| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg | |||
| 500mg | |||
| 1g | |||
| Other Sizes |
| Targets |
WYE-176182 targets the apical sodium-dependent bile salt transporter (SLC10A2). SLC10A2 is responsible for the reabsorption of bile salts from the intestine, playing a critical role in enterohepatic circulation. Inhibition of SLC10A2 reduces bile salt reabsorption, which can lower cholesterol levels and modulate metabolic pathways. The compound is a valuable tool for studying bile acid metabolism.
|
|---|---|
| ln Vitro |
Biological activity of WYE-176182 is characterized by its ability to inhibit the SLC10A2 bile salt transporter. It functions as an antagonist of this transporter. Specific potency values such as IC50 have not been extensively reported in the available literature. The compound is used in research to study bile acid transport and its physiological and pathological roles.
|
| ln Vivo |
In vivo activity of WYE-176182 has not been extensively reported in the available literature. As an SLC10A2 inhibitor, the compound would be expected to reduce bile salt reabsorption and potentially lower cholesterol levels in vivo. Further studies would be required to evaluate its pharmacokinetics, efficacy, and therapeutic potential in animal models of metabolic and gastrointestinal diseases.
|
| Enzyme Assay |
SLC10A2 transporter activity is measured using cell-based uptake assays. Cells expressing SLC10A2 are incubated with radiolabeled or fluorescent bile salts in the presence of WYE-176182 at varying concentrations. Uptake is measured by scintillation counting or fluorescence detection. Inhibition is calculated from the reduction in bile salt uptake. IC50 values are determined from dose-response curves.
|
| Cell Assay |
Cellular activity of WYE-176182 is evaluated in cells expressing the SLC10A2 bile salt transporter. Cells are treated with the compound at varying concentrations, and bile salt uptake is measured using labeled substrates. The compound's ability to inhibit transporter-mediated bile salt uptake is assessed. Cellular toxicity may also be evaluated using cell viability assays.
|
| Animal Protocol |
In vivo evaluation of WYE-176182 would typically involve animal models of hypercholesterolemia or bile acid metabolism disorders. Animals would be administered the compound orally or intravenously at various doses. Plasma and tissue bile salt levels would be measured. Efficacy would be evaluated by assessing changes in cholesterol levels and bile acid profiles. Such studies have not been extensively reported for this compound.
|
| ADME/Pharmacokinetics |
WYE-176182 has a molecular formula of C13H10N2O6S and a molecular weight of 322.29. It is stored as powder at -20°C for up to 3 years. In solvent, it can be stored at -80°C for up to 6 months or at -20°C for up to 1 month. The compound is a sulfonamide derivative. Its physicochemical properties support its use in transporter inhibition studies.
|
| Toxicity/Toxicokinetics |
Toxicological data for WYE-176182 are limited, as the compound is for research use only. It is not intended for human or therapeutic use. Standard laboratory safety precautions should be followed when handling the compound. Comprehensive toxicology profiling would be required for clinical development.
|
| Additional Infomation |
WYE-176182 is an inhibitor of the apical sodium-dependent bile salt transporter (SLC10A2). It is also known as 4-[(3-nitrophenyl)sulfonylamino]benzoic acid. The compound is used in research to study bile acid transport and its role in metabolic diseases. Inhibition of SLC10A2 reduces bile salt reabsorption, which has implications for cholesterol metabolism and gastrointestinal physiology. WYE-176182 is a valuable tool for studying enterohepatic circulation and bile acid homeostasis.
|
| Molecular Formula |
C13H10N2O6S
|
|---|---|
| Molecular Weight |
322.291
|
| Exact Mass |
322.026
|
| Elemental Analysis |
C, 48.45; H, 3.13; N, 8.69; O, 29.78; S, 9.95
|
| CAS # |
59923-19-2
|
| PubChem CID |
3091374
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.588g/cm3
|
| Boiling Point |
557ºC at 760 mmHg
|
| Flash Point |
290.6ºC
|
| Index of Refraction |
1.674
|
| LogP |
3.77
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
22
|
| Complexity |
516
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C1=CC(=CC(=C1)S(=O)(=O)NC2=CC=C(C=C2)C(=O)O)[N+](=O)[O-]
|
| InChi Key |
CXOGYGMKNVZTHS-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C13H10N2O6S/c16-13(17)9-4-6-10(7-5-9)14-22(20,21)12-3-1-2-11(8-12)15(18)19/h1-8,14H,(H,16,17)
|
| Chemical Name |
4-[[(3-Nitrophenyl)sulfonyl]amino]benzoic acid
|
| Synonyms |
WYE-176182; WYE 176182; WYE176182;
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 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
|
|---|---|
| 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 | 3.1028 mL | 15.5140 mL | 31.0280 mL | |
| 5 mM | 0.6206 mL | 3.1028 mL | 6.2056 mL | |
| 10 mM | 0.3103 mL | 1.5514 mL | 3.1028 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
