1. GPCR/G Protein Neuronal Signaling
  2. Opioid Receptor
  3. CTAP TFA

CTAP TFA is a potent, highly selective, and BBB penetrant μ opioid receptor antagonist, with an IC50 of 3.5 nM. CTAP TFA displays over 1200-fold selectivity over δ opioid (IC50=4500 nM) and somatostatin receptors. CTAP TFA can be used for the study of L-DOPA-induced dyskinesia (LID) and opiate overdose or addiction.

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

Custom Peptide Synthesis

CTAP TFA

CTAP TFA Chemical Structure

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Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

CTAP TFA is a potent, highly selective, and BBB penetrant μ opioid receptor antagonist, with an IC50 of 3.5 nM. CTAP TFA displays over 1200-fold selectivity over δ opioid (IC50=4500 nM) and somatostatin receptors. CTAP TFA can be used for the study of L-DOPA-induced dyskinesia (LID) and opiate overdose or addiction[1][2].

IC50 & Target

μ Opioid Receptor/MOR

3.5 nM (IC50)

δ Opioid Receptor/DOR

4500 nM (IC50)

In Vivo

CTAP TFA (0-1 mg/kg, IP, single) blocks morphine’s antinociceptive effect[1].
CTAP TFA (10 mg/kg; IP, single) has no effect on L-DOPA-induced limb, axial, orolingual, or locomotor abnormal involuntary movements[1].
CTAP TFA is stable in the blood and serum of rats (T1/2 > 500 min), showing that the structure of this peptide offers enzymatic resistance[2].
CTAP TFA is extensively protein-bound to albumin in the perfusion medium (68.2%) and to proteins in rat serum (84.2%)[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Sprague-Dawley rats[1]
Dosage: 0, 0.1, 0.5, 1 mg/kg
Administration: IP, single
Result: Completely blocked morphine’s antinociceptive effect at 0.5 or 1 mg/kg.
Molecular Weight

1104.30 (free base)

Formula

C51H69N13O11S2.xC2HF3O2

Appearance

Solid

Color

White to off-white

Sequence

{d-Phe}-Cys-Tyr-{d-Trp}-Arg-Thr-{Pen}-Thr-NH2 (Disulfide bridge:Cys2-Pen7)

Sequence Shortening

{d-Phe}-CY-{d-Trp}-RT-{Pen}-T-NH2 (Disulfide bridge:Cys2-Pen7)

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Sealed storage, away from moisture and light, under nitrogen

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)

Solvent & Solubility
In Vitro: 

H2O : 100 mg/mL (Need ultrasonic)

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 99.60%

References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
CTAP TFA
Cat. No.:
HY-P1335A
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