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YM-264 

Cat. No.: HY-101833
Handling Instructions

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

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

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].

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].

Solvent & Solubility
In Vitro: 

10 mM in 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
10 mM 0.1850 mL 0.9248 mL 1.8496 mL
*Please refer to the solubility information to select the appropriate solvent.
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
Molecular Weight

540.67

Formula

C₂₈H₃₆N₄O₅S

CAS No.

131888-54-5

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

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
YM-264
Cat. No.:
HY-101833
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YM-264

Cat. No.: HY-101833