[CAS NO. 189362-06-9] K134
PRODUCTS SPECIFICATIONS [189362-06-9]
DESCRIPTION [189362-06-9]
Overview
| MDL | MFCD28502069 |
|---|---|
| Molecular Weight | 399.48 |
| Molecular Formula | C22H29N3O4 |
| SMILES | O=C(NCCCOC1=CC2=C(NC(C=C2)=O)C=C1)N(C3CC3)[C@H]4[C@H](O)CCCC4 |
Summary
K134 is a phosphodiesterase 3 ( PDE3 ) inhibitor. The IC 50 s of K134 toward PDE3A , PDE3B , PDE5 , PDE2 and PDE4 are 0.1, 0.28, 12.1, >300 and >300 µM, respectively.
IC50 & Target
IC50: 0.1 µM (PDE3A), 0.28 µM (PDE3B), 12.1 μM (PDE5) [1]
In Vitro
K134 (K-134) inhibits rat platelet aggregation induced by collagen and ADP in a dose-dependent manner in vitro. The half-maximal (50%) inhibitory concentration (IC 50 ) values of K134 are 2.5 µM and 3.2 µM, respectively. In vitro experiments, K134 also inhibits mouse platelet aggregation induced by collagen and ADP in a dose-dependent manner, and the IC 50 s are 5.5 µM and 6.7 µM, respectively [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
K134 (K-134) significantly prolongs middle cerebral artery (MCA) occlusion time at doses >10 mg/kg, and reduces cerebral infarct size at 30 mg/kg in the stroke model (n = 12, 87.5±5.6 vs. 126.8±7.5 mm 3 , P<0.01), indicating its potent antithrombotic effect. The overall bleeding risk of K134 is assessed in general in mice. Single oral administration of K134 does not prolong bleeding time at a dose of 30 mg/kg compared to control (106±5 vs. 110±5 s, not significant). Moreover, 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. Next, the effects of PDE3 inhibitors on thrombus formation are also investigated in an arteriovenous shunt model in rats. K134 significantly reduces the incidence of occlusive shunt thrombi at doses above 10 mg/kg (half-maximal effective dose: ED 50 =11 mg/kg). The plasma concentration of K134 is 0.43±0.08 µM (C max ) at a dose of 10 mg/kg [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT00783081 | Kowa Research Institute, Inc. |
Intermittent Claudication
|
November 2008 | Phase 2 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvent & Solubility
DMSO : 50 mg/mL ( 125.16 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.5033 mL | 12.5163 mL | 25.0325 mL |
| 5 mM | 0.5007 mL | 2.5033 mL | 5.0065 mL |
| 10 mM | 0.2503 mL | 1.2516 mL | 2.5033 mL |