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TC14012 TFA
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
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

 

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].

分子量

2180.44

Formula

C92H141F3N34O21S2

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:

 ContentsAssign value
Acidic amino acidAsp (D), Glu (E), and the C-terminal -COOH.-1
Basic amino acidArg (R), Lys (K), His (H), and the N-terminal -NH2+1
Neutral amino acidGly (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 peptideDetails
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.