TC14012 TFA 是 T140 的血清稳定衍生物，是一种选择性的CXCR4拮抗剂，IC50为 19.3 nM。TC14012 TFA 是有效的CXCR7激动剂，可将 β-arrestin2 募集到 CXCR7，EC50为 350 nM。TC14012 TFA 具有抗HIV活性和抗癌活性。
| 生物活性 | TC14012 TFA, a serum-stable derivative of T140, is a selective and peptidomimeticCXCR4antagonist with anIC50of 19.3 nM. TC14012 TFA is a potentCXCR7agonist with anEC50of 350 nM for recruiting β-arrestin 2 toCXCR7. TC14012 TFA hasanti-HIVactivity and anti-cancer activity[1][2]. |
| IC50& Target[1][2] | CXCR4 19.3 nM (IC50, antagonist site) | CXCR7 350 nM (EC50, agonist site) | HIV |
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体外研究
(In Vitro) | 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].
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| 分子量 | |
| Formula | |
| Sequence Shortening | RR-{2Nal}-CY-{Cit}-K-{Cit}-PYR-{Cit}-CR-NH2 (Disulfide bridge:Cys4-Cys13) |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Solvent & Solubility | In Vitro: 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. |
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