yingweiwo

Modipafant racemate

Alias: UK 74505; UK-74505; Modipafant racemate
Cat No.:V15337 Purity: ≥98%
(Rac)-Modipafant (UK-74505) is an oral, selective, long-acting, irreversible platelet-activating factor receptor (PAFR) receptor blocker (antagonist).
Modipafant racemate
Modipafant racemate Chemical Structure CAS No.: 122956-68-7
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
1mg
5mg
Other Sizes

Other Forms of Modipafant racemate:

  • Modipafant
Official Supplier of:
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Top Publications Citing lnvivochem Products
Product Description
(Rac)-Modipafant (UK-74505) is an oral, selective, long-acting, irreversible platelet-activating factor receptor (PAFR) receptor blocker (antagonist). (Rac)-Modipafant prevents severe dengue infection.
Biological Activity I Assay Protocols (From Reference)
ln Vivo
(Rac)-Modipafant (UK-74505) (10 mg/kg; PO; twice daily until day 10) stops serious dengue infection [3]. With an IC50 of 26.3 and 1.12 nM following 0.25 and 60 minutes of preincubation, respectively, (Rac)-Modipafant exhibits a highly selective, time-dependent suppression of PAF-induced aggregation of washed rabbit platelets [4]. (Rac)-Modipafant reduces zymosan-induced joint hyperalgesia in a dose-dependent manner (5–20 mg/kg; oral) [5].
Animal Protocol
Animal/Disease Models: 8 to 10 weeks old balb/c (Bagg ALBino) mouse (DEN-2 strain infection) [3]
Doses: 10 mg/kg
Route of Administration: Po; twice (two times) daily (starting on day 0, 3, 5 or 7 ) until day 10.
Experimental Results: The mortality rate associated with DEN-2 infection was diminished by approximately 50%.

Animal/Disease Models: Male BALB/C (8 to 10 weeks old) wild-type mice [5] Doses: 5, 10 and 20 mg/kg
Route of Administration: Oral
Experimental Results: Dose-dependent inhibition of zymosan-induced joint pain allergy.
References

[1]. 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]. 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]. 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]. 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]. 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.

Additional Infomation
See also: Modipafant (annotation moved to).
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C34H29CLN6O3
Molecular Weight
605.095
Exact Mass
604.199
CAS #
122956-68-7
Related CAS #
Modipafant;122957-06-6
PubChem CID
129796
Appearance
Light yellow to yellow solid powder
Density
1.34g/cm3
Index of Refraction
1.681
LogP
7.329
Hydrogen Bond Donor Count
2
Hydrogen Bond Acceptor Count
7
Rotatable Bond Count
8
Heavy Atom Count
44
Complexity
1120
Defined Atom Stereocenter Count
0
InChi Key
ODRYSCQFUGFOSU-UHFFFAOYSA-N
InChi Code
InChI=1S/C34H29ClN6O3/c1-4-44-34(43)31-30(24-9-5-6-10-25(24)35)29(33(42)40-28-11-7-8-17-37-28)20(2)38-32(31)22-12-14-23(15-13-22)41-21(3)39-26-19-36-18-16-27(26)41/h5-19,30,38H,4H2,1-3H3,(H,37,40,42)
Chemical Name
ethyl 4-(2-chlorophenyl)-6-methyl-2-[4-(2-methylimidazo[4,5-c]pyridin-1-yl)phenyl]-5-(pyridin-2-ylcarbamoyl)-1,4-dihydropyridine-3-carboxylate
Synonyms
UK 74505; UK-74505; Modipafant racemate
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ~50 mg/mL (~82.63 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.13 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.6526 mL 8.2631 mL 16.5262 mL
5 mM 0.3305 mL 1.6526 mL 3.3052 mL
10 mM 0.1653 mL 0.8263 mL 1.6526 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
  • Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume
An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
  • To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
/

Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
+
+
+

Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Contact Us