| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
AZD8309 targets CXCR2, a chemokine receptor involved in neutrophil recruitment and activation. It is a potent and orally available CXCR2 antagonist. By inhibiting CXCR2, it regulates the transmigration of neutrophils. This modulates inflammatory responses and reduces tissue damage in inflammatory diseases.
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| ln Vitro |
In vitro, AZD8309 inhibits CXCR2-mediated neutrophil chemotaxis and transmigration in response to chemokines such as CXCL1 and CXCL8. It belongs to the bicyclic thiazolopyrimidine chemical class. Its ability to inhibit neutrophil recruitment has been demonstrated in various cell-based assays.
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| ln Vivo |
In mice with experimental pancreatitis, AZD8309 (50 mg/kg; twice daily; mouse model) decreases trypsin activation and neutrophil migration [1].
In vivo, AZD8309 significantly reduces MPO in the pancreas and lung, and decreases trypsin and elastase activity in the pancreas. It is an orally active antagonist of CXCR2 that regulates the transmigration of neutrophils. It can be used in the study of inflammatory diseases. |
| Enzyme Assay |
The activity of AZD8309 can be assessed using cell-based chemotaxis assays. Neutrophils are placed in a chamber with a membrane separating them from a solution containing a chemokine such as CXCL8. The number of cells that migrate across the membrane in the presence or absence of varying concentrations of AZD8309 is counted. The IC50 for inhibition of chemotaxis is determined from dose-response curves.
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| Cell Assay |
To evaluate the cellular effects of AZD8309, neutrophils are treated with the compound, and the inhibition of CXCR2-mediated signaling and chemotaxis is assessed. The effects on neutrophil activation and degranulation are evaluated.
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| Animal Protocol |
Animal/Disease Models: Experimental pancreatitis male C57BL6 mice (25-30 g) [1]
Doses: 50 mg/kg Route of Administration: po (oral gavage); start 3 hrs (hrs (hours)) before induction of pancreatitis, twice a day Experimental Results: in umbrella shape In pancreatitis, MPO was Dramatically diminished in the pancreas and lungs (8 hrs (hrs (hours)) and 24 hrs (hrs (hours))), and trypsin and elastase activities in the pancreas (8 hrs (hrs (hours))) were Dramatically diminished. diminished serum cytokine levels as well as histopathological damage. In vivo studies with AZD8309 typically involve administration to animals via oral routes. In models of inflammatory diseases such as pancreatitis or lung inflammation, the compound's effects on neutrophil infiltration, tissue damage, and inflammatory markers are assessed. |
| ADME/Pharmacokinetics |
AZD8309 has a molecular formula of C18H17N5O2S2 and a molecular weight of 399.49. Its CAS number is 333742-48-6. The compound is a potent, orally available CXCR2 antagonist. It is soluble in DMSO and other organic solvents. The purity is typically >98%.
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| Toxicity/Toxicokinetics |
Specific toxicology data for AZD8309 are not detailed in the available literature. However, as an immune modulator, it may have effects on the immune system. As with all research compounds, standard safety precautions should be taken during handling.
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| References | |
| Additional Infomation |
AZD8309 is a potent, orally available CXCR2 antagonist used in research on inflammatory diseases. It regulates neutrophil transport and reduces tissue damage in inflammatory conditions. It is a valuable tool for studying the role of CXCR2 in inflammation. It is not a clinically approved drug.
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| Molecular Formula |
C15H14F2N4O2S2
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|---|---|
| Molecular Weight |
384.424067020416
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| Exact Mass |
384.052
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| CAS # |
333742-48-6
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| Related CAS # |
333742-48-6;
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| PubChem CID |
12073810
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| Appearance |
White to off-white solid powder
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| LogP |
2.9
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
25
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| Complexity |
479
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| Defined Atom Stereocenter Count |
1
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| SMILES |
S1C(NC2C1=C(N=C(N=2)SCC1C=CC=C(C=1F)F)N[C@H](C)CO)=O
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| InChi Key |
SRHSMXLXWORYJK-SSDOTTSWSA-N
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| InChi Code |
InChI=1S/C15H14F2N4O2S2/c1-7(5-22)18-12-11-13(21-15(23)25-11)20-14(19-12)24-6-8-3-2-4-9(16)10(8)17/h2-4,7,22H,5-6H2,1H3,(H2,18,19,20,21,23)/t7-/m1/s1
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| Chemical Name |
(R)-5-((2,3-difluorobenzyl)thio)-7-((1-hydroxypropan-2-yl)amino)thiazolo[4,5-d]pyrimidin-2(3H)-one
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| Synonyms |
AZD8309 AZD-8309 AZD 8309
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 : ~50 mg/mL (~130.07 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6013 mL | 13.0066 mL | 26.0132 mL | |
| 5 mM | 0.5203 mL | 2.6013 mL | 5.2026 mL | |
| 10 mM | 0.2601 mL | 1.3007 mL | 2.6013 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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