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TC-T 6000

Katalog-Nr.GC50098

TC-T 6000 ist ein potenter und selektiver Inhibitor des menschlichen ENT4 (Equilibrative Nukleosidtransporter 4) mit einer IC50 von 74,4 nM.

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TC-T 6000 Chemische Struktur

Cas No.: 949467-71-4

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10 mg
215,00 $
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50 mg
792,00 $
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Sample solution is provided at 25 µL, 10mM.

Description of TC-T 6000

TC-T 6000, a Dipyridamole analog, is a potent and selective human ENT4 (Balanced nucleoside transporter 4) inhibitor with an IC50 of 74.4nM. Making it about 38 times more potent than Dipyridamole [1].

TC-T 6000(10μM; 24h) shows no cytotoxicity against PK15/hENT4 cells.

References:
[1]. Wang C, Lin W, et,al. Dipyridamole analogs as pharmacological inhibitors of equilibrative nucleoside transporters. Identification of novel potent and selective inhibitors of the adenosine transporter function of human equilibrative nucleoside transporter 4 (hENT4). Biochem Pharmacol. 2013 Dec 1;86(11):1531-40. doi: 10.1016/j.bcp.2013.08.063. Epub 2013 Sep 7. PMID: 24021350; PMCID: PMC3866046.

Protocol of TC-T 6000

Cell experiment [1]:

Cell lines

PK15/hENT cells (PK15 cells stably expressing hENT4)

Preparation Method

Cells were seeded at 5×103 cells were seeded in 96-well plates, treated with 10μM test TC-T 6000 and incubated at 37 ℃ in phenol-free MEM for 24h.

Reaction Conditions

10μM; 24h

Applications

TC-T 6000 shows no cytotoxicity against PK15/hENT4 cells.
Transporter inhibition assays [1]:

Preparation Method

Transport activity of cells transiently transfected with hENT4 was examined with [3H] Adenosine. K15/hENT4 cells were incubated with transport buffer containing TC-T 6000 at pH 6.0 for 15min before addition of 0.2μM [3H] Adenosine, and then further incubation for 2min. Uptake was terminated by rapidly aspirating the incubation mixture and washing cells three times with ice-cold PBS. The cells were solubilized overnight in 400μl of 5% Triton X-100 and 200μl of cell lysate was counted using a scintillation counter. Protein concentration in the cell lysate was determined using the BCA protein assay kit. The concentrations of test compounds that caused 50% inhibition of [3H] Adenosine uptake (IC50) were calculated using a nonlinear fitting method in the Prism 4 program.

Reaction Conditions

10μM; 15min

Applications

TC-T 6000 is a potent and selective human ENT4 (Balanced nucleoside transporter 4) inhibitor with an IC50 of 74.4nM.

References:
[1]. Wang C, Lin W, et,al. Dipyridamole analogs as pharmacological inhibitors of equilibrative nucleoside transporters. Identification of novel potent and selective inhibitors of the Adenosine transporter function of human equilibrative nucleoside transporter 4 (hENT4). Biochem Pharmacol. 2013 Dec 1;86(11):1531-40. doi: 10.1016/j.bcp.2013.08.063. Epub 2013 Sep 7. PMID: 24021350; PMCID: PMC3866046.

Chemical Properties of TC-T 6000

Cas No. 949467-71-4 SDF
Canonical SMILES CC(C)CN(CC(C)C)C2=NC(NCCO)=NC1=C(N(CC(C)C)CC(C)C)N=C(NCCO)N=C12
Formula C26H48N8O2 M.Wt 504.71
Löslichkeit Soluble in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of TC-T 6000

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 1.9813 mL 9.9067 mL 19.8134 mL
5 mM 0.3963 mL 1.9813 mL 3.9627 mL
10 mM 0.1981 mL 0.9907 mL 1.9813 mL
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In vivo Formulation Calculator (Clear solution) of TC-T 6000

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.

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