| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 50mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
Ladarixin Sodium targets the chemokine receptors CXCR1 and CXCR2. It acts as an allosteric, non-competitive dual antagonist. By blocking these receptors, it inhibits neutrophil migration and reduces inflammation. It is being studied for its potential to preserve pancreatic beta-cell function in type 1 diabetes.
|
|---|---|
| ln Vitro |
Human polymorphonuclear leukocytes (PMN) are inhibited in their migration to CXCL8 (IC50 0.7 nM) by ladararixin [2].
In vitro, Ladarixin Sodium is a potent and selective dual CXCR1/2 antagonist. It inhibits CXCR1 and CXCR2-mediated signaling and chemotaxis. It is the sodium salt form of Ladarixin, which has been shown to inhibit PMN migration to CXCL8 with an IC50 of 0.7 nM. Detailed in vitro activity data are available in the primary literature. |
| ln Vivo |
In a single OVA exposure scenario, ladararixin (10 mg/kg; oral, once daily) decreases allergic airway inflammation. In a chronic OVA exposure model, ladararixin decreases bronchial hyperresponsiveness, remodeling, and allergic airway inflammation [1]. Ladararixin (10 mg/kg; orally, once day for 8 days) decreases the fibrosis and inflammation of the lungs caused by bleomycin in mice [1]. Ladararixin (10 mg/kg; once daily, oral) prevents mice's influenza A infection from getting worse when exposed to cigarette smoke [1]. Additionally, ladararixin successfully lowers polymorphonuclear leukocyte infiltration generated by CXCL8 in a number of animal models without significantly lowering systemic neutrophil numbers in a dose-related manner [2].
In vivo, Ladarixin Sodium is being investigated for its potential in treating inflammatory conditions including COPD, asthma, and type 1 diabetes. It may help preserve pancreatic beta-cell function in type 1 diabetes. It is an orally active compound. Detailed in vivo efficacy data are available in preclinical literature. |
| Enzyme Assay |
In vitro binding assays for Ladarixin Sodium typically involve evaluating its inhibition of CXCR1 and CXCR2 using calcium flux assays or chemotaxis assays. Cells expressing CXCR1 or CXCR2 are treated with varying concentrations of the compound and stimulated with CXCL8. Calcium mobilization is measured using fluorescent indicators. IC50 values are calculated from dose-response curves.
|
| Cell Assay |
Cell-based assays for Ladarixin Sodium involve culturing human polymorphonuclear leukocytes (PMNs) or cells expressing CXCR1/CXCR2. Cells are treated with Ladarixin Sodium at concentrations ranging from 0.01 nM to 10 µM. Chemotaxis is assessed using transwell migration assays toward CXCL8. Calcium flux is measured using fluorescent indicators. Cytotoxicity is assessed by standard viability assays.
|
| Animal Protocol |
Animal/Disease Models: Mouse (cigarette smoke induced exacerbation model of influenza A infection) [1]
Doses: 10 mg/kg Route of Administration: Oral one time/day on days 2, 3 and 4 after infection Experimental Results: Dramatically attenuated exacerbation of lethality and respiratory changes noted in the CSFlu group. In vivo animal experiments for Ladarixin Sodium typically involve administration to rodent models of inflammation or type 1 diabetes via oral gavage. Inflammatory markers are measured. Pancreatic beta-cell function is assessed by measuring insulin production and glucose tolerance. Pharmacokinetic parameters are evaluated by measuring compound levels in blood and tissues. Toxicity is assessed by monitoring body weight and organ histology. |
| ADME/Pharmacokinetics |
Ladarixin Sodium (molecular weight 397.32, formula C11H11F3NNaO6S2) is orally active. It is the sodium salt of Ladarixin. It is soluble in DMSO. Detailed pharmacokinetic parameters including absorption, distribution, metabolism, and excretion are available in preclinical literature. It has favorable properties for oral administration.
|
| Toxicity/Toxicokinetics |
No detailed toxicology data are specifically available for Ladarixin Sodium from the search results. As a CXCR1/2 antagonist, potential toxicity may include effects on immune function. Comprehensive toxicological evaluation including acute, subchronic, and genotoxicity studies has likely been conducted in preclinical development. The compound is for research use only.
|
| References |
|
| Additional Infomation |
Ladarexin sodium is the sodium salt form of lardaraxine, a small-molecule dual inhibitor with high oral bioavailability that inhibits CXC motif chemokine receptors 1 (CXCR1) and 2 (CXCR2), exhibiting potential anti-inflammatory and antitumor activities. After oral administration, lardaraxine selectively targets and allosterically binds to CXCR1 and CXCR2, thereby preventing their activation by their ligands and the pro-inflammatory chemokine interleukin-8 (IL-8 or CXCL8). This inhibits CXCR1/2-mediated signaling, thereby suppressing the inflammatory process, reducing the recruitment and migration of immunosuppressive myeloid-derived suppressor cells (MDSCs) and neutrophils in the tumor microenvironment (TME), and eliminating the immunosuppressive properties of the TME. This enables effector cells, such as natural killer (NK) cells and cytotoxic T lymphocytes (CTLs), to kill and eliminate cancer cells and inhibit tumor cell migration, metastasis, angiogenesis, and proliferation. CXCR1 and CXCR2 are G protein-coupled receptors located on myeloid cells and certain tumor cells, playing crucial roles in the immunosuppressive properties of the tumor microenvironment (TME), tumor metastasis, chemotherapy resistance, and myeloid cell suppression. They also play a key role in inflammation and are elevated in a variety of inflammatory diseases.
Ladarixin Sodium (DF-2156A) (CAS#: 865625-56-5) is an orally active, allosteric, non-competitive dual CXCR1/2 antagonist. It is used for research of COPD, asthma, and type 1 diabetes. Molecular weight: 397.32, formula: C11H11F3NNaO6S2. |
| Molecular Formula |
C11H11F3NNAO6S2
|
|---|---|
| Molecular Weight |
397.323122262955
|
| Exact Mass |
396.987
|
| CAS # |
865625-56-5
|
| Related CAS # |
Ladarixin;849776-05-2
|
| PubChem CID |
23709380
|
| Appearance |
White to off-white solid powder
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
10
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
24
|
| Complexity |
630
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
C[C@H](C1=CC=C(C=C1)OS(=O)(=O)C(F)(F)F)C(=O)[N-]S(=O)(=O)C.[Na+]
|
| InChi Key |
QICAUCDBOAKDNS-OGFXRTJISA-M
|
| InChi Code |
InChI=1S/C11H12F3NO6S2.Na/c1-7(10(16)15-22(2,17)18)8-3-5-9(6-4-8)21-23(19,20)11(12,13)14/h3-7H,1-2H3,(H,15,16)/q+1/p-1/t7-/m1./s1
|
| Chemical Name |
sodium (R)-(methylsulfonyl)(2-(4-(((trifluoromethyl)sulfonyl)oxy)phenyl)propanoyl)amide
|
| Synonyms |
DF-2156A DF2156A DF 2156A DF-2156 DF2156 DF 2156
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~251.69 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.29 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.29 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.29 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5169 mL | 12.5843 mL | 25.1686 mL | |
| 5 mM | 0.5034 mL | 2.5169 mL | 5.0337 mL | |
| 10 mM | 0.2517 mL | 1.2584 mL | 2.5169 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA