| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 50mg | |||
| 100mg | |||
| Other Sizes |
| Targets |
BAY 60-6583 targets the adenosine A2B receptor, a G protein-coupled receptor (GPCR). It acts as a partial agonist, binding to the receptor and activating downstream signaling pathways. Its affinity (Ki) for human/mouse/rat A2B receptors is 114/136/100 nM, respectively, as determined by binding assays with [3H]PSB-603.
|
|---|---|
| ln Vitro |
In CHO cells expressing recombinant human A1, A2A, or A2B ARs, BAY 60-6583 displays EC50 values for receptor activation >10,000 nM for both A1 and A2A AR and 3 nM for A2B AR subtype[1]. When baY 60-6583 (0 -10 μM) is used without siRNA, its highest agonist effect is 68%, which is notably different from when 5, 50, and 500 nM siRNA are present (54%, 48%, and 36%, respectively). In T24 cells, it displays BAY EC50 values of 98±22, 102±17, 127±31, and 93±19 nM, respectively, in the absence and presence of siRNA[3]. In RAW264.7 preosteoclasts, BAY 60-6583 (5 μM; 24 hours) boosts cell accumulation at the G1 phase while decreasing the G2/M phase[4]. While BAY 60-6583 (5 μM; 24 hours) does not influence M-CSF-induced ERK1/2 activation in RAW264, it selectively suppresses the activation of Akt by M-CSF.[4] Seven preosteoclasts.
In vitro, BAY 60-6583 activates the A2B receptor with high potency (EC50 = 3 nM). Its selectivity for A2B over other adenosine receptor subtypes is confirmed in radioligand binding and functional assays. It is used as a research tool to study the role of A2B receptors in various physiological processes. |
| ln Vivo |
In ischemic rabbit hearts, BAY 60-6583 (intravenous injection; 100 mcg/kg) decreases the infarction area soon before reperfusion[1]. ?When used as a pre-treatment, BAY 60-6583 (intraperitoneal injection; 2 mg/kg) greatly reduces the amount of lung damage caused by lipopolysaccharide (LPS). IL-6 levels in WT-mice, although the administration of BAY 60-6583 fails to abolish these inflammatory markers in?A2BAR?//? ?mice [2]. ?Intratumoral treatment of BAY 60-6583 results in a considerable increase in tumor-infiltrating MDSCs; it has no effect on the cells' capacity to inhibit T-cell proliferation or maturation stage, and it also promotes the creation of CCL2 and IL-10 within the tumor tissue[5].
In vivo, BAY 60-6583 has been shown to have cardioprotective effects in myocardial ischemia models. It is a research compound used to study the therapeutic potential of A2B receptor activation in cardiovascular and other diseases. |
| Enzyme Assay |
The in vitro receptor binding assay for BAY 60-6583 involves measuring its affinity for the A2B receptor. This is typically done using a radioligand binding assay with [3H]PSB-603 and membrane preparations from cells expressing the receptor. Competition binding experiments are performed to determine the Ki.
|
| Cell Assay |
Cell Cycle Analysis[4]
Cell Types: RAW264.7 preosteoclasts Tested Concentrations: 5 μM Incubation Duration: 48 hrs (hours) Experimental Results: Caused an arrest of cells at the G1 phase. Western Blot Analysis[4] Cell Types: RAW264.7 preosteoclasts Tested Concentrations: 5 μM Incubation Duration: 48 hrs (hours) Experimental Results: demonstrated an inhibition of M-CSF-mediated Akt activation and resulted in the decrease of osteoclast proliferation. In vitro cellular assays for BAY 60-6583 are performed on cells expressing the A2B receptor. The functional activity is measured by its ability to increase cAMP levels. The EC50 for receptor activation is determined. |
| Animal Protocol |
Animal/Disease Models: A2BAR−/− mice on a C57BL/6J mice[1]
Doses: 2 mg/kg Route of Administration: intraperitoneal (ip)injection; 2 mg/kg Experimental Results: Demonstrated attenuation of lung inflammation and pulmonary edema in wild-type but not in gene-targeted mice for the A2BAR. In vivo animal experiments for BAY 60-6583 are conducted in models of myocardial ischemia, such as the left anterior descending (LAD) coronary artery occlusion model in rodents. The compound is administered, and its effects on infarct size, cardiac function, and survival are assessed. |
| ADME/Pharmacokinetics |
BAY 60-6583 has been studied in preclinical models and has characterized pharmacokinetic properties. It is typically administered intraperitoneally or intravenously. Its half-life and metabolism have been studied in animals. It is typically stored as a powder.
|
| Toxicity/Toxicokinetics |
Specific toxicity data for BAY 60-6583 are not readily available in the public domain, as it is primarily a research compound. Its selectivity for A2B receptors suggests a potentially favorable safety profile. As with all research chemicals, standard laboratory safety practices should be followed.
|
| References |
|
| Additional Infomation |
BAY 60-6583 belongs to the cyanopyridine class of compounds. Its chemical name is 6-amino-3,5-dicyano-4-(4-hydroxyphenyl)-2-thiopyridine, in which the hydrogen atoms on the hydroxyl and thio groups are replaced by cyclopropylmethyl and carboxamide methyl groups, respectively. It exhibits adenosine A2B receptor agonist, cardioprotective, and anti-inflammatory activities. It is an aminopyridine, cyanopyridine, aryl sulfide, monocarboxylic acid amide, aromatic ether, and cyclopropane compound.
BAY 60-6583 is a research compound used to study the adenosine A2B receptor. It is not an FDA-approved drug and is exclusively for research purposes. It is a valuable tool for investigating the role of A2B receptors in cardiovascular diseases and other conditions. |
| Molecular Formula |
C19H17N5O2S
|
|---|---|
| Molecular Weight |
379.43558
|
| Exact Mass |
379.11
|
| CAS # |
910487-58-0
|
| PubChem CID |
11717831
|
| Appearance |
White to light yellow solid powder
|
| LogP |
4.171
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
27
|
| Complexity |
629
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
ZTYHZMAZUWOXNC-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C19H17N5O2S/c20-7-14-17(12-3-5-13(6-4-12)26-9-11-1-2-11)15(8-21)19(24-18(14)23)27-10-16(22)25/h3-6,11H,1-2,9-10H2,(H2,22,25)(H2,23,24)
|
| Chemical Name |
2-[6-amino-3,5-dicyano-4-[4-(cyclopropylmethoxy)phenyl]pyridin-2-yl]sulfanylacetamide
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~263.55 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 4.17 mg/mL (10.99 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 41.7 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: ≥ 4.17 mg/mL (10.99 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 41.7 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6355 mL | 13.1773 mL | 26.3546 mL | |
| 5 mM | 0.5271 mL | 2.6355 mL | 5.2709 mL | |
| 10 mM | 0.2635 mL | 1.3177 mL | 2.6355 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.
|
|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
