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

发表于2024年1月4日由Whatman官网

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	–		–	–

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FC131

发表于2023年12月16日由Whatman官网

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。

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

* Please select Quantity before adding items.

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.

CXCR4 antagonist 4

发表于2023年11月2日由Whatman官网

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 4 Chemical Structure

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

* Please select Quantity before adding items.

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) 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

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