| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 100mg | |||
| Other Sizes |
| Targets |
AZ-1355 targets lipid metabolism and platelet aggregation pathways. It elevates the prostaglandin I₂ (PGI₂)/thromboxane A₂ (TXA₂) ratio, which is associated with vasodilation and inhibition of platelet aggregation. It may also interfere with leukotriene biosynthesis, potentially through 5-lipoxygenase or related pathways. Its lipid-lowering effects are mediated through mechanisms that reduce serum cholesterol levels.
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|---|---|
| ln Vitro |
In vitro, AZ-1355 elevates the prostaglandin I₂/thromboxane A₂ ratio, indicating its potential to promote vasodilation and inhibit platelet aggregation. It may also interfere with leukotriene biosynthesis. These activities suggest its potential as an anti-inflammatory and cardiovascular protective agent.
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| ln Vivo |
Rats treated with AZ-1355 at 50 mg/kg had a substantial reduction in serum TG, while at 100 mg/kg, rats showed a drop in both serum TC and serum TG. Rats fed CE-2 had lower total liver TC when given AZ-1355 (100 mg/kg), and rats fed a high-fat diet had lower liver TC when given the 50 mg/kg dose. In Triton hyperlipidemic mice, AZ-1355 (150 mg/kg) consistently lowers blood total cholesterol (TC) [1].
In vivo, AZ-1355 inhibits platelet aggregation and lowers serum total cholesterol levels. At a dose of 150 mg/kg, it reproducibly lowers serum total cholesterol in Triton hyperlipidemic mice. It is an orally active lipid-lowering agent. Its anti-inflammatory activity has also been investigated in vivo. |
| Enzyme Assay |
In vitro assays for AZ-1355 are conducted to evaluate its effects on prostaglandin I₂ and thromboxane A₂ production. Cells or tissues are incubated with the compound, and PGI₂ and TXA₂ levels are measured by ELISA or radioimmunoassay. Platelet aggregation assays are performed using platelet-rich plasma, and aggregation is induced by ADP or other agonists. 5-Lipoxygenase inhibition assays may also be conducted.
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| Cell Assay |
Cellular assays for AZ-1355 are performed using relevant cell lines to study its effects on lipid metabolism and inflammation. Cells are treated with compound concentrations ranging from 0.1 to 100 µM. Lipid accumulation is assessed using Oil Red O staining or by measuring cellular cholesterol levels. Inflammatory cytokine production (e.g., TNF-α, IL-6) is measured by ELISA.
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| Animal Protocol |
In vivo animal studies for AZ-1355 are conducted in Triton hyperlipidemic mice. The compound is administered orally at doses such as 150 mg/kg. Blood samples are collected to measure serum total cholesterol, triglycerides, and other lipid parameters. Platelet aggregation assays may be performed ex vivo. Inflammatory markers are also assessed in models of inflammation.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of AZ-1355 are not well characterized. The compound has a molecular weight of 299.33 and a molecular formula of C₁₇H₁₇NO₄. It is orally active, suggesting it has reasonable oral bioavailability. Standard PK studies in rodents would be required to determine half-life, bioavailability, and tissue distribution.
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| Toxicity/Toxicokinetics |
Toxicological data for AZ-1355 are limited. As a research compound, it is designated for laboratory use only. No significant acute toxicity has been reported at the doses used in efficacy studies. Standard toxicity screening would involve acute and repeated-dose studies in rodents.
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| References | |
| Additional Infomation |
AZ-1355 is an orally active lipid-lowering agent that inhibits platelet aggregation and elevates the PGI₂/TXA₂ ratio. It lowers serum total cholesterol in hyperlipidemic mice. It has a molecular weight of 299.33 and formula C₁₇H₁₇NO₄. It is not clinically approved.
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| Molecular Formula |
C17H17NO4
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|---|---|
| Molecular Weight |
299.32118
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| Exact Mass |
299.116
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| CAS # |
75451-07-9
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| PubChem CID |
339237
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| Appearance |
White to off-white solid powder
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| Density |
1.2g/cm3
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| Boiling Point |
489.2ºC at 760 mmHg
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| Flash Point |
249.7ºC
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| Index of Refraction |
1.57
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| LogP |
3.727
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
22
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| Complexity |
389
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(C1=CC=C2OC3=C(OC)C=CC=C3CNC2=C1)OCC
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| InChi Key |
ZKMRNPBEBOXDCJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H17NO4/c1-3-21-17(19)11-7-8-14-13(9-11)18-10-12-5-4-6-15(20-2)16(12)22-14/h4-9,18H,3,10H2,1-2H3
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| Chemical Name |
ethyl 10-methoxy-5,6-dihydrobenzo[b][1,4]benzoxazepine-3-carboxylate
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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: ~12.5 mg/mL (~41.8 mM; with ultrasonication and warming by heating to 60°C)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (4.18 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 can add 100 μL of DMSO stock solution (12.5 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 saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.25 mg/mL (4.18 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 DMSO stock solution (12.5 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 | 3.3409 mL | 16.7045 mL | 33.4091 mL | |
| 5 mM | 0.6682 mL | 3.3409 mL | 6.6818 mL | |
| 10 mM | 0.3341 mL | 1.6705 mL | 3.3409 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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