1. GPCR/G Protein
    Immunology/Inflammation
    Anti-infection
  2. CXCR
    HIV
  3. TC14012 TFA

TC14012 TFA 

Cat. No.: HY-P1102A
Handling Instructions

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 an EC50 of 350 nM for recruiting β-arrestin 2 to CXCR7. TC14012 TFA has anti-HIV activity and anti-cancer activity.

For research use only. We do not sell to patients.

Custom Peptide Synthesis

TC14012 TFA Chemical Structure

TC14012 TFA Chemical Structure

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Description

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 an EC50 of 350 nM for recruiting β-arrestin 2 to CXCR7. TC14012 TFA has anti-HIV activity and anti-cancer activity[1][2].

IC50 & Target[1][2]

CXCR4

19.3 nM (IC50, antagonist site)

CXCR7

350 nM (EC50, agonist site)

HIV

 

In Vitro

TC14012 TFA (1 mM) inhibits by 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 at 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 in U373 cells. Upon stimulation with TC14012 TFA, CXCR7 and the CXCR7-Cter4 chimera are able to recruit arrestin, whereas CXCR4 and CXCR4-Cter7 remain silent[2].

Molecular Weight

2180.44

Formula

C₉₂H₁₄₁F₃N₃₄O₂₁S₂

Sequence

Arg-Arg-{2Nal}-Cys-Tyr-{Cit}-Lys-{Cit}-Pro-Tyr-Arg-{Cit}-Cys-Arg-NH2 (Disulfide bridge:Cys4-Cys13)

Sequence Shortening

RR-{2Nal}-CY-{Cit}-K-{Cit}-PYR-{Cit}-CR-NH2 (Disulfide bridge:Cys4-Cys13)

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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.
References
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  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

TC14012TC 14012TC-14012CXCRHIVCXC chemokine receptorsC-X-C motif chemokine receptorsHuman immunodeficiency viruserk1/2phosphorylationβ-arrestin2Inhibitorinhibitorinhibit

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TC14012 TFA
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