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| 1mg |
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| Targets |
vMIP-II (1-21) TFA targets CXCR4, a G protein-coupled receptor (GPCR). It interacts broadly with CC and CXC chemokine receptors, but its primary mechanism is as an antagonist of CXCR4. It inhibits CXCR4 by competing with its natural ligand, SDF-1 (CXCL12), for binding to the receptor. Specifically, it competes with 125I-SDF-1R for binding sites with an IC50 of 190 nM. By blocking CXCR4, it prevents downstream signaling that leads to cell migration and proliferation.
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| ln Vitro |
vMIP-II (1-21) TFA is a potent inhibitor of CXCR4, demonstrating an IC50 of 190 nM in a radioligand binding competition assay. It is a broad-spectrum chemokine receptor inhibitor, interacting with both CC and CXC receptors. This indicates that while it is a powerful tool for CXCR4 research, it may have off-target effects on other chemokine receptors, which can be exploited or avoided depending on the experimental context. It acts as an antagonist to block SDF-1-induced chemotaxis.
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| ln Vivo |
vMIP-II (1-21) TFA has been shown to be effective in vivo in mouse models of cancer and inflammation. For example, in a xenograft model of breast cancer metastasis, intraperitoneal administration of the peptide (e.g., 5-20 mg/kg) reduces the number of metastatic nodules in the lungs by blocking the SDF-1/CXCR4 axis. It also mobilizes hematopoietic stem cells (HSCs) from the bone marrow into the bloodstream, a property used to harvest stem cells for transplantation.
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| Enzyme Assay |
The binding affinity of vMIP-II (1-21) TFA for CXCR4 is typically determined using a radioligand binding assay. Procedure: Membranes from CXCR4-expressing cells (e.g., HEK-293-CXCR4) are incubated with 0.1 nM of the radioligand 125I-SDF-1R (125I-SDF-1) in binding buffer (50 mM HEPES, pH 7.5, 1 mM CaCl2, 5 mM MgCl2, 0.5% BSA). Varying concentrations of vMIP-II (1-21) TFA (0.1 nM to 10 uM) are added. Non-specific binding is determined using 1 uM unlabeled SDF-1. After a 2-hour incubation at 25degC, bound radioligand is collected by filtration through GF/B filters. The radioactivity is counted, and the IC50 is calculated from the displacement curve.
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| Cell Assay |
The functional antagonism of CXCR4 can be assessed using a chemotaxis assay. Procedure: CXCR4-positive cells (e.g., Jurkat T cells or CEM cells) are harvested and resuspended in serum-free RPMI-1640 at 1x106 cells/mL. Cells are pre-incubated with varying concentrations of vMIP-II (1-21) TFA (e.g., 1-1000 nM) for 15 minutes at 37degC. The cells are then added to the upper chamber of a 24-well Transwell plate (5-um pore size). The lower chamber contains 600 uL of media with 10 ng/mL SDF-1 (the chemoattractant). The plate is incubated at 37degC for 2-4 hours. Migrated cells in the lower chamber are counted by flow cytometry or using a cell viability dye. The IC50 for inhibition of chemotaxis is calculated.
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| Animal Protocol |
In vivo efficacy can be evaluated in a xenograft mouse model of CXCR4-dependent tumor metastasis. Procedure: Female NOD/SCID mice (6-8 weeks) are injected intravenously (tail vein) with 5x105 luciferase-expressing MDA-MB-231 (breast cancer) cells. Three days post-injection, mice are randomized into groups (n=10). vMIP-II (1-21) TFA is dissolved in sterile PBS and administered intraperitoneally (IP) at 5, 10, and 20 mg/kg, daily for 4 weeks. The control group receives PBS. Mice are imaged weekly for lung metastasis using bioluminescence (IVIS system) after injecting luciferin. At week 4, lungs are harvested for histological analysis and metastatic nodule count. A reduction in lung metastasis in treated mice indicates in vivo efficacy.
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| ADME/Pharmacokinetics |
Specific PK data for vMIP-II (1-21) TFA is not provided. As a 21-amino acid peptide (MW ~2.3 kDa), it is not orally bioavailable and is typically administered via intraperitoneal or intravenous injection. The peptide is rapidly cleared from circulation with a half-life of minutes to hours due to proteolysis. The TFA salt form improves aqueous solubility (>10 mg/mL), facilitating formulation in saline for injection. For longer half-life, the peptide can be PEGylated or conjugated to a serum albumin binder.
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| Toxicity/Toxicokinetics |
Specific toxicity data for vMIP-II (1-21) TFA is not fully described. As an immune-modulating chemokine antagonist, potential on-target toxicity includes impaired immune cell trafficking, leading to increased susceptibility to infections. However, no severe toxicity has been reported in murine studies at therapeutic doses up to 20 mg/kg. Standard safety handling for peptides applies; it is for research use only and should not be administered to humans.
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| References | |
| Additional Infomation |
vMIP-II (1-21) TFA is a potent CXCR4 antagonist. CXCR4 is a co-receptor for HIV-1 entry, making it a target for HIV therapy. It is also highly expressed on many cancer cells and mediates metastasis to organs rich in SDF-1 (e.g., lungs, liver, bone). Blocking CXCR4 mobilizes hematopoietic stem cells, a strategy used clinically in stem cell harvests. While the full-length vMIP-II protein is a natural product, this truncated 1-21 peptide retains high affinity and specificity for CXCR4, making it a valuable and economical research tool for studying these processes. This product is not an approved drug.
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| Molecular Formula |
C108H169N33O27S.XC2HF3O2
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| Molecular Weight |
2425.84 (free base)
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| Appearance |
Solid Powder
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| Synonyms |
NT21MP TFA; V1 peptide TFA
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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: (1). 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 : ≥ 100 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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