| Size | Price | |
|---|---|---|
| Other Sizes |
| Targets |
Fluorogen activating protein (FAP)-fluorogen binding[1] -log EC50: 6.61 (AM2.2-β2AR), 6.37 (AM2.2-GPR32)[1]
Fluorogen activating protein (FAP)-fluorogen binding. Fluorogen binding modulator-1 is a nonfluorescent inhibitor that modulates the interaction between fluorogen activating proteins (FAPs) and fluorogens. The compound targets the fluorogen binding site on FAPs, modulating the binding of fluorogenic dyes. It has -log EC50 values of 6.61 for AM2.2-β2AR and 6.37 for AM2.2-GPR32. |
|---|---|
| ln Vitro |
Fluorogen binding modulator-1 is a nonfluorescent inhibitor of fluorogen-FAP binding pairs. It modulates fluorogen binding with -log EC50 values of 6.61 for AM2.2-β2AR and 6.37 for AM2.2-GPR32. The compound's ability to modulate fluorogen-FAP interactions makes it a useful tool for studying protein labeling and imaging technologies.
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| ln Vivo |
No in vivo activity data has been reported for Fluorogen binding modulator-1 in the available literature. As a research tool for studying fluorogen-FAP interactions, its primary applications are in in vitro and cell-based systems for protein labeling and imaging. The compound is not intended for therapeutic use and its in vivo effects have not been characterized.
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| Enzyme Assay |
Binding assays are used to measure the modulatory activity of Fluorogen binding modulator-1 on fluorogen-FAP interactions. Fluorescence-based assays are performed using fluorogen activating proteins (e.g., AM2.2-β2AR and AM2.2-GPR32) and fluorogenic dyes in the presence of increasing concentrations of the compound. Changes in fluorescence intensity are measured to determine the compound's modulatory effects, with -log EC50 values of 6.61 and 6.37 for the respective FAPs.
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| Cell Assay |
Cellular assays using cells expressing fluorogen activating proteins (FAPs) are employed to evaluate the activity of Fluorogen binding modulator-1. Cells expressing AM2.2-β2AR or AM2.2-GPR32 are incubated with fluorogenic dyes in the presence of increasing concentrations of the compound. Fluorogen binding and activation are measured by fluorescence microscopy or flow cytometry to assess the compound's modulatory effects.
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| Animal Protocol |
No animal experiments have been reported for Fluorogen binding modulator-1. As a research tool for studying fluorogen-FAP interactions, its primary applications are in in vitro and cell-based systems. The compound is not intended for therapeutic use, and in vivo studies would only be relevant for specialized imaging applications.
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| ADME/Pharmacokinetics |
As a small molecule with molecular weight of 403.88 g/mol and molecular formula C16H22ClN3O5S, Fluorogen binding modulator-1 is a nonfluorescent compound. It is soluble in DMSO (10 mM). The compound is stored at -20°C with stability of at least 2 years. Pharmacokinetic properties have not been characterized as the compound is primarily used as a research tool for in vitro applications.
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| Toxicity/Toxicokinetics |
No toxicity data has been reported for Fluorogen binding modulator-1. As a research-use-only compound, it is not intended for human therapeutic use. Standard safety precautions should be observed when handling. Preliminary toxicity screening would typically involve assessment of cell viability in relevant cell lines prior to cellular assays. The compound is for research purposes only.
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| References | |
| Additional Infomation |
4-{N-[(4-chlorophenyl)sulfonyl]-N-methylglycyl}piperazine-1-carboxylic acid ethyl ester is a sulfonamide in which a methyl group and a 2-[4-(ethoxycarbonyl)piperazine-1-yl]-2-oxoethyl substituent are attached to the nitrogen atom, and a 4-chlorophenyl group is attached to the sulfonyl group. It is both a sulfonamide and a carbamate.
Fluorogen binding modulator-1 (CAS#: 510716-65-1) is a nonfluorescent small-molecule inhibitor that modulates fluorogen activating protein (FAP)-fluorogen binding. It has -log EC50 values of 6.61 for AM2.2-β2AR and 6.37 for AM2.2-GPR32. The compound has a molecular formula of C16H22ClN3O5S and molecular weight of 403.88. It is a research tool for studying protein labeling and imaging technologies. Purity: >98% (HPLC). |
| Molecular Formula |
C16H22CLN3O5S
|
|---|---|
| Molecular Weight |
403.88
|
| Exact Mass |
403.096
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| CAS # |
510716-65-1
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| PubChem CID |
1073012
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| Appearance |
Typically exists as solid at room temperature
|
| LogP |
1.3
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
26
|
| Complexity |
594
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CCOC(=O)N1CCN(CC1)C(=O)CN(C)S(=O)(=O)C2=CC=C(C=C2)Cl
|
| InChi Key |
GVRRKYYMISVYGI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H22ClN3O5S/c1-3-25-16(22)20-10-8-19(9-11-20)15(21)12-18(2)26(23,24)14-6-4-13(17)5-7-14/h4-7H,3,8-12H2,1-2H3
|
| Chemical Name |
ethyl 4-[2-[(4-chlorophenyl)sulfonyl-methylamino]acetyl]piperazine-1-carboxylate
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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 | 2.4760 mL | 12.3799 mL | 24.7598 mL | |
| 5 mM | 0.4952 mL | 2.4760 mL | 4.9520 mL | |
| 10 mM | 0.2476 mL | 1.2380 mL | 2.4760 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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