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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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K134 Chemical Structure
K134, CAS 189362-06-9
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25 mg 6-8 weeks $ 1,670.00
50 mg 6-8 weeks $ 2,180.00
100 mg 6-8 weeks $ 2,800.00
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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

TargetMolReferences and Literature

1. Yoshida H, et al. K-134, a phosphodiesterase 3 inhibitor, prevents brain damage by inhibiting thrombus formation in a rat cerebral infarction model. PLoS One. 2012;7(10):e46432.

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Keywords

K134 189362-06-9 Metabolism PDE K 134 OPC33509 OPC-33509 K-134 OPC 33509 inhibitor inhibit

 

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