| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
PP2A (protein phosphatase 2A). TRC-766 binds to PP2A but lacks phosphatase activation capabilities. It is a negative control for RTC-5 (TRC-382), a PP2A activator, and is used to distinguish between specific PP2A binding and functional activation.
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| ln Vitro |
TRC-766, a structurally identical but physiologically inert drug that is similar to PP2A (SMAP), is administered to the cells in escalating concentrations as a pharmacologic control. A crucial donor of hydrogen bonds for NH sulfonamide is absent in TRC-766. Though TRC-766 continues to bind PP2A, it does not activate the phosphatase, which is why it was hypothesized not to have an impact on cell viability[1].
TRC-766 binds to protein phosphatase 2A (PP2A) but does not activate the phosphatase. It is chemically similar to PP2A-activating small molecules (SMAPs) like RTC-5 (TRC-382), but lacks an N-H sulfonamide hydrogen bond donor that is essential for activation. Therefore, it serves as a perfect negative control to rule out non-specific effects in PP2A activation assays. |
| ln Vivo |
TRC-766 is not used as a therapeutic agent but as a research tool to control for PP2A binding in cellular and biochemical assays. It has no intrinsic in vivo activity as a PP2A activator. It is used in animal studies to demonstrate that the effects of PP2A activators (e.g., RTC-5) are due to specific PP2A activation rather than non-specific binding.
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| Enzyme Assay |
For non-cellular assays, purified PP2A enzyme is incubated with TRC-766 in assay buffer (e.g., 50 mM Tris-HCl, pH 7.0, 0.1 mM EGTA, 0.1% beta-mercaptoethanol). Binding is assessed by surface plasmon resonance (SPR), isothermal titration calorimetry (ITC), or pull-down assays. Phosphatase activity is measured using a fluorogenic substrate (e.g., DiFMUP) in the presence of TRC-766; no activation should be observed, confirming its role as a negative control.
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| Cell Assay |
For cell-based assays, cells are treated with increasing doses of TRC-766 (1-50 uM) alongside the PP2A activator RTC-5 (TRC-382). PP2A activity in cell lysates is measured using a fluorogenic substrate or by assessing dephosphorylation of PP2A substrates (e.g., phospho-AKT, phospho-c-Myc). TRC-766 should not increase PP2A activity or substrate dephosphorylation, serving as a control for specificity.
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| Animal Protocol |
For animal studies, TRC-766 is administered intraperitoneally or orally to mice at doses comparable to those used for RTC-5 (e.g., 10-50 mg/kg). Tissues (e.g., liver, brain, tumor) are collected, and PP2A activity is measured in lysates. TRC-766 should not alter PP2A activity or downstream signaling, confirming that any effects of RTC-5 are due to specific PP2A activation rather than non-specific binding.
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| ADME/Pharmacokinetics |
TRC-766 is typically dissolved in DMSO for in vitro use. For in vivo administration, it can be formulated in vehicles such as 10% DMSO, 40% PEG300, 5% Tween-80, and 45% saline. The compound has a molecular weight of 524.98 and a molecular formula of C25H24ClF3N2O3S. Detailed pharmacokinetic parameters are not extensively reported.
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| Toxicity/Toxicokinetics |
Toxicological data for TRC-766 are limited to research studies. As a negative control compound, it is generally well tolerated at research doses. No significant systemic toxicity has been reported in animal studies. Standard safety precautions for handling research chemicals should be followed. It is not intended for human use.
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| References | |
| Additional Infomation |
TRC-766 (CAS: 1810734-44-1) is a negative control for RTC-5 (TRC-382), a small-molecule activator of protein phosphatase 2A (PP2A). It binds to PP2A but does not activate the phosphatase, making it an essential tool for validating PP2A activation studies. TRC-766 is not an approved drug and is intended for research applications only.
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| Molecular Formula |
C25H24CLF3N2O3S
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|---|---|
| Molecular Weight |
524.9829
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| Exact Mass |
524.114
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| CAS # |
1810734-44-1
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| PubChem CID |
122188560
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| Appearance |
White to off-white solid powder
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| LogP |
7.2
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
35
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| Complexity |
786
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1C([H])=C([H])C2C([H])([H])C([H])([H])C3=C([H])C([H])=C([H])C([H])=C3N(C=2C=1[H])C([H])([H])C([H])([H])C([H])([H])N(C([H])([H])[H])S(C1C([H])=C([H])C(=C([H])C=1[H])OC(F)(F)F)(=O)=O
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| InChi Key |
HXSYJRNSDWIKPO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H24ClF3N2O3S/c1-30(35(32,33)22-13-11-21(12-14-22)34-25(27,28)29)15-4-16-31-23-6-3-2-5-18(23)7-8-19-9-10-20(26)17-24(19)31/h2-3,5-6,9-14,17H,4,7-8,15-16H2,1H3
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| Chemical Name |
N-[3-(2-chloro-5,6-dihydrobenzo[b][1]benzazepin-11-yl)propyl]-N-methyl-4-(trifluoromethoxy)benzenesulfonamide
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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) |
DMSO: 150 mg/mL (285.73 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 | 1.9048 mL | 9.5242 mL | 19.0483 mL | |
| 5 mM | 0.3810 mL | 1.9048 mL | 3.8097 mL | |
| 10 mM | 0.1905 mL | 0.9524 mL | 1.9048 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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