| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Targets |
Foropafant targets the platelet-activating factor (PAF) receptor. PAF is a potent phospholipid mediator of inflammation and thrombosis. By binding to the PAF receptor with high affinity (Ki = 57 pM), foropafant blocks PAF-induced downstream signaling. This inhibits platelet aggregation, leukocyte activation, and vascular permeability.
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| ln Vitro |
In vitro, foropafant is a highly potent PAF receptor antagonist, with a Ki of 57 pM. It potently inhibits PAF-induced aggregation of rabbit and human platelets. Its competitive and selective nature has been characterized in receptor binding assays.
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| ln Vivo |
In vivo, foropafant is orally bioavailable. It inhibits PAF-mediated inflammatory and thrombotic responses. Its high potency and oral activity make it a promising candidate for treating PAF-related disorders, such as asthma, sepsis, and thrombosis.
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| Enzyme Assay |
In vitro receptor binding assays for foropafant measure its ability to displace [3H]PAF from the PAF receptor on platelet membranes. The Ki of 57 pM is determined from competition binding curves. Its selectivity for the PAF receptor over other receptors is assessed using broad screening panels.
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| Cell Assay |
In vitro cell-based assays for foropafant involve measuring its inhibition of PAF-induced platelet aggregation. Platelets are treated with the compound and then stimulated with PAF. Aggregation is measured using a platelet aggregometer. Its effects on leukocyte activation can also be assessed.
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| Animal Protocol |
In vivo animal experiments for foropafant have been conducted in models of PAF-induced shock and thrombosis. The compound is typically administered orally. Efficacy is measured by survival rates, inhibition of platelet aggregation, and reduction of inflammatory markers.
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| ADME/Pharmacokinetics |
Foropafant has a molecular weight of 464.71 and a molecular formula of C28H40N4S. It has a density of 1.1±0.1 g/cm3 and a boiling point of 571.6±60.0 °C. Its purity is typically ≥98%.
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| Toxicity/Toxicokinetics |
Foropafant is for research use only and is not intended for human use. Its safety profile is being evaluated in preclinical studies. As a potent PAF receptor antagonist, its toxicity is related to its mechanism of action. Standard safety precautions should be taken when handling.
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| References | |
| Additional Infomation |
Foropafant (SR27417) is a highly potent, competitive, selective, and orally bioavailable PAF receptor antagonist. It inhibits PAF binding with a Ki of 57 pM. It potently inhibits PAF-induced platelet aggregation. It has potential therapeutic applications in inflammatory and thrombotic diseases.
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| Molecular Formula |
C28H40N4S
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|---|---|
| Molecular Weight |
464.716
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| Exact Mass |
464.297
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| CAS # |
136468-36-5
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| PubChem CID |
119368
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| Appearance |
White to off-white solid powder
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| Density |
1.065g/cm3
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| Boiling Point |
571.6ºC at 760mmHg
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| Flash Point |
299.5ºC
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| Vapour Pressure |
4.49E-13mmHg at 25°C
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| Index of Refraction |
1.575
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| LogP |
7.143
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
33
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| Complexity |
548
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
VVBFISAUNSXQGZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C28H40N4S/c1-19(2)23-14-24(20(3)4)27(25(15-23)21(5)6)26-18-33-28(30-26)32(13-12-31(7)8)17-22-10-9-11-29-16-22/h9-11,14-16,18-21H,12-13,17H2,1-8H3
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| Chemical Name |
N,N-dimethyl-N'-(pyridin-3-ylmethyl)-N'-[4-[2,4,6-tri(propan-2-yl)phenyl]-1,3-thiazol-2-yl]ethane-1,2-diamine
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| Synonyms |
SR27417; SR 27417; SR-27417
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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 : ~100 mg/mL (~215.18 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.38 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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. Solubility in Formulation 2: 2.5 mg/mL (5.38 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. 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 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.38 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1518 mL | 10.7592 mL | 21.5183 mL | |
| 5 mM | 0.4304 mL | 2.1518 mL | 4.3037 mL | |
| 10 mM | 0.2152 mL | 1.0759 mL | 2.1518 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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