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| 10mg |
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| 100mg |
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| 250mg |
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Paquinimod (ABR‑215757; ABR215757) is a novel and potent S100A9 inhibitor that can prevent S100A9 binding to TLR-4 (Toll like receptor-4). Paquinimod reduces pathology in experimental collagenase-induced osteoarthritis, also has antiviral effects by rescuing the pneumonia with substantial reduction of viral loads in SARS-CoV-2-infected mice. Paquinimod treatment of collagenase-induced OA (CIOA) resulted in significantly reduced synovial thickening (57%), osteophyte size at the medial femur (66%) and cruciate ligaments (67%) and cartilage damage at the medial tibia (47%) and femur (75%; n=7, untreated n=6). Paquinimod reduces leukocyte recruitment during sterile inflammation. Paquinimod also reduced priming of proinflammatory effector CD4(+) T cells.
| ln Vivo |
The S100 family includes the calcium-binding protein S100A9. An immunomodulatory substance called paquinimod stops S100A9 from attaching to TLR-4. The pathology in experimental collagenase-induced osteoarthritis is reduced by prophylactic treatment with the S100A9 inhibitor Paquinimod[1]. In the NOD mouse, paquinimod is a strong inhibitor of the development of insulitis and diabetes. In order to evaluate the preventive effectiveness of Paquinimod on the development of diabetes in female NOD mice, groups of mice are given daily doses of Paquinimod at 0.04, 0.2, 1, and 5 mg/kg/day from week 10 to week 20. From 10 weeks of age to the experiment's endpoint at 40 weeks of age, glycosuria is examined once a week. The development of diabetes in the mice treated with paquinimod is clearly reduced in a dose-dependent manner[2].
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| Animal Protocol |
Mice
After being exposed to increasing concentrations of CO2, female NOD/MrkTac mice are cervically dislocated to induce unconsciousness. In order to examine how the Q-compound Paquinimod affects the onset of glycosuria and insulitis, mice are given daily doses of approximately 0.04, 0.2, 1, and 5 mg/kg body weight/day of Paquinimod dissolved in drinking water at varying concentrations. Paquinimod is administered to the mice beginning at either 10 or 15 weeks of age. In the various trials that are conducted, the length of the treatment varies from 5 to 23 weeks[2]. |
| References |
| Molecular Formula |
C21H22N2O3
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|---|---|
| Molecular Weight |
350.42
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| Exact Mass |
350.163
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| Elemental Analysis |
C, 71.98; H, 6.33; N, 7.99; O, 13.70
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| CAS # |
248282-01-1
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| Appearance |
White to off-white solid powder.
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| SMILES |
O=C(C1=C(O)C2=C(N(C)C1=O)C=CC=C2CC)N(CC)C3=CC=CC=C3
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| InChi Key |
DIKSYHCCYVYKRO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H22N2O3/c1-4-14-10-9-13-16-17(14)19(24)18(20(25)22(16)3)21(26)23(5-2)15-11-7-6-8-12-15/h6-13,24H,4-5H2,1-3H3
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| Chemical Name |
N,5-diethyl-4-hydroxy-1-methyl-2-oxo-N-phenyl-1,2-dihydroquinoline-3-carboxamide
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| Synonyms |
ABR‑215757; ABR 215757; ABR215757; Paquinimod.
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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 : 62.5~70 mg/mL ( 178.36~199.76 mM )
Ethanol : ~17 mg/mL H2O : < 0.1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.13 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: ≥ 2.08 mg/mL (5.94 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 10% DMSO+40% PEG300+5% Tween-80+45% Saline: ≥ 2.5 mg/mL (7.13 mM) Solubility in Formulation 4: 5 mg/mL (14.27 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 | 2.8537 mL | 14.2686 mL | 28.5372 mL | |
| 5 mM | 0.5707 mL | 2.8537 mL | 5.7074 mL | |
| 10 mM | 0.2854 mL | 1.4269 mL | 2.8537 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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