K134 (OPC33509) (Synonyms: OPC33509) |
رقم الكتالوجGC32633
One-Click Copy Product Info
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K134 (OPC33509) هو مثبط فسفودايستراز 3 (PDE3).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 189362-06-9
Sample solution is provided at 25 µL, 10mM.
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K134 is a phosphodiesterase 3 (PDE3) inhibitor. The IC50s of K134 toward PDE3A, PDE3B, PDE5, PDE2 and PDE4 are 0.1, 0.28, 12.1, >300 and >300 µM, respectively.
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 (IC50) 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 IC50s are 5.5 µM and 6.7 µM, respectively[1].
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 mm3, 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: ED50=11 mg/kg). The plasma concentration of K134 is 0.43±0.08 µM (Cmax) at a dose of 10 mg/kg[1].
[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.
Animal experiment: | Mice[1] Male ICR mice, 5-8 weeks old, are used. K134 (K-134) and Warfarin are suspended and dissolved in 1% HPMC, respectively, and orally administered to ICR mice at 10 min or 24 h before testing of bleeding, respectively. Each mouse is placed in a restrainer, which exposes the tail. A 27G disposable needle is inserted about 6 mm into a tail vein 2 cm from the tip of the tail. Immediately after the operation, sheets of filter paper are placed under the injury site every 15 sec to absorb the blood, and the time point at which no blood is observed on the filter paper is regarded as the bleeding time. |
References: [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. | |
| Cas No. | 189362-06-9 | SDF | |
| المرادفات | OPC33509 | ||
| Canonical SMILES | O=C(NCCCOC1=CC2=C(NC(C=C2)=O)C=C1)N(C3CC3)[C@H]4[C@H](O)CCCC4 | ||
| Formula | C22H29N3O4 | M.Wt | 399.48 |
| الذوبان | DMSO : 50 mg/mL (125.16 mM; Need ultrasonic) | Storage | 4°C, away from moisture and light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5033 mL | 12.5163 mL | 25.0325 mL |
| 5 mM | 500.7 μL | 2.5033 mL | 5.0065 mL |
| 10 mM | 250.3 μL | 1.2516 mL | 2.5033 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 22 reference(s) in Google Scholar.)