1. GPCR/G Protein Immunology/Inflammation
  2. CXCR Apelin Receptor (APJ)
  3. ALX 40-4C Trifluoroacetate

ALX 40-4C Trifluoroacetate is a small peptide inhibitor of the chemokine receptor CXCR4, inhibits SDF-1 from binding CXCR4 with a Ki of 1 μM, and suppresses the replication of X4 strains of HIV-1; ALX 40-4C Trifluoroacetate also acts as an antagonist of the APJ receptor, with an IC50 of 2.9 μM.

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ALX 40-4C Trifluoroacetate

ALX 40-4C Trifluoroacetate 構造式

容量 価格(税別) 在庫状況 数量
1 mg $100 在庫あり
5 mg $250 在庫あり
10 mg $400 在庫あり
25 mg $600 お問い合わせ
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100 mg   お問い合わせ  

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Based on 1 publication(s) in Google Scholar

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製品説明

ALX 40-4C Trifluoroacetate is a small peptide inhibitor of the chemokine receptor CXCR4, inhibits SDF-1 from binding CXCR4 with a Ki of 1 μM, and suppresses the replication of X4 strains of HIV-1; ALX 40-4C Trifluoroacetate also acts as an antagonist of the APJ receptor, with an IC50 of 2.9 μM.

IC50 & Target[1][3]

SDF-1-CXCR4

1 μM (Ki)

APJ receptor

2.9 μM (IC50)

体外実験

ALX 40-4C Trifluoroacetate is a small peptide inhibitor of the chemokine receptor CXCR4, interacts with the second extracellular loop of CXCR4 and inhibits infection exclusively by blocking direct virus-CXCR4 interactions[1]. ALX 40-4C shows potent anti HIV-1 effect, with EC50s of 0.34 ± 0.04 μg/mL, 0.37 ± 0.01 μg/mL for HIV-1 NL4-3, NC10, and 0.18 ± 0.11 μg/mL, 0.06 ± 0.02 μg/mL for HIV-1 HXB2, HC43, respectively, and with a CC50 (50% cytotoxic concentration) of 21 μg/mL. ALX 40-4C also exhibits potent activity against env-recombinant HIV, with EC50s of 0.38 ± 0.01 μg/mL, 0.40 ± 0.0 μg/mL for HIV-1 NL4-3 env, NC10, and 1.34 ± 0.06 μg/mL, 1.02 ± 0.29 μg/mL for HIV-1 HXB2 env, HC43, and a CC50 of 21 μg/mL[2]. ALX 40-4C binds to APJ with an IC50 of 2.9 μM. ALX 40-4C inhibits HIV-1 gp120/APJ-mediated cell membrane fusion, with an IC50s of 3.41 μM and 3.1 μM for IIIB isolate and 89.6 isolate, respectively[3].

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

分子量

1464.74 (free base)

分子式

C56H113N37O10.xC2HF3O2

Appearance

Solid

Color

White to off-white

Sequence

Ac-{d-Arg}-{d-Arg}-{d-Arg}-{d-Arg}-{d-Arg}-{d-Arg}-{d-Arg}-{d-Arg}-{d-Arg}-NH2

Sequence Shortening

Ac-{d-Arg}-{d-Arg}-{d-Arg}-{d-Arg}-{d-Arg}-{d-Arg}-{d-Arg}-{d-Arg}-{d-Arg}-NH2

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Sealed storage, away from moisture
Powder -80°C 2 years
  -20°C 1 year
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

H2O : 50 mg/mL (Need ultrasonic)

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純度とドキュメンテーション
参考文献
キナーゼ実験
[3]

The stably transfected cells are harvested in PBS (Ca2+ and Mg2+ free) plus 0.5 nM EDTA and washed twice with PBS. Ligand binding experiments are performed using a single concentration (0.2 nM) of 125I-Apelin-13 in the absence or presence of increasing concentrations of unlabeled Apelin-13 or ALX 40-4C in a final volume of 100 μL of binding buffer (50 nM Hepes, pH 7.4, 1 nM CaCl2, 5 nM MgCl2, 0.1% bovine serum albumin) containing 5 × 105 cells. Nonspecific binding is determined by the addition of 1 μM unlabeled Apelin-13. Samples are incubated for 90 min at room temperature. The incubation is terminated by separating the cells from the binding buffer by centrifugation and washing once with 500 μL of cold binding buffer. Bound ligands are determined by counting gamma emissions. At least three independent experiments are performed[3].

MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。

参考文献
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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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    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.

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製品名:
ALX 40-4C Trifluoroacetate
製品番号:
HY-P7061A
数量:
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