TC14012 TFA
Based on 4 publication(s) in Google Scholar
TC14012 TFA, a serum-stable derivative of T140, is a selective and peptidomimetic CXCR4 antagonist with an IC50 of 19.3 nM. TC14012 TFA is a potent CXCR7 agonist with an EC50 of 350 nM for recruiting β-arrestin 2 to CXCR7. TC14012 TFA has anti-HIV activity and anti-cancer activity.
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- Formule: C92H141F3N34O21S2
- Masse moléculaire:2180.44
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) TC14012 TFA
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Activité biologique
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CXCR4 19.3 nM (IC50, antagonist site) |
CXCR7 350 nM (EC50, agonist site) |
HIV |
TC14012 TFA (1 mM) inhibits more than 95% the infection of the CXCR4-expressing cells by the HXB2 (X4) or 89.6 (dual-tropic) strain whereas TC14012 TFA (1 mM) does not inhibit all the infection of the CCR5-expressing cells by the SF162 (R5) or 89.6 (dualtropic) strain[1].
TC14012 TFA leads to erk 1/2 phosphorylation in U373 cells, which express endogenous CXCR7 but not CXCR4. Upon stimulation with TC14012 TFA, CXCR7 and the CXCR7-Cter4 chimera are able to recruit arrestin, whereas CXCR4 and CXCR4-Cter7 remain silent[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Masse moléculaire 2180.44
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Formule C92H141F3N34O21S2
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Sequence Shortening
RR-{2Nal}-CY-{Cit}-K-{Cit}-PYR-{Cit}-CR-NH2 (Disulfide bridge:Cys4-Cys13)
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (4)
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Journal Impact Factor
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Most Recent
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Biochem Pharmacol
Targeting the CXCR7 pathway with TC14012 to inhibit endothelial necroptosis and lung cancer metastasis. [Abstract]2025 Jun:236:116852. PMID: 40049294 -
Cell Mol Life Sci
Crosstalk between purinergic receptor P2Y11 and chemokine receptor CXCR7 is regulated by CXCR4 in human macrophages. [Abstract]2024 Mar 13;81(1):132. PMID: 38472446 -
Biochem Biophys Res Commun
2023 Jul 5:664:59-68. PMID: 37141639 -
Solvant et solubilité
H2O
Peptide Solubility and Storage Guidelines:
1. Calculate the length of the peptide.
2. Calculate the overall charge of the entire peptide according to the following table:
| Contents | Assign value | |
| Acidic amino acid | Asp (D), Glu (E), and the C-terminal -COOH. | -1 |
| Basic amino acid | Arg (R), Lys (K), His (H), and the N-terminal -NH2 | +1 |
| Neutral amino acid | Gly (G), Ala (A), Leu (L), Ile (I), Val (V), Cys (C), Met (M), Thr (T), Ser (S), Phe (F), Tyr (Y), Trp (W), Pro (P), Asn (N), Gln (Q) | 0 |
3. Recommended solution:
| Overall charge of peptide | Details |
| Negative (<0) |
1. Try to dissolve the peptide in water first. 2. If water fails, add NH4OH (<50 μL). 3. If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide. |
| Positive (>0) |
1. Try to dissolve the peptide in water first. 2. If water fails, try dissolving the peptide in a 10%-30% acetic acid solution. 3. If the peptide still does not dissolve, try dissolving the peptide in a small amount of DMSO. |
| Zero (=0) |
1. Try to dissolve the peptide in organic solvent (acetonitrile, methanol, etc.) first. 2. For very hydrophobic peptides, try dissolving the peptide in a small amount of DMSO, and then dilute the solution with water to the desired concentration. |
Pureté et documentation
Références
[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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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