| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| ln Vitro |
AZM198 (10 μM) reduced reactive oxygen species production, neutrophil degranulation, and neutrophil extracellular trap (NET) formation in TNFα-prestimulated and PR3-ANCA-activated human neutrophils, and attenuated the activity of myeloperoxidase, an enzyme-active enzyme, in PMA-stimulated human neutrophils [1]. In a system of TNFα-prestimulated, PR3-ANCA-activated neutrophils co-cultured with endothelial cells for 18 h, AZM198 (10 μM; 18 h) alleviated human neutrophil-mediated endothelial cell damage [1]. AZM198 (10 μM; 2 h) reduced NET formation in phorbol ester (PMA)-induced human neutrophil isolates from healthy donors [2].
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| ln Vivo |
In a mouse crescentic glomerulonephritis model, AZM198 (133-400 μmol/kg; orally; every 12 hours for 7 days) reduced kidney injury markers, including glomerular thrombosis, proteinuria, and plasma creatinine levels, without enhancing adaptive immune responses [1]. In a mouse crescentic glomerulonephritis model, AZM198 (133 μmol/kg; orally; twice daily for 48 hours) did not significantly reduce early glomerular neutrophil aggregation [1]. In a mouse adoptive transfer model, AZM198 (400 μmol/kg; orally; twice daily for 7 days) did not enhance antigen-specific T cell responses [1]. In this mouse model of antineutrophil cytoplasmic antibody-associated vasculitis, AZM198 (400 μmol/kg; administered by gavage; twice daily for 7 days) had no protective effect on the histological or biochemical markers of the disease [2]. AZM198 (500 μmol/kg; orally; administered continuously via feed formulation; 26 weeks) increased the survival rate of male SR-BIΔCT/ΔCT/Ldlr-/- mice fed a high-fat diet by 92% (up to 63%), reduced the incidence of major adverse cardiovascular events by 57%-75%, and alleviated inflammatory activity in cardiac fibrosis, liver injury, and atherosclerotic lesions [3]. AZM198 inhibited MPO activity in vulnerable atherosclerotic plaques, increased fibrous cap thickness by 65%, reduced intraplaque fibrin and hemosiderin, and promoted the formation of a more stable plaque phenotype in Apoe-/- mice with plaque instability caused by tandem stenosis [4].
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| Cell Assay |
Cell viability assay [1]
Cell Types: Endothelial cell-neutrophil co-culture Tested Concentrations: 10 μM; containing TNFα (2 ng/well) Incubation Duration: 18 hours Experimental Results: Reduced neutrophil-mediated endothelial cell damage. |
| Animal Protocol |
Animal/Disease Models:C57BL/6 (female, 10-12 weeks old, average weight 25 g, intravenously injected with sheep nephrotoxic serum mixed with LPS 1:1) [1]
Doses: 133 μmol/kg Route of Administration: Oral; twice daily; 48 hours Experimental Results: The median total cellular fluorescence (CTCF) corrected for Ly6g was 26.5 (23-70.7) AU, and there was no significant reduction in glomerular neutrophil infiltration compared with the vector control group. Animal/Disease Models:BALB/c (female) [1] Doses: 400 μmol/kg Route of Administration: Oral; twice daily for 7 days Experimental Results: The median frequency of CD44highCD4+ cells was 12.6% (11.8%-13.8%), and the number of activated total T cells was not significantly increased compared with the vector control group. The median frequency of CD44highKJ+CD4+ cells was 1.9% (1.64%-3.14%), and the number of activated ovalbumin-specific T cells was not significantly increased compared with the vector control group. Animal/Disease Models:C57BL6/J mice (female, 8 weeks old, G-CSF, anti-myeloperoxidase IgG and lipopolysaccharide-induced anti-neutrophil cytoplasmic antibody vasculitis model) [2] Doses: 400 μmol/kg per dose (total daily dose 128 mg/kg) Route of Administration: Gavage; twice daily; 7 days Experimental Results: There were no significant differences in the percentage of glomerular crescents, the number of glomerular neutrophils, the number of CD68 positive cells in or around the glomeruli, the serum creatinine level on day 7 or the urinary albumin/creatinine ratio on day 6 compared with the control group. |
| References |
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| Molecular Formula |
C14H13CLN4OS
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|---|---|
| Molecular Weight |
320.80
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| CAS # |
1933460-23-1
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| Appearance |
White to off-white solid
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| SMILES |
O=C1NC(N(CC2=CC=C(C=C2CN)Cl)C3=C1NC=C3)=S
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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 : ~16.67 mg/mL (~51.96 mM; ultrasonic and warming and heat to 60°C)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.67 mg/mL (5.21 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 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 canAdd 100 μL of DMSO stock solution (16.7 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of physiological saline: Dissolve 0.9 g of sodium chloride in double-distilled water and dilute to 100 mL to obtain clear physiological saline. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.67 mg/mL (5.21 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 canAdd 100 μL of DMSO stock solution (16.7 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1172 mL | 15.5860 mL | 31.1721 mL | |
| 5 mM | 0.6234 mL | 3.1172 mL | 6.2344 mL | |
| 10 mM | 0.3117 mL | 1.5586 mL | 3.1172 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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