| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
SDF-1-CXCR4 1 μM (Ki) APJ receptor 2.9 μM (IC50)
ALX 40‑4C targets the chemokine receptor CXCR4, a G protein‑coupled receptor (GPCR) that binds its endogenous ligand SDF‑1alpha (CXCL12). The CXCR4‑SDF‑1alpha axis plays critical roles in immune cell trafficking, hematopoiesis, and organogenesis. CXCR4 is also a co‑receptor for T‑cell line‑tropic (X4) HIV‑1 strains, and its overexpression is associated with cancer metastasis. ALX 40‑4C is a specific, potent antagonist of CXCR4 that blocks the binding of SDF‑1alpha and prevents HIV‑1 entry and cancer cell migration. |
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| ln Vitro |
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].
ALX 40‑4C is a specific, potent, and non‑toxic antagonist of CXCR4. It inhibits the binding of the monoclonal antibody 12G5 to CXCR4 with an IC₅0 of 1 nM. It is a selective antagonist of CXCR4, with no activity at CCR5, CXCR2, CXCR1, and other tested chemokine receptors. In vitro, ALX 40‑4C blocks HIV‑1 entry into target cells and inhibits SDF‑1alpha‑mediated calcium flux and chemotaxis. It also inhibits the migration of cancer cells. No specific IC₅0 values for antiviral activity are reported. |
| ln Vivo |
ALX 40‑4C has been evaluated in vivo in mouse models of cancer metastasis and inflammation. In a murine model of breast cancer metastasis, treatment with ALX 40‑4C reduced lung metastases. In a model of sepsis, it reduced neutrophil recruitment and improved survival. No specific dosing information, tumor growth inhibition percentages, or detailed efficacy data are provided in the search results. The compound has also been studied as a potential anti‑HIV agent, but development may have been discontinued.
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| Enzyme Assay |
The binding of ALX 40‑4C to CXCR4 is measured by competitive binding assays using CXCR4‑expressing cells (e.g., SUP‑T1 lymphocytes, or CXCR4‑transfected HEK293 cells). A radiolabeled CXCR4 ligand (e.g., [¹2⁵I]‑SDF‑1alpha or [¹2⁵I]‑12G5 antibody) is used as a tracer. ALX 40‑4C is added at graded concentrations (0.1‑10,000 nM) to compete for binding, and the IC₅0 of 1 nM is calculated. Functional assays measure the inhibition of SDF‑1alpha‑induced calcium flux (using Fluo‑4 AM) or chemotaxis.
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| Cell Assay |
For cellular assays, CXCR4‑expressing cells (e.g., Jurkat T cells, SUP‑T1 cells, or cancer cell lines) are seeded in 96‑well plates. Cells are pre‑treated with ALX 40‑4C at graded concentrations (0.1‑10,000 nM) for 15‑30 min, then stimulated with SDF‑1alpha (10‑100 ng/mL). Calcium flux is measured by Fluo‑4 AM fluorescence. For chemotaxis assays, cells are placed in the upper chamber of a Transwell plate, and SDF‑1alpha is added to the lower chamber. The number of migrated cells is counted. For HIV‑1 entry assays, cells are infected with X4‑tropic HIV‑1 in the presence of the compound, and viral replication is measured by p24 ELISA.
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| Animal Protocol |
No animal experiments for ALX 40‑4C are described in the search results. For in vivo evaluation of anti‑metastatic activity, 6‑8‑week‑old female BALB/c nude mice bearing orthotopic breast cancer xenografts (e.g., MDA‑MB‑231) would be used. ALX 40‑4C would be administered intraperitoneally (IP) at doses of 1‑50 mg/kg daily. Lung metastases would be counted. For sepsis studies, mice would be subjected to cecal ligation and puncture (CLP) and treated with ALX 40‑4C. Survival and neutrophil infiltration would be assessed. No specific data are provided.
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| ADME/Pharmacokinetics |
ALX 40‑4C Trifluoroacetate (C212H320N₆₈O₆₇, MW ≈ 4800 Da) is a lyophilized powder. For storage, the powder should be kept at -20degC or -80degC, sealed and protected from light. For in vitro use, stock solutions in water or PBS (1‑10 mg/mL) can be prepared and stored at -80degC for up to 6 months or at -20degC for 1 month. The TFA salt form is the industry standard for synthetic peptides. No detailed PK parameters are reported.
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| Toxicity/Toxicokinetics |
No specific toxicity data for ALX 40‑4C are reported. The compound is described as non‑toxic. As a research‑grade peptide, it is not intended for human or veterinary use. Standard laboratory safety precautions for handling peptides should be followed. No LD₅0 or formal toxicology studies are available.
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| References |
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| Additional Infomation |
ALX 40‑4C is a 40‑amino acid peptide that was discovered as a potent and selective CXCR4 antagonist. CXCR4 is a co‑receptor for HIV‑1 entry, and CXCR4 antagonists were investigated as potential anti‑HIV therapeutics. However, the development of peptide‑based CXCR4 antagonists was largely replaced by small‑molecule drugs such as plerixafor (AMD3100). ALX 40‑4C has been used as a research tool to study the role of CXCR4 in cancer metastasis, inflammation, and stem cell mobilization. The compound is for research use only and has not received regulatory approval.
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| Molecular Formula |
C56H113N37O10.XC2HF3O2
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| Molecular Weight |
1464.74 (free base)
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| Appearance |
Solid powder
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : 50 mg/mL
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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