| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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Purity: ≥98%
Ladarixin (DF2156A), 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 by ladararixin (IC50, 0.7 nM) [2].
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| ln Vivo |
In a single OVA exposure scenario, ladararixin (10 mg/kg; oral once daily) decreases allergic airway variables. Ladararixin (10 mg/kg; face once daily for 8 days) decreases pulmonary bleomycin in mice effects in vivo and fibrosis[1]. Ladararixin attenuates allergic airway factors, cough, and asthmatic hyperresponsiveness in a chronic OVA exposure paradigm. Ladararixin (10 mg/kg); once daily for three days on the face. days) to shield the nails from recurrent harmful infections brought on by cigarette smoking [1]. In several animal models, ladarixin cardiotype dramatically lowers systemic neutrophils without appreciably affecting CXCL8-induced polymorphonuclear leukocyte respiration.
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| Animal Protocol |
Animal/Disease Models: Mouse (cigarette smoke-induced exacerbation of influenza A virus infection model) [ 1]
Doses: 10 mg/kg Route of Administration: Po one time/day on days 2, 3 and 4 after infection. Experimental Results: Cell count [2]. The worsening of lethality and respiratory changes noted in the CSFlu group was Dramatically attenuated. |
| References |
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| Additional Infomation |
Ladarixin is under investigation in clinical trial NCT04628481 (A Study of Oral Ladarixin in New-onset Type 1 Diabetes and a Low Residual Β-Cell Function).
Ladarixin is 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. Drug Indication Treatment of type I diabetes mellitus |
| Molecular Formula |
C11H12F3NO6S2
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|---|---|
| Molecular Weight |
375.3332
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| Exact Mass |
375.006
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| CAS # |
849776-05-2
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| Related CAS # |
Ladarixin sodium;865625-56-5
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| PubChem CID |
11372270
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| Appearance |
White to off-white solid powder
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| LogP |
4.096
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
23
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| Complexity |
624
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C[C@H](C1=CC=C(C=C1)OS(=O)(=O)C(F)(F)F)C(=O)NS(=O)(=O)C
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| InChi Key |
DDLPYOCJHQSVSZ-SSDOTTSWSA-N
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| InChi Code |
InChI=1S/C11H12F3NO6S2/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)/t7-/m1/s1
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| Chemical Name |
4-((2R)-1-Oxo-1-(methanesulfonamido)propan-2-yl)phenyl trifluoromethanesulfonate
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| Synonyms |
DF-2156A DF2156A DF 2156A DF-2156 DF2156 DF 2156 Ladarixin
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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 |
| 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) |
DMSO : ~100 mg/mL (~266.43 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.66 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 (6.66 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 (6.66 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 10 mg/mL (26.64 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6643 mL | 13.3216 mL | 26.6432 mL | |
| 5 mM | 0.5329 mL | 2.6643 mL | 5.3286 mL | |
| 10 mM | 0.2664 mL | 1.3322 mL | 2.6643 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.
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