 mL working solution as an example, add 50 μL of 9 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
* <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.)
Preparing Stock Solutions
Biological Activity
Description
Erteberel (LY500307) is a potent, selective estrogen receptor
β agonist with EC50 of 0.66 nM,
demonstrating 32-fold selectivity against estrogen receptor
α. It is currently in Phase 2.
Targets
ERβ
0.66 nM(EC50)
In vitro
Erteberel (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. It 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. The cocrystal structures of
this compound with ERα and ERβ show significant
differences in the manner in which it binds within
the binding pockets. It displays a different orientation
corresponding to a (ca. 180°) rotation on its
bisphenol axis, and the A ring phenol, while
bound to histidine in both structures, locates to
different sides of the imidazole functionality for this
interaction explaining the observed selectivity for ERβ.
In Vivo
Oral administration of Erteberel (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.
Features
Demonstrates significantly higher binding activity
toward ERβ than ERα.
Sellecks 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.
