This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
K134
Catalog No. T15640 CAS
189362-06-9
Synonyms:
OPC33509
K134 is an inhibitor of phosphodiesterase 3. The IC50s of K134 for PDE3A, PDE3B, PDE5, PDE2 and PDE4 are 0.1, 0.28, 12.1, <300 and <300 μM, respectively.
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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
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Biological Description
Chemical Properties
Storage
& Solubility Information
Description
K134 is an inhibitor of phosphodiesterase 3. The IC50s of K134 for PDE3A, PDE3B, PDE5, PDE2 and PDE4 are 0.1, 0.28, 12.1, >300 and >300 μM, respectively.
Targets&IC50
PDE3A:0.1 μM, PDE3B:0.28 μM, PDE5:12.1 μM
In vitro
K134 (K-134) inhibits rat platelet aggregation caused by collagen and ADP in a dose-dependent manner in vitro. K134 also inhibits mouse platelet aggregation induced by collagen and ADP in a dose-dependent manner (IC50s: 5.5 μM and 6.7 μM, respectively), in vitro experiments. The half-maximal (50%) inhibitory concentration (IC50) values of K134 are 2.5 μM and 3.2 μM, respectively [1].
In vivo
K134 obviously decreases the incidence of occlusive shunt thrombi at doses above 10 mg/kg (half-maximal effective dose: ED50=11 mg/kg). The effects of PDE3 inhibitors on thrombus formation are also investigated in an arteriovenous shunt model in rats. The plasma concentration of K134 is 0.43±0.08 μM (Cmax) at a dose of 10 mg/kg. K134 obviously prolongs middle cerebral artery (MCA) occlusion time at doses >10 mg/kg and decreases cerebral infarct size at 30 mg/kg in the stroke model (n?=?12, 87.5±5.6 vs. 126.8±7.5 mm3, P<0.01), indicating its potent antithrombotic effect. The overall bleeding risk of K134 is assessed in general in mice. K134 (30 mg/kg; Single oral administration) does not prolong bleeding time at a dose of compared to control (106±5 vs. 110±5 s, not significant). A sufficiently high enough plasma concentration of K134 (13.6±2.3 μM) is detected to inhibit platelet aggregation at 10 min after single administration in mice at a dose of 30 mg/kg, which is the same time point as the above test of bleeding time [1].
Synonyms
OPC33509
Molecular Weight
399.48
Formula
C22H29N3O4
CAS No.
189362-06-9
Storage
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Method for preparing DMSO master liquid: mg
drug pre-dissolved in μL DMSO (Master liquid concentration
mg/mL),
Method for preparing in vivo formulation:Take μL
DMSO master liquid, next add μL PEG300, mix and clarify, next add μL
Tween 80,mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation:Take μL
DMSO master liquid, next add μL Corn oil,mix and clarify.
Note:
Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.