2. GPCR/G Protein Immunology/Inflammation Anti-infection
  3. CXCR HIV
  4. CXCR4 antagonist 4

CXCR4 antagonist 4 是一种有效，具有口服活性的 CXCR4 拮抗剂 (IC50=24 nM)，可降低 CYP 2D6 的活性，提高 PAMPA 的通透性，有效抑制人类免疫缺陷病毒的进入 (IC50=7 nM).

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CXCR4 antagonist 4 Chemical Structure

CXCR4 antagonist 4 Chemical Structure

CAS No. : 2761009-30-5

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CXCR4 antagonist 4 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

CXCR4 antagonist 4 is a potent, orally active CXCR4 antagonist (IC50=24 nM) with diminished CYP 2D6 activity, improved PAMPA permeability, potent inhibition of human immunodeficiency virus entry (IC50=7 nM)[1].

IC50 & Target

CXCR4

24 nM (IC50)

HIV

7 nM (IC50)

体外研究
(In Vitro)

CXCR4 antagonist 4 (Compound 30, 0.1~10 µM, 48 hours) displays the inhibition potencies against the X4 virus in TZM-bl cells (IC50=7 nM) [1].

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

CXCR4 antagonist 4 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: TZM-bl cells
Concentration: 0.1, 1, 10 µM
Incubation Time: 48 hours
Result: Displayed inhibition potencies against the X4 virus (IC50=7 nM)
体内研究
(In Vivo)

CXCR4 antagonist 4 (3, 10, 30 mg/kg) demonstrates better oral Bioavailability in a dose dependent and reached 27% for the 30 mg/kg[1]. Pharmacokinetic Parameters of CXCR4 antagonist 4 in mice[1].

Route Dose(mg/kg) T1/2(h) Cmax(ng/mL) C12h (ng/mL) AUC0-8h(h*ng/mL) % FPO (0-8 h) Cl (L/h/kg) Vd (L/kg)
iv 3 5.89 116 265 11.3 96.3
po 3 12.8 1.50 34.3 12.9
po 10 54.8 14.3 190 215
po 30 169 34.8 717 27.1

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

Animal Model: mice[1]
Dosage: 3, 10, 30 mg/kg
Administration:
Result: Demonstrated better oral bioavailability in a dose dependent and reached 27% for the 30 mg/kg.
分子量

497.67

Formula

C29H41F2N5
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

CXCR4 antagonist 4 相关分类

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  • 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:

CXCR4 antagonist 42761009-30-5CXCRHIVCXC chemokine receptorsC-X-C motif chemokine receptorsHuman immunodeficiency virusoral bioavailabilityTZM-bl cellsCXCR4X4 virusInhibitorinhibitorinhibit

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