YM-264
Based on 1 Customer Validation
YM-264 is a selective, potent and orally active platelet-activating factor (PAF) antagonist with a pKi value of 8.85 for rabbit platelet membranes.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.24%
- CAS. Nr.: 131888-54-5
- Formel: C28H36N4O5S
- Molecular Weight:540.67
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Speicherung:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
pKi: 8.85 (PAF, rabbit platelet membranes)[1].
The anti-platelet-activating factor effect of YM-264 is examined in vitro. YM-264 inhibits [3H] platelet-activating factor binding to rabbit platelet membranes with a pKivalue of 8.85. YM-264 inhibits the platelet-activating factor-induced human, rabbit and guinea-pig platelet aggregation with pA2 values of 8.68, 8.33 and 8.14, 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.
Chemical Information
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CAS. Nr. 131888-54-5
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Appearance Solid
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Molecular Weight 540.67
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Formel C28H36N4O5S
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Color White to light yellow
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SMILES
O=C(N1CCN(CCC(C2=CC=CC=C2)(C)C)CC1)C3NC(C4=CC=CN=C4)SC3.O=C(O)/C=C/C(O)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (184.96 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). 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). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.62 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 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.62 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)
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.
Protokoll
Guine Pigs[2]
Male Hartley guinea pigs weighing approximately 300 g are sensitized. The animals are fixed in position with the nose and mouth directed toward the center of the cylinder. Ovalbumin (10 mg/mL) is administered daily for 10 min. On the ninth or tenth day, all of the animals exhibit asthmatic symptoms. Two booster inhalations of AO (10 mg/mL) are subsequently given to the guinea pigs for 5 min at weekly intervals. Forty-five animals are randomized into three experimental groups by the order of their capture from shipping crate. Each group is further divided into three subgroups for control, YM-264 (1 mg/kg) and YM-264 (3 mg/kg). One week after the second booster inhalation, 16 animals for AH experiment are randomly divided into three subgroups for control and YM-264 treatment (1 and 3 mg/kg), and they are exposed to aerosolized OA (10 mg/mL) for 5 min. A dose of 1 or 3 mg/kg of YM264 is administered orally 30 min before and again, 3 h after the exposure to OA. The control group receives 0.5% methylcellulose in the same volume as YM-264[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (276 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Yamada T, et al. Pharmacological properties of YM264, a potent and orally active antagonist of platelet-activating factor. Arch Int Pharmacodyn Ther. 1990 Nov-Dec;308:123-36. [Content Brief]
[2]. Arima M, et al. Effect of YM264 on the airway hyperresponsiveness and the late asthmatic response in a guinea pig model of asthma. Chest. 1995 Aug;108(2):529-34. [Content Brief]
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). 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 | 1.8496 mL | 9.2478 mL | 18.4956 mL | 46.2389 mL |
| 5 mM | 0.3699 mL | 1.8496 mL | 3.6991 mL | 9.2478 mL | |
| 10 mM | 0.1850 mL | 0.9248 mL | 1.8496 mL | 4.6239 mL | |
| 15 mM | 0.1233 mL | 0.6165 mL | 1.2330 mL | 3.0826 mL | |
| 20 mM | 0.0925 mL | 0.4624 mL | 0.9248 mL | 2.3119 mL | |
| 25 mM | 0.0740 mL | 0.3699 mL | 0.7398 mL | 1.8496 mL | |
| 30 mM | 0.0617 mL | 0.3083 mL | 0.6165 mL | 1.5413 mL | |
| 40 mM | 0.0462 mL | 0.2312 mL | 0.4624 mL | 1.1560 mL | |
| 50 mM | 0.0370 mL | 0.1850 mL | 0.3699 mL | 0.9248 mL | |
| 60 mM | 0.0308 mL | 0.1541 mL | 0.3083 mL | 0.7706 mL | |
| 80 mM | 0.0231 mL | 0.1156 mL | 0.2312 mL | 0.5780 mL | |
| 100 mM | 0.0185 mL | 0.0925 mL | 0.1850 mL | 0.4624 mL |
YM-264 Related Classifications
HY-101833 Related Classifications
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