CXCR4 antagonist 4

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CXCR4 antagonist 4

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

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).

生物活性

CXCR4 antagonist4 is a potent, orally activeCXCR4antagonist (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].

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)	T_1/2(h)	C_max(ng/mL)	C_12h(ng/mL)	AUC_0-8h(h*ng/mL)	% F_PO(0-8 h)	Cl (L/h/kg)	V_d(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

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

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.