Art. -Nr.: HY-U00186

K134

(Synonyms: OPC33509)

Kundenbewertung

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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Reinheit: 99.76%
CAS. Nr.: 189362-06-9
Formel: C₂₂H₂₉N₃O₄
Molecular Weight:399.48

Speicherung:

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)

K134 Chemical Structure

CAS. Nr.: 189362-06-9

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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.

IC₅₀ & Target

PDE2

PDE3

Alle Phosphodiesterase (PDE) Isoform-spezifische Produkte anzeigen :

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 (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.

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 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 (C_max) at a dose of 10 mg/kg^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 189362-06-9
Appearance Solid
Molecular Weight 399.48
Formel C₂₂H₂₉N₃O₄
Color White to off-white
SMILES

O=C(NCCCOC1=CC2=C(NC(C=C2)=O)C=C1)N(C3CC3)[C@H]4[C@H](O)CCCC4
Synonyms

OPC33509
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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)

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.26 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Protokoll

Animal Administration^[1]

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.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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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K134

Metabolism/Protease Compound Library

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Multi-Target Compound Library

Bioactive Compound Library Max

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Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle Phosphodiesterase (PDE) Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

K134

Metabolism/Protease Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Anti-Cardiovascular Disease Compound Library

Anti-Alzheimer's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Anti-Colorectal Cancer Compound Library

Antidepressant Compound Library

Metabolic Enzyme Compound Library

Cysteine Targeted Covalent Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle Phosphodiesterase (PDE) Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

K134 Related Classifications

HY-U00186 Related Classifications