2. GPCR/G Protein Immunology/Inflammation
  3. CXCR
  4. YU241279

YU241279 是一种口服有效的 CXCR5 抑制剂。YU241279 可抑制表达 CXCR5 的细胞中由 CXCL13 介导的 Gαq 依赖性钙内流，以及 Gαi2 依赖性 cAMP 降低。YU241279 可抑制表达 CXCR5 的淋巴瘤细胞增殖。YU241279 可降低植入淋巴瘤组织的小鼠外周血和骨髓中的肿瘤负荷。YU241279 在小鼠口服给药期间具有耐受性，能维持稳定的血药浓度且代谢无变化。YU241279 可用于血管免疫母细胞性 T 细胞淋巴瘤和伯基特 B 细胞淋巴瘤的研究。

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YU241279

YU241279 Chemical Structure

CAS No. : 1092445-63-0

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YU241279 相关抗体

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CXCR CXCR1 CXCR2 CXCR3 CXCR4 CXCR7 CXCR6

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

YU241279 is an orally active CXCR5 inhibitor. YU241279 inhibits CXCL13-mediated Gαq-dependent calcium influx and Gαi2-dependent cAMP reduction in CXCR5-expressing cells. YU241279 inhibits the proliferation of CXCR5-expressing lymphoma cells. YU241279 reduces tumor burden in the peripheral blood and bone marrow of mice implanted with lymphoma tissues. YU241279 is well tolerated during oral administration in mice, maintains stable plasma drug concentrations, and shows no metabolic changes. YU241279 can be used in the research of angioimmunoblastic T-cell lymphoma and Burkitt B-cell lymphoma[1].

体外研究
(In Vitro)

YU241279 (compound 2) 可强效抑制稳定表达人 CXCR5 的分裂阻滞 HEK-293 细胞中 Gaq 介导的 Ca2+内流，在 HBSS 缓冲液中的 IC50 值为 166.4 nM，在 HBSS 缓冲液+1% BSA 中的 IC50 值为 444.4 nM[1]。
YU241279 可强效抑制稳定表达人 CXCR5 的分裂阻滞 HEK-293 细胞中由 Gαi2 介导的 cAMP 降低，在 HBSS buffer 中的 IC50 值为 341.1 nM，在 HBSS buffer + 1% BSA 中的 IC50 值为 584.5 nM[1]。
YU241279 (1-30 μM; 7 d) 呈剂量依赖性抑制表达 CXCR5 的 Raji 伯基特 B 细胞淋巴瘤细胞的增殖，在低至 1 μM 的浓度下即可观察到显著的抑制作用[1]。

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

YU241279 相关抗体:

Cell Proliferation Assay[1]

Cell Line: CXCR5-expressing Raji Burkitt's B-cell lymphoma cells
Concentration: 1-30 μM
Incubation Time: 7 days
Result: Induced a dose-dependent decrease in Raji cell proliferation over 7 days.
Significantly reduced proliferation relative to DMSO control at 1 μM (p<0.01).
Significantly reduced proliferation relative to DMSO control at 3 μM, 10 μM, and 30 μM (p<0.005 for each).
体内研究
(In Vivo)

YU241279 (compound 2) (40 mg/kg；灌胃；每日 2 次；连续 42 天) 可在 NSG 小鼠中使 AITL 肿瘤负荷显著降低[1]。

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

Animal Model: NSG (NOD/SCID, IL-2R knockout; 8 animals per group)[1]
Dosage: 40 mg/kg
Administration: oral gavage; twice daily; 42 days
Result: Reduced absolute percentage of human CD45+ cells in bone marrow to 10.6%.
Reduced absolute percentage of human CD45+ cells in peripheral blood to 44.5%.
Maintained 5 surviving mice at study end.
分子量

351.44

Formula

C22H25NO3
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

YU241279 相关分类

  • 摩尔计算器

  • 稀释计算器

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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.

Keywords:

YU2412791092445-63-0YU 241279YU-241279CXCRCXC chemokine receptorsC-X-C motif chemokine receptorsangioimmunoblastic T cell lymphomaBurkitt's B-cell lymphomaCXCR5-expressing cellsGaqGai2miceHEK-293 cellslymphoma cellsCXCR5CXCL13Inhibitorinhibitorinhibit

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目录号：
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