2. GPCR/G Protein
  3. Platelet-activating Factor Receptor (PAFR)
  4. YM-264

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.

For research use only. We do not sell to patients.

YM-264 Chemical Structure

YM-264 Chemical Structure

CAS No. : 131888-54-5

Size Stock
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
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YM-264 Related Antibodies

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

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.

IC50 & Target

pKi: 8.85 (PAF, rabbit platelet membranes)[1].
In Vitro

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.

YM-264 Related Antibodies
In Vivo

There are no significant differences in baseline airway responsiveness between control and YM-264 treated groups. Airway hyperresponsiveness induced by antigen exposure is significantly inhibited by the administration of YM-264. The baseline Rrs is 0.40 (0.02) cm H2O/mL/s in the control group (n=6). In the YM-264 treated groups, the baseline Rrs is 0.39 (0.01) and 0.36 (0.01) cm H2O/mL/s at a doses of 1 mg/kg (n=5) and 3 mg/kg (n=6), respectively. The Rrs during the IAR significantly increase from baseline to 0.92 (0.10) cm H2O/mL/s in control (p=0.0002), 0.81 (0.12) in YM-264 1 mg/kg (p=0.01), and 1.06 (0.29) in YM-264 3 mg/kg (p=0.048). Reelevation of Rrs in the late phase is observed in the control group after antigen challenge. At this phase, Rrs significantly increase to 0.72 (0.10) cm H2O/mL/s (p=0.0101) from the baseline (0.40) at 6 h after the exposure of antigen. In contrast, YM-264 at the doses of 1 and 3 mg/kg show significant inhibition of reelevation of Rrs as compared with control. YM-264 inhibit the eosinophil infiltration dose dependently[2].

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

540.67

Formula

C28H36N4O5S
CAS No.
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8496 mL 9.2478 mL 18.4956 mL
5 mM 0.3699 mL 1.8496 mL 3.6991 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References
Animal Administration
[2]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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). 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
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YM-264 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

YM-264131888-54-5YM264YM 264Platelet-activating Factor Receptor (PAFR)Inhibitorinhibitorinhibit

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