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[CAS NO. 122956-68-7] (Rac)-Modipafant
| Ships within | Stock | Price | Qty | Total |
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| Catalog: | HY-108908 |
| Brand: | MCE |
| CAS: | 122956-68-7 |
Overview
| MDL | MFCD00864793 |
|---|---|
| Molecular Weight | 605.09 |
| Molecular Formula | C34H29ClN6O3 |
| SMILES | O=C(C1=C(C2=CC=C(N3C(C)=NC4=C3C=CN=C4)C=C2)NC(C)=C(C(NC5=NC=CC=C5)=O)C1C6=CC=CC=C6Cl)OCC |
Summary
In Vivo
(Rac)-Modipafant (UK-74505) (10 mg/kg; p.o.; twice a day until day 10) prevents Severe Dengue Infection
[3]
.
(Rac)-Modipafant exhibits highly selective, time-dependent inhibition of PAF-induced aggregation of rabbit washed platelets (IC
50
=26.3 and 1.12 nM after 0.25 and 60 min preincubation, respectively)
[4]
.
(Rac)-Modipafant (5-20 mg/kg; p.o.) dose-dependently inhibits the Zymosan -induced articular hyperalgesia
[5]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | 8- to 10-week-old BALB/c mice (DEN-2 strain infected) [3] |
| Dosage: | 10 mg/kg |
| Administration: | P.o.; twice a day (started on days 0, 3, 5, or 7) until day 10 |
| Result: | Decreased by approximately 50% the lethality associated with DEN-2 infection. |
| Animal Model: | Male BALB/C (8- to 10- week-old) wild-type mice [5] |
| Dosage: | 5, 10 and 20 mg/kg |
| Administration: | P.o. |
| Result: | Dose-dependently inhibited the Zymosan -induced articular hyperalgesia. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 50 mg/mL ( 82.63 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.6526 mL | 8.2632 mL | 16.5265 mL |
| 5 mM | 0.3305 mL | 1.6526 mL | 3.3053 mL |
| 10 mM | 0.1653 mL | 0.8263 mL | 1.6526 mL |
-
1.
References
- [1] O'Connor BJ, et al. Inhibitory effect of UK,74505, a potent and specific oral platelet activating factor (PAF) receptor antagonist, on airway and systemic responses to inhaled PAF in humans. Am J Respir Crit Care Med. 1994;150(1):35-40.
- [2] Alabaster VA, et al. UK-74,505, a novel and selective PAF antagonist, exhibits potent and long lasting activity in vivo. Agents Actions Suppl. 1991;34:221-227.
- [3] Parry MJ, Alabaster VA, et al. Pharmacological profile of UK-74,505, a novel and selective PAF antagonist with potent and prolonged oral activity. J Lipid Mediat Cell Signal. 1994;10(3):251-268.
- [4] Souza DG, et al. Essential role of platelet-activating factor receptor in the pathogenesis of Dengue virus infection. Proc Natl Acad Sci U S A. 2009;106(33):14138-14143.
- [5] Guerrero AT, et al. The role of PAF/PAFR signaling in zymosan-induced articular inflammatory hyperalgesia [published correction appears in Naunyn Schmiedebergs Arch Pharmacol. 2013 Apr;386(4):351. Zaperlon, Ana C [corrected to Zarpelon, Ana C]]. Naunyn Sc
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