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> (Rac)-Modipafant [122956-68-7]

(Rac)-Modipafant [122956-68-7]

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Cat# HY-108908-50mg

Size : 50mg

Brand : MedChemExpress


(Rac)-Modipafant (UK-74505) is an orally active, selective, long-acting irreversible platelet activating factor receptor (PAFR) antagonist. (Rac)-Modipafant prevents dengue infection.

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

(Rac)-Modipafant Chemical Structure

(Rac)-Modipafant Chemical Structure

CAS No. : 122956-68-7

This product is a controlled substance and not for sale in your territory.

Based on 1 publication(s) in Google Scholar

Other Forms of (Rac)-Modipafant:

  • Modipafant Get quote
Description

(Rac)-Modipafant (UK-74505) is an orally active, selective, long-acting irreversible platelet activating factor receptor (PAFR) antagonist. (Rac)-Modipafant prevents dengue infection[1][2][3].

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 (IC50=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].

MedChemExpress (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.
Molecular Weight

605.09

Formula

C34H29ClN6O3
CAS No.

122956-68-7
Appearance

Solid

Color

Light yellow to yellow

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
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
In Vitro: 

DMSO : 50 mg/mL (82.63 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 1.6526 mL 8.2632 mL 16.5265 mL
5 mM 0.3305 mL 1.6526 mL 3.3053 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. 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 (4.13 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.
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).
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

  • [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.  [Content Brief]

    [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.  [Content Brief]

    [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.  [Content Brief]

    [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.  [Content Brief]

    [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 Schmiedebergs Arch Pharmacol. 2013;386(1):51-59.  [Content Brief]

  • [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 Schmiedebergs Arch Pharmacol. 2013;386(1):51-59.

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. 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 1.6526 mL 8.2632 mL 16.5265 mL 41.3162 mL
5 mM 0.3305 mL 1.6526 mL 3.3053 mL 8.2632 mL
10 mM 0.1653 mL 0.8263 mL 1.6526 mL 4.1316 mL
15 mM 0.1102 mL 0.5509 mL 1.1018 mL 2.7544 mL
20 mM 0.0826 mL 0.4132 mL 0.8263 mL 2.0658 mL
25 mM 0.0661 mL 0.3305 mL 0.6611 mL 1.6526 mL
30 mM 0.0551 mL 0.2754 mL 0.5509 mL 1.3772 mL
40 mM 0.0413 mL 0.2066 mL 0.4132 mL 1.0329 mL
50 mM 0.0331 mL 0.1653 mL 0.3305 mL 0.8263 mL
60 mM 0.0275 mL 0.1377 mL 0.2754 mL 0.6886 mL
80 mM 0.0207 mL 0.1033 mL 0.2066 mL 0.5165 mL
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(Rac)-Modipafant Related Classifications

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Keywords:

(Rac)-Modipafant122956-68-7UK-74505UK74505UK 74505Dengue virusFlavivirusDENVselectivelong-actingirreversiblearticularinflammatoryhyperalgesiadengueinfectionInhibitorinhibitorinhibit