标签归档：cxcr

CXCR4 antagonist 4

发表于由

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).

CXCR4 antagonist 4amp;;

CXCR4 antagonist 4 Chemical Structure

规格 是否有货
100 mg ; 询价 ;
250 mg ; 询价 ;
500 mg ; 询价 ;

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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.

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
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.
参考文献

  • [1]. Jecs E, et al. Synthesis and Evaluation of Novel Tetrahydronaphthyridine CXCR4 Antagonists with Improved Drug-like Profiles. J Med Chem. 2022, 65(5):4058-4084.

BDPA-Zn CXCR4拮抗剂BDPA-Zn 品牌：FUJIFILM Wako

发表于由

BDPA-Zn

CXCR4拮抗剂BDPA-Zn

品牌：FUJIFILM Wako
CAS No.：360579-05-1
储存条件：2-10℃
纯度：–
产品编号

(生产商编号)

 等级 规格 运输包装 零售价(RMB) 库存情况 参考值

024-16431

 for Cellbiology 10 mg –

BDPA-Zn CXCR4拮抗剂BDPA-Zn 品牌：FUJIFILM Wako

 – –


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FC131

发表于由

FC131;

FC131 是一种有效的 CXCR4 拮抗剂，可以抑制 [125I]-SDF-1 与 CXCR4 结合，IC50 值为 4.5 nM。FC131 具有抗 HIV 的活性。

FC131amp;;

FC131 Chemical Structure

CAS No. : 606968-52-9

规格 价格 是否有货
1 mg ￥2500 询问价格 货期
5 mg ￥7500 询问价格 货期
10 mg ￥12750 询问价格 货期

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FC131 的其他形式现货产品:

FC131 TFA

生物活性

FC131 is a potent CXCR4 antagonist. FC131 inhibits [125I]-SDF-1 binding to CXCR4 with an IC50 of 4.5 nM. FC131 has anti-HIV activity[1].

IC50 Target

125I-SDF-CXCR4

4.5 nM (IC50)

HIV

;

分子量

729.83

Formula

C36H47N11O6
CAS 号

606968-52-9
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.
Solvent Solubility
In Vitro:;

H2O

Peptide Solubility and Storage Guidelines:

1.;;Calculate the length of the peptide.

2.;;Calculate the overall charge of the entire peptide according to the following table:

; Contents Assign value
Acidic amino acid Asp (D), Glu (E), and the C-terminal -COOH. -1
Basic amino acid Arg (R), Lys (K), His (H), and the N-terminal -NH2 +1
Neutral amino acid Gly (G), Ala (A), Leu (L), Ile (I), Val (V), Cys (C), Met (M), Thr (T), Ser (S), Phe (F), Tyr (Y), Trp (W), Pro (P), Asn (N), Gln (Q) 0

3.;;Recommended solution:

Overall charge of peptide Details
Negative (lt;0) 1.;;Try to dissolve the peptide in water first.
2.;;If water fails, add NH4OH (lt;50 μL).
3.;;If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide.
Positive (gt;0) 1.;;Try to dissolve the peptide in water first.
2.;;If water fails, try dissolving the peptide in a 10%-30% acetic acid solution.
3.;;If the peptide still does not dissolve, try dissolving the peptide in a small amount of DMSO.
Zero (=0) 1.;;Try to dissolve the peptide in organic solvent (acetonitrile, methanol, etc.) first.
2.;;For very hydrophobic peptides, try dissolving the peptide in a small amount of DMSO, and then dilute the solution with water to the desired concentration.
参考文献

  • [1]. Tamamura H, et al. Stereoselective synthesis of [L-Arg-L/D-3-(2-naphthyl)alanine]-type (E)-alkene dipeptide isosteres and its application to the synthesis and biological evaluation of pseudopeptide analogues of the CXCR4 antagonist FC131. J Med Chem. 2005 Jan 27;48(2):380-91.