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100mg | ||
250mg | ||
500mg |
ln Vitro |
More than 95% of the HXB2 (X4) or 89.6 (ambitropic) strains cannot infect CXCR4-expressing cells when TC14012 (1 mM) is present. In contrast, TC14012 (1 mM) cannot prevent the infection of SF162 (R5) or 89.6 (ambitropic) CCR5-expressing cells. Upon infection with TC14012, U373 cells—which express endogenous CXCR7 but not CXCR4—phosphorylate erk 1/2. CXCR7 and CXCR7-Cter4 chimeras can recruit inhibitory proteins following TC14012 stimulation, while CXCR4 and CXCR4-Cter7 cannot [2].
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References |
[1]. H Tamamura, et al. Development of specific CXCR4 inhibitors possessing high selectivity indexes as well as complete stability in serum based on an anti-HIV peptide T140. Bioorg Med Chem Lett. 2001 Jul 23;11(14):1897-902.
[2]. Stéphanie Gravel, et al. The peptidomimetic CXCR4 antagonist TC14012 recruits beta-arrestin to CXCR7: roles of receptor domains. J Biol Chem. 2010 Dec 3;285(49):37939-43. |
Molecular Formula |
C90H140N34O19S2
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Molecular Weight |
2066.421
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CAS # |
368874-34-4
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Related CAS # |
TC14012 TFA
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SMILES |
N=C(N)NCCC[C@@H](C(N)=O)NC([C@H]1NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H]2CCCN2C([C@H](NC([C@@H](NC([C@@H](NC([C@@H](NC(=O)[C@H](CSSC1)NC([C@@H](NC([C@@H](NC([C@@H](N)CCCNC(N)=N)=O)CCCNC(N)=N)=O)CC3=CC4=CC=CC=C4C=C3)=O)CC5=CC=C(O)C=C5)=O)CCCNC(N)=O)=O)CCCCN)=O)CCCNC(N)=O)=O)=O)CC6=CC=C(O)C=C6)=O)CCCNC(N)=N)=O)CCCNC(N)=O)=O)=O
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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, 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) |
DMSO : ~25 mg/mL (~12.10 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.67 mg/mL (0.81 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.67 mg/mL (0.81 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1.67 mg/mL (0.81 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 0.4839 mL | 2.4196 mL | 4.8393 mL | |
5 mM | 0.0968 mL | 0.4839 mL | 0.9679 mL | |
10 mM | 0.0484 mL | 0.2420 mL | 0.4839 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.