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| Targets |
Modipafant racemate is a racemic 1,4-dihydropyridine compound that functions as an orally active, selective, and long-acting irreversible antagonist of the platelet-activating factor receptor (PAFR). By antagonizing PAFR, it inhibits the actions of platelet-activating factor (PAF), a key mediator in inflammation and immune responses. The compound's mechanism involves inhibiting PAF-induced platelet aggregation and other PAF-mediated effects. Modipafant racemate is used to study inflammatory and allergic conditions, such as arthritis and ischemia/reperfusion injury.
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| ln Vitro |
In vitro, Modipafant racemate inhibits PAF-induced aggregation of washed platelets in rabbits. Its activity as a PAFR antagonist is characterized by potent inhibition of PAF-mediated platelet aggregation. The compound's in vitro activity demonstrates its ability to block PAF signaling. Modipafant racemate is used as a research tool to study the role of PAF in inflammation and immune responses.
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| 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].
In vivo, Modipafant racemate can be used to study arthritis and ischemia/reperfusion (I/R) in the superior mesenteric artery (SMA) of the rat. It is an orally active compound that has been investigated for its potential in treating inflammatory and allergic conditions, such as asthma, by blocking the effects of PAF. Its in vivo efficacy is attributed to its ability to antagonize PAFR and inhibit PAF-mediated inflammation. The compound's long-acting irreversible antagonism provides sustained effects. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for Modipafant racemate typically involve measuring its binding affinity to the platelet-activating factor receptor (PAFR). Radioligand binding assays using membrane preparations expressing PAFR are performed to determine the binding affinity. These assays confirm the compound's mechanism of action as a PAFR antagonist. The compound's selectivity for PAFR over other receptors can also be assessed.
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| Cell Assay |
In vitro cellular assays for Modipafant racemate typically involve measuring its ability to inhibit PAF-induced platelet aggregation. Platelets are treated with the compound and stimulated with PAF, and aggregation is measured using aggregometry. The compound inhibits PAF-induced aggregation in a concentration-dependent manner. These cell-based studies demonstrate the compound's functional antagonism at PAFR and its ability to block PAF-mediated platelet activation.
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| 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. In vivo animal models for Modipafant racemate include models of arthritis and ischemia/reperfusion (I/R) injury in the rat. The compound is administered orally, and disease severity or tissue damage is assessed. Modipafant racemate has been investigated for its potential in treating inflammatory conditions by blocking the effects of PAF. Doses and administration routes are optimized based on the specific model and experimental endpoints. These studies provide evidence for the compound's in vivo efficacy in inflammatory and ischemic conditions. |
| ADME/Pharmacokinetics |
Modipafant racemate has a molecular formula of C34H29ClN6O3 and a molecular weight of 605.09 g/mol. It is a racemic 1,4-dihydropyridine compound. The compound is typically stored under appropriate conditions to maintain stability. Its physicochemical properties support its use in both in vitro and in vivo studies. Modipafant racemate's solubility and formulation for administration should be optimized based on specific experimental requirements.
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| Toxicity/Toxicokinetics |
Modipafant racemate is a PAFR antagonist with a well-characterized mechanism of action. As with any drug, potential toxicity may include effects on the cardiovascular and immune systems. The compound's safety profile should be evaluated in preclinical toxicology studies. Modipafant racemate is for research use only and is not approved for human therapeutic use. It represents a valuable tool for studying PAF biology and its role in inflammation.
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| References |
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| Additional Infomation |
See also: Modipafant (note moved to).
Modipafant racemate (CAS# 122956-68-7), also known as (Rac)-Modipafant or UK-74505, is an orally active, selective, and long-acting irreversible antagonist of the platelet-activating factor receptor (PAFR). It inhibits PAF-induced aggregation of washed platelets in rabbits. The compound can be used to study arthritis and ischemia/reperfusion (I/R) in the superior mesenteric artery (SMA) of the rat. It is for research use only and is not approved for human therapeutic use. |
| Molecular Formula |
C34H29CLN6O3
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| Molecular Weight |
605.095
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| Exact Mass |
604.199
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| CAS # |
122956-68-7
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| Related CAS # |
Modipafant;122957-06-6
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| PubChem CID |
129796
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.34g/cm3
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| Index of Refraction |
1.681
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| LogP |
7.329
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
44
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| Complexity |
1120
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
ODRYSCQFUGFOSU-UHFFFAOYSA-N
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| 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)
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| 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
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| Synonyms |
UK 74505; UK-74505; Modipafant racemate
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~82.63 mM)
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| 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.
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.
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