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CCR4 Antagonist (CAS 864289-85-0)

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Alternate Names:
2-(1,4′-Bipiperidin)-1′-yl-N-cycloheptyl-6,7-dimethoxy-4-quinazolinamine; C-021
Application:
CCR4 Antagonist is a diaminoquinazoline compound and potent antagonist of CCR4
CAS Number:
864289-85-0
Purity:
≥97%
Molecular Weight:
467.66
Molecular Formula:
C27H41N5O2
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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CCR4 Antagonist is a cell-permeable diaminoquinazoline compound that acts as a potent antagonist against the G-protein-coupled chemokine receptor CKR-4 (CCR4). CCR4 Antagonist is shown to inhibit CCL22/CCR4-mediated chemotaxis in both murine and human cultures. The CCR4 receptor primarily binds to certain chemokines, particularly CCL17 (TARC) and CCL22 (MDC). These chemokines are involved in the directed migration (chemotaxis) of specific immune cells, notably T-helper type 2 (Th2) lymphocytes. Th2 cells are implicated in allergic responses and certain other immune responses. CCR4 can be overexpressed on certain cancer cells, particularly some types of T-cell leukemia and lymphoma. Blocking CCR4 might impair the migration and survival of these cancer cells.


CCR4 Antagonist (CAS 864289-85-0) References

  1. Discovery of potent CCR4 antagonists: Synthesis and structure-activity relationship study of 2,4-diaminoquinazolines.  |  Yokoyama, K., et al. 2008. Bioorg Med Chem. 16: 7021-32. PMID: 18539035
  2. Palladin mediates stiffness-induced fibroblast activation in the tumor microenvironment.  |  McLane, JS. and Ligon, LA. 2015. Biophys J. 109: 249-64. PMID: 26200861
  3. Melatonin Modulates the Microenvironment of Glioblastoma Multiforme by Targeting Sirtuin 1.  |  Lai, SW., et al. 2019. Nutrients. 11: PMID: 31207928
  4. Cross-talk between iNKT cells and CD8 T cells in the spleen requires the IL-4/CCL17 axis for the generation of short-lived effector cells.  |  Valente, M., et al. 2019. Proc Natl Acad Sci U S A. 116: 25816-25827. PMID: 31796596
  5. CCL22 signaling contributes to sorafenib resistance in hepatitis B virus-associated hepatocellular carcinoma.  |  Gao, Y., et al. 2020. Pharmacol Res. 157: 104800. PMID: 32278046
  6. CCR4 antagonist (C021) influences the level of nociceptive factors and enhances the analgesic potency of morphine in a rat model of neuropathic pain.  |  Bogacka, J., et al. 2020. Eur J Pharmacol. 880: 173166. PMID: 32407723
  7. Blockade of CCR4 Diminishes Hypersensitivity and Enhances Opioid Analgesia - Evidence from a Mouse Model of Diabetic Neuropathy.  |  Bogacka, J., et al. 2020. Neuroscience. 441: 77-92. PMID: 32592824
  8. CCR4 Antagonist (C021) Administration Diminishes Hypersensitivity and Enhances the Analgesic Potency of Morphine and Buprenorphine in a Mouse Model of Neuropathic Pain.  |  Bogacka, J., et al. 2020. Front Immunol. 11: 1241. PMID: 32760393
  9. Recombinant CCL17 Enhances Hematoma Resolution and Activation of CCR4/ERK/Nrf2/CD163 Signaling Pathway After Intracerebral Hemorrhage in Mice.  |  Deng, S., et al. 2020. Neurotherapeutics. 17: 1940-1953. PMID: 32783091
  10. Recombinant CCL17-dependent CCR4 activation alleviates neuroinflammation and neuronal apoptosis through the PI3K/AKT/Foxo1 signaling pathway after ICH in mice.  |  Deng, S., et al. 2021. J Neuroinflammation. 18: 62. PMID: 33648537
  11. Chemokine receptor antagonists with α1-adrenergic receptor blocker activity.  |  DeSantis, AJ., et al. 2021. J Basic Clin Physiol Pharmacol. 33: 519-523. PMID: 34144642
  12. Skin-resident dendritic cells mediate postoperative pain via CCR4 on sensory neurons.  |  Silva, JR., et al. 2022. Proc Natl Acad Sci U S A. 119: PMID: 35046040
  13. CCL17 drives fibroblast activation in the progression of pulmonary fibrosis by enhancing the TGF-β/Smad signaling.  |  Wang, QR., et al. 2023. Biochem Pharmacol. 210: 115475. PMID: 36870575

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

CCR4 Antagonist, 1 mg

sc-221406A
1 mg
$82.00

CCR4 Antagonist, 5 mg

sc-221406
5 mg
$112.00

CCR4 Antagonist, 10 mg

sc-221406B
10 mg
$139.00

Where can I order this product in Netherlands?

Asked by: ydolen
Thank you for your question. You can order online by visiting scbt.com or sending an email to europe@scbt.com. Please contact customer care if you have any questions or if you reqire information on availability or a quotation.
Answered by: SCBT Heidelberg Support
Date published: 2019-01-06

使用该拮抗剂抑制CCR4后,如何观察抑制效果?

Asked by: L Y F
感谢您的提问。关于此问题的详细细节,欢迎通过:电话(+86) 021-60936350、邮箱asia@scbio.cn、或选择网页上Live Chat中的“中文支持”,联系我们的技术支持部门。 Thank you for your inquiry. For more detailed information about this question, please contact our Asian Technical Service team at (+86) 021-60936350 or asia@scbio.cn or by live chat on our website.
Answered by: Technical Support 15
Date published: 2017-12-03
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Rated 5 out of 5 by from McMillinMcMillin, M. et al. (PubMed 25012628) induced hepatic encephalopathy in mice via injection of azoxymethane (AOM) in the presence or absence of INCB 3284, a CCR2 inhibitor, or CCR4 Antagonist (C021). Mice were monitored for neurological decline and time to coma was recorded. They found that administration of INCB 3284 or C021 significantly improved the neurological outcomes of AOM-treated mice, reduced microglia activation, reduced phosphorylation of ERK1/2, and alleviated AOM-induced cytokine upregulation. -SCBT Publication Review
Date published: 2015-02-11
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CCR4 Antagonist is rated 5.0 out of 5 by 1.
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