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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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Other Sizes |
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Purity: ≥98%
BAY-60-7550 (BAY-607550; BAY607550) is a novel, potent and selective PDE2 inhibitor with the potential to be used for the treatment of anxiety disorders. It inhibits PDE2 with IC50 values of 2.0 nM (bovine) and 4.7 nM (human). BAY-60-7550 antagonizes oxidative stress-induced anxiety-like behavioral effects in mice by increasing cGMP signaling. Phosphodiesterases (PDEs) are key regulatory enzymes of intracellular cAMP/cGMP levels. These second messengers play important regulatory roles in controlling steroidogenesis in the adrenal. Disruption of PDEs has been associated with a number of adrenal diseases.
Targets |
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ln Vitro |
In comparison to the control, Bay 60-7550 (1 μM) raises cGMP in neuronal cells [F (6,14) for Bay 60-7550=12.97, p<0.05]. In comparison to NMDA alone, Bay 60-7550 increased cGMP even more when NMDA (30 μM) was present. The rise in cGMP in neuronal cultures caused by Bay 60-7550+NMDA is blocked by the NMDA receptor antagonist MK -801 (10 μM) [1]. Comparing IPAH patients' PASMC proliferation to untreated control cells, BAY 60-7550 (1 μM) dramatically inhibited it [2].
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ln Vivo |
When compared to vehicle + restraint stress settings, the PDE2 inhibitor Bay 60-7550 (1 mg/kg) corrected the behavioral alterations caused by restraint stress, leading to an increase in the percentage of open arm entry and open arm time. Comparing the vehicle-treated group to the non-stressed mice, Bay 60-7550 demonstrated a dosage-dependent increase in open arm entrance percentage and open arm time; notable increases were seen at a dose of 3 mg/kg. Compared to mice given a vehicle, non-stressed mice treated with Bay 60-7550 saw a dose-dependent increase in both the number and length of head immersions; at doses of 1 and 3 mg/kg, a noteworthy increase was noted [1].
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Enzyme Assay |
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Cell Assay |
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Animal Protocol |
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References |
[1]. Masood A, et al. Anxiolytic effects of phosphodiesterase-2 inhibitors associated with increased cGMP signaling. J Pharmacol Exp Ther. 2009 Nov;331(2):690-9.
[2]. Bubb KJ, et al. Inhibition of phosphodiesterase 2 augments cGMP and cAMP signaling to ameliorate pulmonary hypertension. Circulation. 2014 Aug 5;130(6):496-507 |
Molecular Formula |
C27H32N4O4
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Molecular Weight |
476.56738
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CAS # |
439083-90-6
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O=C1NC(CC2=CC=C(OC)C(OC)=C2)=NN3C1=C(C)N=C3[C@H]([C@H](O)C)CCCC4=CC=CC=C4
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InChi Key |
MYTWFJKBZGMYCS-NQIIRXRSSA-N
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InChi Code |
InChI=1S/C27H32N4O4/c1-17-25-27(33)29-24(16-20-13-14-22(34-3)23(15-20)35-4)30-31(25)26(28-17)21(18(2)32)12-8-11-19-9-6-5-7-10-19/h5-7,9-10,13-15,18,21,32H,8,11-12,16H2,1-4H3,(H,29,30,33)/t18-,21+/m1/s1
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Chemical Name |
2-(3,4-dimethoxybenzyl)-7-((2R,3R)-2-hydroxy-6-phenylhexan-3-yl)-5-methylimidazo[5,1-f][1,2,4]triazin-4(3H)-one
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Synonyms |
BAY 60-7550; BAY-607550; BAY607550; BAY 607550; BAY60-7550; BAY-60-7550;
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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 : ≥ 33.3 mg/mL (~69.87 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.25 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: ≥ 2.5 mg/mL (5.25 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.25 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.0983 mL | 10.4916 mL | 20.9833 mL | |
5 mM | 0.4197 mL | 2.0983 mL | 4.1967 mL | |
10 mM | 0.2098 mL | 1.0492 mL | 2.0983 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.