| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
Poly(ADP-ribose) glycohydrolase (PARG). TFMU-ADPr diammonium acts as a general substrate for monitoring PARG activity. PARG is the primary enzyme responsible for the catabolism of poly(ADP-ribose) (PAR) chains, which are synthesized by PARP enzymes during DNA damage repair and other cellular processes.
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| ln Vitro |
TFMU-ADPr diammonium directly reports total PAR hydrolase activity by releasing a fluorophore. It is a versatile tool for evaluating small molecule inhibitors in vitro and probing the regulation of ADP-ribosyl catabolic enzymes. This assay system enables high-throughput screening for PARG inhibitors and allows for the detailed characterization of their mechanism of action in enzymatic assays.
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| ln Vivo |
In vivo activity data for TFMU-ADPr diammonium are not applicable, as it is a substrate used exclusively for in vitro enzyme assays to monitor PARG activity. It is not administered to animals for therapeutic efficacy studies. The compound is used to measure PARG activity in cell lysates or tissue homogenates from experimental models, helping to understand the enzyme's role in cellular homeostasis.
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| Enzyme Assay |
PARG enzyme activity assay: Recombinant PARG enzyme (0.1-1.0 nM) is incubated with increasing concentrations of TFMU-ADPr diammonium (0-100 uM) in assay buffer (50 mM HEPES, pH 7.5, 50 mM NaCl, 3 mM MgCl2, 0.01% Triton X-100, 1 mM DTT) for 15-60 min at 37degC. The reaction is terminated by adding a stop solution. Fluorescence is measured (ex=380 nm, em=460 nm), and kinetic parameters (Km, Vmax) are calculated.
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| Cell Assay |
Cell-based PARG activity assay: Cells (2-5 × 10⁵) are lysed in a buffer containing 0.5% Triton X-100 and protease inhibitors. Lysates (10-50 ug protein) are incubated with TFMU-ADPr diammonium (50-100 uM) in PARG assay buffer for 60 min at 37degC. Released fluorescence is measured as above. PARG activity can be normalized to protein concentration. For inhibitor studies, compounds are pre-incubated with lysates before adding substrate.
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| Animal Protocol |
Not directly applicable. TFMU-ADPr diammonium is a biochemical substrate used in cell-free and cell-based assays for PARG activity. It may be used in ex vivo experiments to measure PARG activity in tissue homogenates from animal models of disease. The diammonium salt form enhances solubility and stability for enzymatic assays.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for TFMU-ADPr diammonium are not applicable, as it is not a therapeutic drug but rather an in vitro biochemical reagent. The diammonium salt form (MW 805.5) ensures good water solubility, making it suitable for high-throughput screening and detailed enzymatic studies. The compound should be stored at -80degC, protected from light.
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| Toxicity/Toxicokinetics |
Toxicity data for TFMU-ADPr diammonium are not available, as it is a research reagent for in vitro use only. It is not intended for human or animal consumption. Standard safety precautions for handling laboratory chemicals should be observed. The product is for non-human research only and not for therapeutic or veterinary use.
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| References |
[1]. Drown BS, et al. Monitoring Poly(ADP-ribosyl)glycohydrolase Activity with a Continuous Fluorescent Substrate. Cell Chem Biol. 2018 Dec 20;25(12):1562-1570.e19.
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| Additional Infomation |
TFMU-ADPr diammonium is a fluorescent substrate used in research for studying PARG and ADP-ribose metabolism. It has not entered clinical trials and is not approved for therapeutic use. The compound is a tool for drug discovery and for investigating the role of PARG in DNA damage repair, cancer, and neurodegenerative diseases. For research use only.
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| Molecular Formula |
C25H32F3N7O16P2
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|---|---|
| Related CAS # |
TFMU-ADPr;2412923-11-4;TFMU-ADPr triethylamine
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| Appearance |
White to off-white solid powder
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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 (e.g. under nitrogen), 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) |
H2O :~125 mg/mL (~155.18 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.) |
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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