2. GPCR/G Protein Immunology/Inflammation
  3. CXCR
  4. CXCR4-IN-3

CXCR4-IN-3 (compound XVI) 是一种针对炎症相关受体 CXCR4 的口服有效抑制剂，IC50 为 3.2 nM。CXCR4-IN-3 表现出强效抗趋化活性，抑制率为 79.19±2.33%。CXCR4-IN-3 具有抗炎活性。CXCR4-IN-3 可用于 IBD (炎症性肠病)研究。

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CXCR4-IN-3 Chemical Structure

CXCR4-IN-3 Chemical Structure

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CXCR4-IN-3 相关抗体

Top Publications Citing Use of Products

查看 CXCR 亚型特异性产品:

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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

CXCR4-IN-3 (compound XVI) is an orally active and potent inhibitor targeting the inflammation-related receptor CXCR4, with an IC50 of 3.2 nM. CXCR4-IN-3 exhibits potent antichemotactic activity, at 79.19±2.33% inhibition. CXCR4-IN-3 shows anti-inflammatory activity. CXCR4-IN-3 can be used for IBD (inflammatory bowel disease) research[1].

IC50 & Target

CXCR4

3.2 nM (IC50)

体内研究
(In Vivo)

CXCR4-IN-3 (compound XVI) (25 mg/kg，灌胃，每天两次，连续 14 天)可缓解 DSS (葡聚糖硫酸钠)诱发的 IBD (炎症性肠病)，并与炎症细胞数量减少和炎症因子分泌减少有关[1]。
CXCR4-IN-3 (静脉注射 (2 mg/kg), 灌胃给药 (20 mg/kg)；一次)表现出合理的药代动力学特性[1]。

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

Animal Model: Male C57BL/6 mice (8 weeks, n=8 per group, DSS-Induced Colitis Model)[1]
Dosage: 25 mg/kg
Administration: Intragastrically, 100 μL/10 g, twice a day for 14 consecutive days
Result: Markedly relieved the condition of IBD; Significantly decreased the myeloperoxidase (MPO) levels; Blocked chronic inflammation of the intestinal tract.
Animal Model: Male Sprague-Dawley rats[1]
Dosage: iv (2 mg/kg) ig (20 mg/kg)
Administration: IV or IG, once (Pharmacokinetic Analysis)
Result: Pharmacokinetic Parameters of CXCR4-IN-3 in male Sprague-Dawley rats[1].
IV (2 mg/kg) IG (20 mg/kg)
Tmax (h) 0.08 0.25
t1/2 (h) 0.81±0.10 1.71±0.08
Cmax (ng/mL) 351.42±18.92 1436.41±805.36
AUC0-t (ng/mL∗h) 330.37±22.00 3010.81±283.96
AUC0-∞ (ng/mL∗h) 340.29±26.61 3070.77±325.73
CL (mL/h/kg) 5901.52±463.48 6565.45±741.43
V (mL/kg) 6037.79±278.59 16161.66±1798.44
F (%) 91.14
分子量

339.43

Formula

C20H25N3O2
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

CXCR4-IN-3 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

CXCR4-IN-3CXCRCXC chemokine receptorsC-X-C motif chemokine receptorsinflammatory bowel diseaseantichemotacticorally activeInhibitorinhibitorinhibit

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