| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 100mg | |||
| 250mg |
Purity: ≥98%
| Targets |
ERB-196 acts as an estrogen receptor agonist with non-steroidal selectivity. It binds to and activates estrogen receptors, mimicking the effects of endogenous estrogens. The non-steroidal nature of ERB-196 suggests that it may offer a different selectivity profile compared to steroidal estrogens, potentially providing tissue-specific effects. Its mechanism involves the modulation of estrogen receptor-mediated gene transcription, which can influence various physiological processes, including cell proliferation, differentiation, and inflammation.
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| ln Vitro |
In vitro, ERB-196 demonstrates estrogen receptor agonist activity. Specific in vitro assay data, such as IC50 or EC50 values for receptor binding or transactivation, are not detailed in the available sources. The compound is characterized as a non-steroidal selective estrogen receptor agonist. It has been shown to significantly reduce histopathologic evidence of injury to the gastrointestinal mucosal surface in in vivo models, indicating a protective effect on mucosal tissues.
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| ln Vivo |
A non-steroidal selective agonist of the estrogen receptor-beta (ERβ) is ERB-196. Histopathological evidence of gastrointestinal mucosal surface damage was significantly reduced by ERB-196 (control, 0.7±0.1 vs. 2.3±0.2; p<0.05). The 10-cm segment of the small intestinal mucosa demonstrated a higher degree of mucosal mass preservation compared to the control treatment (63±20 [ERB-196] vs. 31±24 [control]); however, this difference was not statistically significant (p<0.06). ERB-196 administration proved to be very successful in averting death. According to the model of neutropenic rats, ERB-196 led to a significant increase in survival when compared to vehicle controls [1].
In vivo, ERB-196 has been shown to significantly reduce histopathologic evidence of injury to the gastrointestinal mucosal surface (0.7±0.1 vs. 2.3±0.2 for control; p<0.05). The mucosal mass of 10-cm segments of small bowel mucosa showed better preservation with ERB-196 treatment (63±20) compared to control (31±24), though this difference was not statistically significant (p<0.06). ERB-196 administration was highly effective in preventing lethality in preclinical models, significantly increasing survival compared to vehicle control. |
| Enzyme Assay |
A receptor binding assay for ERB-196 would typically involve incubating various concentrations of the test compound with estrogen receptor (ERα or ERβ) in a buffer containing a radiolabeled ligand (e.g., [³H]-estradiol). After incubation at 4°C for an appropriate period (e.g., 2-16 hours), bound and free ligands are separated using a filtration method or charcoal-dextran precipitation. The amount of radioligand bound to the receptor is measured by scintillation counting. The IC50 value for displacement of the radioligand is calculated from the competition curve. Specific protocols are not detailed in the available literature.
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| Cell Assay |
To evaluate ERB-196's activity, a reporter gene assay can be performed using HEK293 or MCF-7 cells transiently or stably transfected with an estrogen-responsive element (ERE)-luciferase reporter construct and estrogen receptor expression plasmids. Cells are seeded in 96-well plates and treated with varying concentrations of ERB-196 (e.g., 0.01 nM to 10 μM) for 24-48 hours. Luciferase activity is measured using a luminometer after adding the appropriate substrate. EC50 values for transcriptional activation are calculated. Cell viability is assessed using a standard cytotoxicity assay to distinguish specific receptor-mediated effects from non-specific toxicity.
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| Animal Protocol |
In a neutropenic rat model, ERB-196 has been evaluated for its protective effects. Animals are treated with ERB-196 or vehicle control, and the compound's ability to prevent gastrointestinal injury and improve survival is assessed. The specific dosing regimen (e.g., dose, route of administration, frequency) is not detailed in the available summaries. The key endpoints measured include histopathologic scoring of the gastrointestinal mucosa, preservation of mucosal mass, and overall survival rates. Efficacy is expressed as the reduction in injury score and the increase in survival percentage compared to the control group.
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| ADME/Pharmacokinetics |
Specific pharmacokinetic data for ERB-196, such as half-life, bioavailability, or volume of distribution, are not provided in the available sources. The compound is a small molecule with a molecular weight of 279.27, which is generally favorable for oral bioavailability. Standard pharmacokinetic studies would typically involve administering the compound to rodents or other animal models and measuring plasma concentrations over time using LC-MS/MS to determine key PK parameters.
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| Toxicity/Toxicokinetics |
Specific toxicity data for ERB-196 are not detailed in the available references. In the in vivo studies described, the compound was administered at doses that were effective in preventing lethality without mention of overt toxicity. This suggests that ERB-196 may have a tolerable safety profile at the tested doses. As a research compound, it is intended for laboratory use only and is not approved for human therapeutic applications.
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| References | |
| Additional Infomation |
ERB-196 is also known as WAY-202196. Its chemical name is 3-(3-fluoro-4-hydroxyphenyl)-7-hydroxy-1-naphthonitrile. The compound has a CAS number of 550997-55-2 and a molecular weight of 279.26. It is classified under endocrinology/hormones and is used as an estrogen receptor agonist in research. The product is available with a purity of 99% and is stored as a powder at -20°C for long-term stability.
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| Molecular Formula |
C17H10NO2F
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|---|---|
| Molecular Weight |
279.2652
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| Exact Mass |
279.07
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| CAS # |
550997-55-2
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| PubChem CID |
6102691
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| Appearance |
Light brown to brown solid powder
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| LogP |
3.928
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
21
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| Complexity |
420
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
NSSOSHDCWCMNDM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H10FNO2/c18-16-7-10(2-4-17(16)21)12-5-11-1-3-14(20)8-15(11)13(6-12)9-19/h1-8,20-21H
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| Chemical Name |
3-(3-fluoro-4-hydroxyphenyl)-7-hydroxynaphthalene-1-carbonitrile
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| Synonyms |
ERB-196; WAY-202196; ERB196; WAY202196; ERB 196; WAY 202196;
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
Ethanol : ~16 mg/mL (~57.29 mM)
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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 | 3.5808 mL | 17.9038 mL | 35.8076 mL | |
| 5 mM | 0.7162 mL | 3.5808 mL | 7.1615 mL | |
| 10 mM | 0.3581 mL | 1.7904 mL | 3.5808 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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