| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
|
Purity: ≥98%
Ladarixin sodium (DF 2156A), an investigational small-molecule drug, is a potent, orally bioavailable, non-competitive, dual allosteric inhibitor of CXCR1 and CXCR2 interleukin-8 (IL-8A and IL-8B, respectively). In preclinical studies, ladarixin was shown to prevent and reverse diabetes in NOD mice. The potency of CXCR1/2 inhibition may prevent inflammation- and autoimmunity-mediated damage of pancreatic islets. CXCR1/2 inhibition blocks and reverses type 1 diabetes in mice.
| ln Vitro |
Human polymorphonuclear leukocytes (PMN) are inhibited in their migration to CXCL8 (IC50 0.7 nM) by ladararixin [2].
|
|---|---|
| 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].
|
| 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. |
| References |
|
| Additional Infomation |
Ladarixin Sodium is the sodium salt form of ladarixin, an orally bioavailable, small molecule, dual inhibitor of C-X-C motif chemokine receptors 1 (CXCR1) and 2 (CXCR2), with potential anti-inflammatory and antineoplastic activities. Upon oral administration, ladarixin selectively targets and allosterically binds to CXCR 1 and 2, thereby preventing CXCR1 and CXCR2 activation by their ligand and pro-inflammatory chemokine interleukin 8 (IL-8 or CXCL8). This inhibits CXCR1/2-mediated signaling, which inhibits inflammatory processes, reduces both the recruitment and migration of immunosuppressive myeloid-derived suppressor cells (MDSCs) and neutrophils in the tumor microenvironment (TME), and abrogates the immunosuppressive-induced nature of the TME. This allows effector cells, such as natural killer (NK) cells and cytotoxic T-lymphocytes (CTLs), to kill and eliminate cancer cells, and inhibits tumor cell migration, metastasis, angiogenesis and tumor cell proliferation. CXCR1 and 2, G protein-coupled receptor proteins located on myeloid cells and certain tumor cells, play key roles in the immunosuppressive nature of the TME, tumor metastasis, resistance to chemotherapeutic agents and myeloid cell suppression. They also play a key role in inflammation and their expression is elevated in several inflammatory-driven diseases.
|
| 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