2. GPCR/G Protein Immunology/Inflammation
  3. CXCR
  4. CXCR6 antagonist 1

CXCR6 antagonist 1 (Compound 81) 是一种具有口服活性的 CXCR6 拮抗剂。CXCR6 antagonist 1 可抑制 CXCR6 受体信号通路，包括 β-arrestin 募集和 Forskolin (HY-15371) 诱导的 cAMP 生成。CXCR6 antagonist 1 可降低肝细胞癌小鼠异种移植模型中的肿瘤生长。CXCR6 antagonist 1 可用于肝细胞癌的相关研究。

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CXCR6 antagonist 1

CXCR6 antagonist 1 Chemical Structure

CAS No. : 2579689-85-1

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CXCR6 antagonist 1 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CXCR6 antagonist 1 (Compound 81) is an orally active CXCR6 antagonist. CXCR6 antagonist 1 inhibits the CXCR6 receptor signaling pathway, including β-arrestin recruitment and Forskolin (HY-15371)-induced cAMP production. CXCR6 antagonist 1 reduces tumor growth in a mouse xenograft model of hepatocellular carcinoma. CXCR6 antagonist 1 can be used in research related to hepatocellular carcinoma[1].

IC50 & Target[1]

CXCR6

 

体外研究
(In Vitro)

CXCR6 antagonist 1 可强效抑制表达 CXCR6 的 DiscoveRx 细胞中 CXCL16 诱导的 β-arrestin 募集，其 IC50 为 40 nM[1]。
CXCR6 antagonist 1 可在表达 CXCR6 的 DiscoveRx 细胞中抑制 Forskolin (HY-15371) 诱导的 cAMP 信号通路，其 IC50 为 540 nM[1]。
CXCR6 antagonist 1 (72 h) 剂量依赖性抑制肝癌细胞 SK-HEP-1 的迁移，其 IC50 为 2.1 μM[1]。

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

CXCR6 antagonist 1 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route Cmax T1/2 AUC CL Vdss
Mice[1] 5 mg/kg i.v. / 1.58 h / 28.4 mL/min/kg 3.32 L/kg
Mice[1] 10 mg/kg p.o. 798 ng/mL 2.82 h 2047 ng·h/mL / /
体内研究
(In Vivo)

CXCR6 antagonist 1 (30-60 mg/kg；灌胃；每日；第 4 天至第 30 天) 可显著降低雌性 NOD/SCID 小鼠体内 SK-HEP-1 肝癌的肿瘤重量[1]。

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

Animal Model: NOD/SCID (female)[1]
Dosage: 30 mg/kg; 60 mg/kg
Administration: p.o.; daily; Day 4 to Day 30
Result: Reduced mean excised tumor weight to 59 ± 9 mg (30 mg/kg dose) and 55 ± 24 mg (60 mg/kg dose), with both doses showing significant reduction relative to vehicle control (P < 0.05).
Achieved tumor growth inhibition comparable to positive control cyclophosphamide.
Caused no deaths, behavioral phenotypes, or distinct body weight differences relative to control.
分子量

549.61

Formula

C27H30F3N3O4S
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

CXCR6 antagonist 1 相关分类

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  • 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:

CXCR6 antagonist 12579689-85-1CXCRCXC chemokine receptorsC-X-C motif chemokine receptorsβ-arrestin recruitmentforskolin-induced cAMP productioncyclophosphamidehuman CXCR6 receptorDiscoveRx cellsfemale NOD/SCID micehepatocellular carcinomamouse xenograft modelCXCL16SK-HEP-1 human hepatoma cellInhibitorinhibitorinhibit

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