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Submit ReviewC 021 dihydrochloride
Description: Potent CCR4 antagonist
Chemical Name: 2-[1,4'-Bipiperidin]-1'-yl-N-cycloheptyl-6,7-dimethoxy-4-quinazolinamine dihydrochloride
Purity: ≥99% (HPLC)
Biological Activity for C 021 dihydrochloride
C 021 dihydrochloride is a potent CCR4 chemokine receptor antagonist (IC50 values are 0.14 and 0.039 μM for inhibition of chemotaxis in human and mouse respectively).
Compound Libraries for C 021 dihydrochloride
C 021 dihydrochloride is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.
Technical Data for C 021 dihydrochloride
| M. Wt | 540.57 |
| Formula | C27H41N5O2.2HCl |
| Storage | Desiccate at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 1784252-84-1 |
| PubChem ID | 56972238 |
| InChI Key | GKJKNYQUFAPLOQ-UHFFFAOYSA-N |
| Smiles | COC1=C(OC)C=C(N=C(N4CCC(N5CCCCC5)CC4)N=C2NC3CCCCCC3)C2=C1.Cl.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for C 021 dihydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 26.96 | 50 | |
| DMSO | 53.93 | 100 |
Preparing Stock Solutions for C 021 dihydrochloride
The following data is based on the product molecular weight 540.57. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.85 mL | 9.25 mL | 18.5 mL |
| 5 mM | 0.37 mL | 1.85 mL | 3.7 mL |
| 10 mM | 0.18 mL | 0.92 mL | 1.85 mL |
| 50 mM | 0.04 mL | 0.18 mL | 0.37 mL |
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Product Datasheets for C 021 dihydrochloride
References for C 021 dihydrochloride
References are publications that support the biological activity of the product.
Yokoyama et al (2009) Potent and orally bioavailable CCR4 antagonists: synthesis and structure-activity relationship study of 2-aminoquinazolines. Bioorg.Med.Chem. 17 64 PMID: 19081254
If you know of a relevant reference for C 021 dihydrochloride, please let us know.
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Keywords: C 021 dihydrochloride, C 021 dihydrochloride supplier, C021, dihydrochloride, potent, CCR4, chemokines, receptors, antagonists, Chemokine, CC, Receptors, 3581, Tocris Bioscience
7 Citations for C 021 dihydrochloride
Citations are publications that use Tocris products. Selected citations for C 021 dihydrochloride include:
Rasheed et al (2018) CCL17/TARC and CCR4 expression in Merkel cell carcinoma. Oncotarget 9 31432 PMID: 30140381
Kwon et al (2015) CCL2 Mediates Neuron-Macrophage Interactions to Drive Proregenerative Macrophage Activation Following Preconditioning Injury. J Neurosci 35 15934 PMID: 26631474
McMillin et al (2014) Neuronal CCL2 is upregulated during hepatic encephalopathy and contributes to microglia activation and neurological decline. J Neuroinflammation 11 121 PMID: 25012628
Lei et al (2021) Recombinant CCL17-dependent CCR4 activation alleviates neuroinflammation and neuronal apoptosis through the PI3K/AKT/Foxo1 signaling pathway after ICH in mice. J Neuroinflammation 18 62 PMID: 33648537
Palchevskiy et al (2019) CCR4 expression on host T cells is a driver for alloreactive responses and lung rejection. JCI Insight 5 PMID: 31085832
Lei et al (2020) Recombinant CCL17 Enhances Hematoma Resolution and Activation of CCR4/ERK/Nrf2/CD163 Signaling Pathway After Intracerebral Hemorrhage in Mice. Neurotherapeutics 17 1940-1953 PMID: 32783091
He et al (2018) Circadian Expression of Migratory Factors Establishes Lineage-Specific Signatures that Guide the Homing of Leukocyte Subsets to Tissues. Immunity 49 1175 PMID: 30527911
Do you know of a great paper that uses C 021 dihydrochloride from Tocris? Please let us know.
Reviews for C 021 dihydrochloride
Average Rating: 1 (Based on 1 Review.)
Have you used C 021 dihydrochloride?
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Unfortunately I found no effect..
By
Anonymous on 12/12/2017
Species: Human
I used it both in vivo and in vitro. In vitro, I was unable to find any impact in chemotaxis towards CCL17
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