K134
Based on 1 Customer Validation
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.
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- Purity: 99.76%
- CAS No.: 189362-06-9
- 화학식: C22H29N3O4
- 분자량:399.48
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보관:
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)
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
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Biological Activity
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PDE2 |
PDE3 |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 189362-06-9
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Appearance Solid
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분자량 399.48
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화학식 C22H29N3O4
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Color White to off-white
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SMILES
O=C(NCCCOC1=CC2=C(NC(C=C2)=O)C=C1)N(C3CC3)[C@H]4[C@H](O)CCCC4
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Synonyms
OPC33509
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선적
Room temperature in continental US; may vary elsewhere.
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보관
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)
용액&용해도
DMSO : 50 mg/mL (125.16 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.26 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
순도&문서
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Data Sheet (273 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5033 mL | 12.5163 mL | 25.0325 mL | 62.5814 mL |
| 5 mM | 0.5007 mL | 2.5033 mL | 5.0065 mL | 12.5163 mL | |
| 10 mM | 0.2503 mL | 1.2516 mL | 2.5033 mL | 6.2581 mL | |
| 15 mM | 0.1669 mL | 0.8344 mL | 1.6688 mL | 4.1721 mL | |
| 20 mM | 0.1252 mL | 0.6258 mL | 1.2516 mL | 3.1291 mL | |
| 25 mM | 0.1001 mL | 0.5007 mL | 1.0013 mL | 2.5033 mL | |
| 30 mM | 0.0834 mL | 0.4172 mL | 0.8344 mL | 2.0860 mL | |
| 40 mM | 0.0626 mL | 0.3129 mL | 0.6258 mL | 1.5645 mL | |
| 50 mM | 0.0501 mL | 0.2503 mL | 0.5007 mL | 1.2516 mL | |
| 60 mM | 0.0417 mL | 0.2086 mL | 0.4172 mL | 1.0430 mL | |
| 80 mM | 0.0313 mL | 0.1565 mL | 0.3129 mL | 0.7823 mL | |
| 100 mM | 0.0250 mL | 0.1252 mL | 0.2503 mL | 0.6258 mL |
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