| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
Fosdagrocorat targets the glucocorticoid receptor (GR) through its active metabolite, Dagrocorat. As a prodrug of Dagrocorat, Fosdagrocorat is converted into the active compound upon administration. Dagrocorat is a selective glucocorticoid receptor modulator that exhibits anti-inflammatory effects while minimizing the side effects typically associated with traditional glucocorticoids. The compound acts by selectively modulating the glucocorticoid receptor, providing anti-inflammatory benefits without significantly affecting metabolic or bone-related pathways. Fosdagrocorat's prodrug design may offer advantages in terms of oral bioavailability or tissue-specific delivery of the active compound.
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| ln Vitro |
Fosdagrocorat demonstrates in vitro activity as a glucocorticoid receptor agonist through its active metabolite Dagrocorat. The compound is a dissociated glucocorticoid receptor agonist. Fosdagrocorat is designed to provide anti-inflammatory effects through selective modulation of the glucocorticoid receptor while minimizing the side effects associated with traditional glucocorticoids. The compound's prodrug nature means that its activity depends on conversion to Dagrocorat. Detailed cellular activity data for the active metabolite are available in the primary literature for Dagrocorat.
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| ln Vivo |
Fosdagrocorat has been evaluated in preclinical and clinical studies for its anti-inflammatory effects. The compound is an orally available, potential dissociated glucocorticoid receptor agonist. Pharmacokinetics and food-effect studies of Fosdagrocorat have been conducted. The compound's prodrug design allows for oral administration and conversion to the active Dagrocorat, which provides anti-inflammatory benefits while minimizing side effects. Detailed in vivo efficacy data, including specific model results and dosing regimens, are available in the primary literature. Fosdagrocorat is a valuable tool for studying dissociated glucocorticoid receptor agonists as therapeutic agents for inflammatory diseases.
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| Enzyme Assay |
The in vitro receptor binding and transactivation assay for Fosdagrocorat measures the compound's ability to bind to and activate the glucocorticoid receptor. However, because Fosdagrocorat is a prodrug, its activity depends on conversion to Dagrocorat. Assays may be performed using the active metabolite or in the presence of enzymes that convert the prodrug to the active form. Glucocorticoid receptor binding affinity is assessed using radioligand binding assays with membrane preparations from cells expressing the human glucocorticoid receptor. For transactivation assays, cells are transfected with a GRE-linked reporter gene and treated with varying concentrations of Fosdagrocorat or Dagrocorat. Reporter gene activity is measured, and EC50 values are determined. The compound is dissolved in DMSO and diluted in assay buffer. Appropriate positive controls and negative controls are included in each assay run.
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| Cell Assay |
The in vitro cellular assay for Fosdagrocorat is performed using cells that express the glucocorticoid receptor and respond to glucocorticoid stimulation. Because Fosdagrocorat is a prodrug, its activity depends on conversion to Dagrocorat. Cells are cultured in appropriate medium and treated with varying concentrations of Fosdagrocorat or vehicle control (DMSO). Cells are stimulated with inflammatory stimuli to induce pro-inflammatory cytokine production. The effects of Fosdagrocorat on inflammatory cytokine production are measured by ELISA or qRT-PCR. The selectivity of the active metabolite for transrepression versus transactivation pathways can be evaluated by measuring the expression of metabolic genes. The prodrug conversion can be confirmed by measuring Dagrocorat levels in cell lysates or medium.
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| Animal Protocol |
In vivo animal experiments with Fosdagrocorat are conducted using rodent models of inflammatory diseases. Fosdagrocorat is administered orally at various doses due to its oral bioavailability. Pharmacokinetic studies may be conducted to assess the conversion of Fosdagrocorat to Dagrocorat and the exposure of the active metabolite. Inflammatory endpoints are measured to assess the compound's anti-inflammatory efficacy. The compound's effects on metabolic parameters are also assessed to evaluate its dissociated profile. At study endpoint, tissues are harvested for analysis of glucocorticoid receptor target gene expression and inflammatory markers. The compound's anti-inflammatory efficacy and side effect profile are compared to traditional glucocorticoids.
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| ADME/Pharmacokinetics |
Pharmacokinetics and food-effect studies of Fosdagrocorat have been conducted. Fosdagrocorat has a molecular weight of 574.53 and a chemical formula of C29H30F3N2O5P. The compound is orally available. For in vivo administration, the compound is typically formulated using appropriate vehicles to ensure adequate solubility and stability. The compound should be stored under conditions recommended by the manufacturer to maintain stability and prevent degradation. Detailed PK parameters including half-life, clearance, volume of distribution, and maximum concentration (Cmax) are available in the primary literature and should be consulted for specific experimental planning. Pharmacokinetics and food-effect studies of Fosdagrocorat have been reported.
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| Toxicity/Toxicokinetics |
Comprehensive toxicological data for Fosdagrocorat are not extensively documented in publicly available sources. As a research-grade compound, Fosdagrocorat is intended for laboratory research purposes only and is not approved for human therapeutic use. Standard laboratory safety practices should be followed when handling this compound, including the use of appropriate personal protective equipment and working in a well-ventilated area. The compound should be stored according to the manufacturer's recommendations to maintain stability and prevent degradation. The compound's dissociated glucocorticoid receptor agonist profile suggests it may have a more favorable side effect profile than traditional glucocorticoids. Comprehensive toxicological profiling is not available from the current search results and would require consultation of the primary literature or safety data sheets.
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| References |
Clin Pharmacol Drug Dev.2018 Mar;7(3):244-255.
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| Additional Infomation |
Fosdagrocorat has been used in research on the treatment of rheumatoid arthritis and in basic scientific trials.
Fosdagrocorat is a research compound developed for studying the role of the glucocorticoid receptor in inflammation and for evaluating dissociated glucocorticoid receptor agonists as therapeutic agents for inflammatory diseases. The compound is also known as PF-04171327. Fosdagrocorat is a prodrug of Dagrocorat, a selective glucocorticoid receptor modulator that exhibits anti-inflammatory effects while minimizing the side effects associated with traditional glucocorticoids. The compound's prodrug design may offer advantages in terms of oral bioavailability or tissue-specific delivery. Fosdagrocorat is not currently in clinical trials nor approved for therapeutic use; it remains an investigational tool compound for preclinical research. Fosdagrocorat is available from various chemical suppliers for research purposes. |
| Molecular Formula |
C29H30F3N2O5P
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| Molecular Weight |
574.527879238129
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| Exact Mass |
574.184
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| CAS # |
1044535-58-1
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| Related CAS # |
1044535-52-5 (Dagrocorat)
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| PubChem CID |
24872952
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| Appearance |
White to off-white solid powder
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| LogP |
6.352
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
40
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| Complexity |
956
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| Defined Atom Stereocenter Count |
3
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| SMILES |
CC1=C(C=CC=N1)NC(=O)C2=CC3=C(C=C2)[C@@]4(CC[C@@](C[C@H]4CC3)(C(F)(F)F)OP(=O)(O)O)CC5=CC=CC=C5
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| InChi Key |
BVXLAHSJXXSWFF-KEKPKEOLSA-N
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| InChi Code |
InChI=1S/C29H30F3N2O5P/c1-19-25(8-5-15-33-19)34-26(35)22-10-12-24-21(16-22)9-11-23-18-28(29(30,31)32,39-40(36,37)38)14-13-27(23,24)17-20-6-3-2-4-7-20/h2-8,10,12,15-16,23H,9,11,13-14,17-18H2,1H3,(H,34,35)(H2,36,37,38)/t23-,27+,28-/m1/s1
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| Chemical Name |
(2R,4aS,10aR)-4a-benzyl-7-((2-methylpyridin-3-yl)carbamoyl)-2-(trifluoromethyl)-1,2,3,4,4a,9,10,10a-octahydrophenanthren-2-yl dihydrogen phosphate
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| Synonyms |
PF-04171327; PF04171327; PF 04171327; PF-4171327; PF4171327; PF 4171327
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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 : ~125 mg/mL (~217.57 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.62 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 20.8 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: ≥ 2.08 mg/mL (3.62 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7406 mL | 8.7028 mL | 17.4055 mL | |
| 5 mM | 0.3481 mL | 1.7406 mL | 3.4811 mL | |
| 10 mM | 0.1741 mL | 0.8703 mL | 1.7406 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.
 Clin Pharmacol Drug Dev.2018 Mar;7(3):244-255. |
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 Reversible inhibition of CYP3A activity in pooled human liver microsomes by PF‐00251802 (dagrocorat), using midazolam as a probe substrate.Clin Pharmacol Drug Dev.2018 Mar;7(3):244-255. |
 Mean plasma concentration–time profile for midazolam ± PF‐04171327 (fosdagrocorat).
Time‐dependent inhibition of CYP3A activity in pooled human liver microsomes by (A) PF‐00251802 (dagrocorat) and (B) PF‐04015475, using midazolam as a probe substrate. |
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