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| 10mg |
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| Targets |
LDV targets α4β1 integrin (also known as VLA-4), a cell surface receptor that mediates cell adhesion and migration. α4β1 integrin is involved in the homing of hematopoietic stem cells and the migration of leukocytes to sites of inflammation. By binding to α4β1 integrin with a Kd of ~12 nM, LDV serves as a ligand for studying integrin-mediated adhesion and signaling, particularly in the context of leukemia and inflammatory diseases.
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| ln Vitro |
A well-characterized VLA-4 ligand known as an LDV small molecule has been utilized to identify conformational changes and VLA-4 affinity[1]. The minimal sequence of fibronectin's CS-1 region required to bind α4β1 integrin is known as LDV[2].
In vitro, LDV binds to α4β1 integrin in leukemia cells. As a non-fluorescent analog of LDV-FITC, it is used as a competitor in binding assays to study integrin-ligand interactions. The Kd for α4β1 integrin binding is approximately 12 nM. These in vitro characteristics support its use in studying integrin-mediated cell adhesion, migration, and signaling in cancer and inflammatory diseases. |
| ln Vivo |
In vivo data for LDV is not extensively reported in publicly available sources. As an α4β1 integrin ligand, the compound has potential applications in animal models of leukemia, inflammation, and autoimmune diseases where integrin-mediated cell adhesion and migration play a role. However, specific published in vivo efficacy studies are not detailed in the current literature. LDV is primarily used as a research tool for studying integrin biology.
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| Enzyme Assay |
The in vitro integrin binding assay for LDV uses purified α4β1 integrin or α4β1-expressing cells. LDV is incubated with the integrin at varying concentrations, and binding is detected using competitive displacement of a fluorescently labeled ligand (e.g., LDV-FITC). The Kd value of ~12 nM is determined from binding curves. Cell adhesion assays may be performed to assess the functional effects of LDV on integrin-mediated adhesion.
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| Cell Assay |
Cellular assays for LDV are conducted in α4β1 integrin-expressing cell lines, such as leukemia cells. Cells are treated with varying concentrations of LDV, and integrin binding is assessed using flow cytometry or fluorescence microscopy with labeled ligands. Cell adhesion and migration assays are performed to evaluate the functional consequences of integrin engagement. The compound's effects on integrin signaling pathways may be assessed by Western blotting.
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| Animal Protocol |
In vivo studies for LDV would typically involve animal models of leukemia, inflammation, or autoimmune diseases. The compound would be administered via intravenous injection or other routes at doses determined by pharmacokinetic studies. Efficacy would be assessed by measuring tumor cell homing, leukocyte migration, or disease progression. However, specific published in vivo protocols for LDV are not available in the current literature. The compound is currently used as a research tool.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for LDV is not extensively reported in publicly available sources. The compound has a molecular weight of 979.13 g/mol and a molecular formula of C48H70N10O12. It has a CAS number of 1155866-55-9. It is soluble in 0.01M PBS (pH 7.4) at 1 mg/mL. Storage: powder at -20°C for 3 years or in solvent at -80°C for 1 year. As a peptide, it is expected to have limited oral bioavailability.
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| Toxicity/Toxicokinetics |
Toxicity data for LDV is limited in publicly available sources. As a peptide ligand for α4β1 integrin, it is expected to have a favorable safety profile. However, as with all research compounds, LDV is intended for research use only and not for human therapeutic applications. Standard in vitro cytotoxicity assays and in vivo tolerability studies would be required for a complete toxicity assessment.
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| References | |
| Additional Infomation |
LDV (CAS 1155866-55-9) is a tripeptide and non-fluorescent analog of LDV-FITC. It is an α4β1 integrin (VLA-4) ligand with a Kd of approximately 12 nM. LDV binds to α4β1 integrin in leukemia cells. It has a molecular formula of C48H70N10O12 and a molecular weight of 979.13 g/mol. LDV is a valuable research tool for studying integrin-mediated cell adhesion, migration, and signaling in cancer and inflammatory diseases.
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| Molecular Formula |
C48H70N10O12
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| Molecular Weight |
979.129211902618
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| Exact Mass |
978.517
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| CAS # |
1155866-55-9
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| PubChem CID |
87384936
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| Appearance |
White to off-white solid powder
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| LogP |
-0.3
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| Hydrogen Bond Donor Count |
11
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| Hydrogen Bond Acceptor Count |
13
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| Rotatable Bond Count |
26
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| Heavy Atom Count |
70
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| Complexity |
1820
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| Defined Atom Stereocenter Count |
7
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| SMILES |
O=C([C@H](C(C)C)NC([C@H](CC(=O)O)NC([C@H](CC(C)C)NC(CC1C=CC(=CC=1)NC(NC1C=CC=CC=1C)=O)=O)=O)=O)N1CCC[C@H]1C(N[C@H](C(N[C@@H](C)C(N[C@H](C(=O)O)CCCCN)=O)=O)C)=O
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| InChi Key |
FQYZPSNPTJYQKB-CGTMUHGOSA-N
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| InChi Code |
InChI=1S/C48H70N10O12/c1-26(2)23-35(53-38(59)24-31-17-19-32(20-18-31)52-48(70)56-33-14-9-8-13-28(33)5)43(64)55-36(25-39(60)61)44(65)57-40(27(3)4)46(67)58-22-12-16-37(58)45(66)51-29(6)41(62)50-30(7)42(63)54-34(47(68)69)15-10-11-21-49/h8-9,13-14,17-20,26-27,29-30,34-37,40H,10-12,15-16,21-25,49H2,1-7H3,(H,50,62)(H,51,66)(H,53,59)(H,54,63)(H,55,64)(H,57,65)(H,60,61)(H,68,69)(H2,52,56,70)/t29-,30-,34-,35-,36-,37-,40-/m0/s1
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| Chemical Name |
(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-3-carboxy-2-[[(2S)-4-methyl-2-[[2-[4-[(2-methylphenyl)carbamoylamino]phenyl]acetyl]amino]pentanoyl]amino]propanoyl]amino]-3-methylbutanoyl]pyrrolidine-2-carbonyl]amino]propanoyl]amino]propanoyl]amino]hexanoic acid
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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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.0213 mL | 5.1066 mL | 10.2131 mL | |
| 5 mM | 0.2043 mL | 1.0213 mL | 2.0426 mL | |
| 10 mM | 0.1021 mL | 0.5107 mL | 1.0213 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
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.
Link: https://clinicaltrials.gov/ct2/show/NCT01260350
Conditions:Chronic Hepatitis C InfectionProducts are for research use only; We do not sell to patients
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