Date published: 2025-12-6

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RS 102895 Hydrochloride (CAS 300815-41-2)

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Alternate Names:
1′-[2-[4-(Trifluoromethyl)phenyl]ethyl]-spiro[4H-3,1-benzoxazine-4,4′-peperidin]-2(1H)-one
Application:
RS 102895 Hydrochloride is a CCR2-selective chemokine receptor antagonist
CAS Number:
300815-41-2
Purity:
>99%
Molecular Weight:
426.86
Molecular Formula:
C21H21F3N2O2•HCl
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
Available in US only.
* Refer to Certificate of Analysis for lot specific data.

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RS 102895 Hydrochloride is a CKR-2B (CCR2)-selective chemokine receptor antagonist (IC50 values are 0.36 and 17.8 muM for inhibition of human recombinant CKR-2B and CKR-1 (CCR2b and CCR1 receptors) respectively). Blocks MCP-1-stimulated calcium influx and chemotaxis with IC50 values of 32 nM and 1.7 muM respectively. Inhibits alpha1A-AR, alpha1D-AR and SR-1A (alpha1A, alpha1D and 5-HT1A receptors).


RS 102895 Hydrochloride (CAS 300815-41-2) References

  1. Identification of the binding site for a novel class of CCR2b chemokine receptor antagonists: binding to a common chemokine receptor motif within the helical bundle.  |  Mirzadegan, T., et al. 2000. J Biol Chem. 275: 25562-71. PMID: 10770925
  2. In vivo MR evaluation of the effect of the CCR2 antagonist on macrophage migration.  |  Lee, Y., et al. 2010. Magn Reson Med. 64: 72-9. PMID: 20572147
  3. Role of human pulmonary fibroblast-derived MCP-1 in cell activation and migration in experimental silicosis.  |  Liu, X., et al. 2015. Toxicol Appl Pharmacol. 288: 152-60. PMID: 26163174
  4. HBD-3 induces NK cell activation, IFN-γ secretion and mDC dependent cytolytic function.  |  Judge, CJ., et al. 2015. Cell Immunol. 297: 61-8. PMID: 26302933
  5. Angiotensin II-C-C chemokine receptor2/5 axis-dependent monocyte/macrophage recruitment contributes to progression of experimental autoimmune myocarditis.  |  Lu, H., et al. 2017. Microbiol Immunol. 61: 539-546. PMID: 29052263
  6. A novel interaction between CX3CR1 and CCR2 signalling in monocytes constitutes an underlying mechanism for persistent vincristine-induced pain.  |  Montague, K., et al. 2018. J Neuroinflammation. 15: 101. PMID: 29625610
  7. NF-KappaB Pathway Is Involved in Bone Marrow Stromal Cell-Produced Pain Relief.  |  Guo, W., et al. 2018. Front Integr Neurosci. 12: 49. PMID: 30459569
  8. Inflammation potentiates miR-939 expression and packaging into small extracellular vesicles.  |  Ramanathan, S., et al. 2019. J Extracell Vesicles. 8: 1650595. PMID: 31489147
  9. MCP-1/CCR-2 axis in adipocytes and cancer cell respectively facilitates ovarian cancer peritoneal metastasis.  |  Sun, C., et al. 2020. Oncogene. 39: 1681-1695. PMID: 31705064
  10. High-salt diet decreases mechanical thresholds in mice that is mediated by a CCR2-dependent mechanism.  |  Fan, A., et al. 2020. J Neuroinflammation. 17: 179. PMID: 32517772
  11. Cancer cell CCR2 orchestrates suppression of the adaptive immune response.  |  Fein, MR., et al. 2020. J Exp Med. 217: PMID: 32667673
  12. Resident stroma-secreted chemokine CCL2 governs myeloid-derived suppressor cells in the tumor microenvironment.  |  Oo, MW., et al. 2022. JCI Insight. 7: PMID: 34874922
  13. Synthesis and antihypertensive activity of 4'-substituted spiro[4H-3,1-benzoxazine-4,4'-piperidin]-2(1H)-ones.  |  Clark, RD., et al. 1983. J Med Chem. 26: 657-61. PMID: 6842505

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

RS 102895 Hydrochloride, 10 mg

sc-204243
10 mg
$125.00
US: Only available in the US

RS 102895 Hydrochloride, 50 mg

sc-204243A
50 mg
$495.00
US: Only available in the US

After dissolving in DMSO, at what temperature should this product be stored?

Asked by: SCM4
We should recommend that solutions be used the same day they are made. If a solution must be stored in DMSO, we recommend aliquotting into useable amounts and freezing the solution for up to 1 month. Repeated freeze/thaw cycles are not recommended.
Answered by: Tech Service 11
Date published: 2017-03-17
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Rated 5 out of 5 by from LiuLiu, et al. (PubMed ID 26163174) found that when pre-treating cultured adult human pulmonary fibroblasts (HPF-a) with RS 102895, a CCR2 inhibitor, the SiO2 induced increase in cell activation and migration (in both 2D and 3D culture systems) was virtually abolished. -SCBT Publication Review
Date published: 2015-03-02
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RS 102895 Hydrochloride is rated 5.0 out of 5 by 1.
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