| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Y-134 specifically targets estrogen receptor α (ERα) and estrogen receptor β (ERβ), with significant selectivity for ERα. Estrogen receptors are nuclear receptors that mediate the effects of the hormone estrogen on gene expression in target tissues. ERα and ERβ are encoded by different genes and have distinct tissue distribution patterns and functions. Y-134 binds to ERα with a Ki of 0.09 nM and to ERβ with a Ki of 11.31 nM, demonstrating approximately 125-fold selectivity for ERα over ERβ. The compound is a derivative of raloxifene, a known SERM, and exhibits strong antagonist activity against both ERα and ERβ. Y-134 shows no cross-reactivity with mineralocorticoid, glucocorticoid, androgen, or progesterone receptors.
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| ln Vitro |
Y134 demonstrated strong antagonistic effect against ER in CV-1 cells co-transfected with plasmids expressing ERα or ERβ and estrogen-responsive element-driven luciferase, with IC50 values for ERα and ERβ and for ERβ, respectively. 2.94 nM [1]. Y134 (0.01 nM-10 μM; 6 d) suppresses the growth of ER-expressing breast cancer cells (MCF-7 and T47D) in response to estrogen [1].
In vitro, Y-134 demonstrates high affinity binding to estrogen receptor α with a Ki of 0.09 nM and to estrogen receptor β with a Ki of 11.31 nM. The compound exhibits approximately 125-fold selectivity for ERα over ERβ. As a SERM, Y-134 exhibits strong antagonist activity against both ERα and ERβ. The compound shows no cross-reactivity with mineralocorticoid, glucocorticoid, androgen, or progesterone receptors, indicating a high degree of receptor selectivity. Y-134's selectivity for ERα over ERβ and its lack of cross-reactivity with other steroid hormone receptors make it a valuable tool for studying ERα-mediated signaling pathways. |
| ln Vivo |
Y134 (1-3 mg/kg/day; orally for 3 days) abolishes E2-induced terminal mammary bud (TEB) growth in ovariectomized rats. Y134 inhibits E2-induced uterine cell proliferation in a dose-dependent manner [1].
In vivo, Y-134 is orally active and has been investigated in preclinical models. As a selective estrogen receptor modulator with ERα selectivity, the compound is expected to modulate estrogen receptor signaling in target tissues. The compound's oral activity supports its use in chronic dosing studies. Y-134's selectivity for ERα over ERβ and its lack of cross-reactivity with other steroid hormone receptors suggest a favorable specificity profile for studying ERα-mediated effects. Specific in vivo efficacy data is available from the primary literature describing the compound. |
| Enzyme Assay |
The binding affinity of Y-134 to estrogen receptors is assessed using radioligand binding assays. Recombinant human ERα or ERβ is incubated with a radiolabeled estrogen ligand (such as [³H]-estradiol) in the presence of varying concentrations of the test compound. Nonspecific binding is determined using a competing estrogen. Ki values are calculated from competition binding curves using appropriate mathematical models. Receptor selectivity is assessed by screening the compound against panels of other steroid hormone receptors, including mineralocorticoid, glucocorticoid, androgen, and progesterone receptors. Functional activity (agonist, antagonist, or partial agonist) is determined using cell-based reporter assays.
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| Cell Assay |
Cell viability assay [1]
Cell Types: MCF-7, T47, MDA-MB-231 Cell Tested Concentrations: 0.01 nM-10 μM Incubation Duration: 6 days Experimental Results: Inhibition of estrogen-stimulated MCF-7 and T47D cell proliferation. There was no effect on MDA-MB-231 cells except for some cytotoxicity observed at high concentrations. Cellular assays for Y-134 are performed using cells expressing estrogen receptors, such as MCF-7 breast cancer cells (which express ERα) or cells transfected with ERα or ERβ expression constructs. Cells are treated with varying concentrations of the compound in the presence or absence of estradiol. Estrogen-responsive reporter gene assays are used to quantify ER-mediated transcriptional activity. Cell proliferation assays are performed to assess the compound's effects on estrogen-dependent cell growth. ER target gene expression is measured by qRT-PCR. |
| Animal Protocol |
Animal/Disease Models: 4weeks old female SD (SD (Sprague-Dawley)) rats, underwent ovariectomy [1]
Doses: 1, 3 mg/kg Route of Administration: Oral daily for 3 days Experimental Results: Elimination of the effect of E2 in a dose-dependent manner . In vivo studies of Y-134 are conducted in rodent models of estrogen-dependent diseases, such as breast cancer or osteoporosis. The compound is typically administered orally via gavage. Tumor growth is monitored in cancer models. Bone density and bone turnover markers are assessed in osteoporosis models. Uterine weight is measured as a marker of estrogenic activity. Pharmacodynamic markers of ER modulation are assessed in target tissues. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of Y-134 (molecular weight 472.60, molecular formula C28H28N2O3S) have been characterized. The compound is orally active and is formulated in suitable vehicles for oral administration. The compound is soluble in DMSO and is typically formulated in vehicles such as PEG-based solutions or oil-based formulations for oral dosing. Storage recommendations include appropriate conditions for research chemicals. Comprehensive PK parameters including oral bioavailability, half-life, and maximum concentration are available from the primary literature.
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| Toxicity/Toxicokinetics |
Y-134 is intended for research use only and is not approved for human therapeutic applications. Comprehensive toxicological evaluations, including acute and repeat-dose toxicity studies in animal models, have been conducted as part of preclinical development. The compound's mechanism of action—modulating estrogen receptor signaling—may affect reproductive tissues and bone, and these effects would be carefully evaluated in toxicology studies. Standard safety pharmacology assessments would include evaluation of effects on reproductive function, bone metabolism, and cardiovascular function.
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| References | |
| Additional Infomation |
[6-hydroxy-2-(4-hydroxyphenyl)-1-benzothiophen-3-yl]-[4-(4-propyl-2-yl-1-piperazinyl)phenyl]methyl ketone is an aromatic ketone.
Y-134 (Y134) is a selective estrogen receptor modulator (SERM) that displays selectivity for ERα over ERβ, with Ki values of 0.09 nM and 11.31 nM, respectively. The compound is a derivative of raloxifene, a known SERM used clinically for the treatment of osteoporosis and breast cancer. Y-134 exhibits strong antagonist activity against both ERα and ERβ and is orally active. The compound shows no cross-reactivity with mineralocorticoid, glucocorticoid, androgen, or progesterone receptors. Y-134 is a valuable research tool for studying ERα-mediated signaling pathways and for validating ERα as a therapeutic target. The compound is available with purity ≥98% for research use. |
| Molecular Formula |
C28H28N2O3S
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| Molecular Weight |
472.603
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| Exact Mass |
472.182
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| Elemental Analysis |
C, 71.16; H, 5.97; N, 5.93; O, 10.16; S, 6.78
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| CAS # |
849662-80-2
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| PubChem CID |
11784736
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.282g/cm3
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| Boiling Point |
722.282ºC at 760 mmHg
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| Flash Point |
390.623ºC
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| Index of Refraction |
1.673
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| LogP |
5.743
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
34
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| Complexity |
681
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| Defined Atom Stereocenter Count |
0
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| SMILES |
OC1C=CC2C(C(C3C=CC(N4CCN(C(C)C)CC4)=CC=3)=O)=C(C3C=CC(O)=CC=3)SC=2C=1
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| InChi Key |
LQEOPHGPHCWOAC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C28H28N2O3S/c1-18(2)29-13-15-30(16-14-29)21-7-3-19(4-8-21)27(33)26-24-12-11-23(32)17-25(24)34-28(26)20-5-9-22(31)10-6-20/h3-12,17-18,31-32H,13-16H2,1-2H3
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| Chemical Name |
[6-Hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl]-[4-[4-(1-methylethyl)-1-piperazinyl]phenyl]methanone
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| Synonyms |
Y-134; Y 134; Y134;
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1160 mL | 10.5798 mL | 21.1595 mL | |
| 5 mM | 0.4232 mL | 2.1160 mL | 4.2319 mL | |
| 10 mM | 0.2116 mL | 1.0580 mL | 2.1160 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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