CTAP

Pricing Availability Delivery Time Qty
Cat.No. 1560 - CTAP | D-Phe-Cys-Tyr-D-Trp-Arg-Thr-Pen-Thr-NH2 (Disulfide bridge: 2 - 7) | CAS No. 103429-32-9
Description: Selective and potent μ antagonist
Datasheet
Citations (5)
Literature

Biological Activity

Potent and selective μ opioid receptor antagonist (IC50 = 3.5 nM). Displays > 1200-fold selectivity over δ opioid and somatostatin receptors. Brain penetrant and active in vivo.

Technical Data

M. Wt 1104.32
Formula C51H69N13O11S2
Sequence FCYWRTXT

(Modifications: Phe-1 = D-Phe, Trp-4 = D-Trp, X = Pen, Disulfide bridge between 2 - 7, Thr-8 = C-terminal amide)

Storage Desiccate at -20°C
CAS Number 103429-32-9
PubChem ID 90479802
InChI Key OFMQLVRLOGHAJI-KOFBULAQSA-N
Smiles [H]N[C@H](CC1=CC=CC=C1)C(=O)N[C@H]1CSSC(C)(C)C(NC(=O)[C@@H](NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H](CC2=CNC3=C2C=CC=C3)NC(=O)[C@H](CC2=CC=C(O)C=C2)NC1=O)[C@@H](C)O)C(=O)N[C@@H]([C@@H](C)O)C(N)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

SolubilitySoluble to 1 mg/ml in water

Preparing Stock Solutions

The following data is based on the product molecular weight 1104.32. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 0.91 mL 4.53 mL 9.06 mL
5 mM 0.18 mL 0.91 mL 1.81 mL
10 mM 0.09 mL 0.45 mL 0.91 mL
50 mM 0.02 mL 0.09 mL 0.18 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

Abbruscato et al (1997) Blood-brain barrier permeability and bioavailability of a highly potent and μ-selective opioid receptor antagonist, CTAP: comparison with morphine. J.Pharmacol.Exp.Ther. 280 402 PMID: 8996221

Kramer et al (1989) Novel peptidic mu opioid antagonists: pharmacologic characterization in vitro and in vivo. J.Pharmacol.Exp.Ther. 249 544 PMID: 2566679

Pelton et al (1986) Design and synthesis of conformationally constrained somatostatin analogues with high potency and specificity for μ opioid receptors. J.Med.Chem. 29 2370 PMID: 2878079


If you know of a relevant reference for CTAP, please let us know.

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Keywords: CTAP, supplier, Selective, potent, μ-opioid, mu-opioid, antagonists, MOP, Receptors, OP3, Mu, Opioid, Receptors, Mu, Opioid, Receptors, Tocris Bioscience

5 Citations for CTAP

Citations are publications that use Tocris products. Selected citations for CTAP include:

Gerhold et al (2015) Pronociceptive and Antinociceptive Effects of Buprenorphine in the Spinal Cord Dorsal Horn Cover a Dose Range of Four Orders of Magnitude. J Neurosci 35 9580 PMID: 26134641

Song et al (2011) Protein kinase Czeta mediates micro-opioid receptor-induced cross-desensitization of chemokine receptor CCR5. J Biol Chem 286 20354 PMID: 21454526

Krook-Magnuson et al (2011) Ivy and neurogliaform interneurons are a major target of μ-opioid receptor modulation. J Neurosci 31 14861 PMID: 22016519

Sengupta et al (2009) Morphine increases brain levels of ferritin heavy chain leading to inhibition of CXCR4-mediated survival signaling in neurons. J Leukoc Biol 29 2534 PMID: 19244528

Happel et al (2008) DAMGO-induced expression of chemokines and chemokine receptors: the role of TGF-β1. Front Cell Neurosci 83 956 PMID: 18252865


Do you know of a great paper that uses CTAP from Tocris? If so please let us know.

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Reviews

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Pathways for CTAP

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