Difelikefalin acetate
Based on 1 publication(s) in Google Scholar
Difelikefalin acetate (CR-845 acetate; FE-202845 acetate) is an orally active peripherally acting kappa opioid receptor agonist. Difelikefalin acetate reduces acute kidney injury, decreases oliguria, maintains urine flow, inhibits cytokine expression, and improves survival in endotoxemia after ischemia/reperfusion. Difelikefalin acetate suppresses pruritus signals and exhibits neuromodulatory antipruritic activity. Difelikefalin acetate can be used in research related to acute kidney injury, chronic kidney disease-associated pruritus, and atopic dermatitis.
For research use only. We do not sell to patients.
- Purity : 99.89%
- CAS No.: 2803411-76-7
- Formula: C38H57N7O8
- Molecular Weight:739.90
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Storage:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Difelikefalin acetate
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Biological Activity
Description
IC50 & Target
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κ Opioid Receptor/KOR |
IL-10 |
In Vitro
Difelikefalin acetate shows a non-significant trend to suppress LPS-induced increases in TNF-α, CCL3, and IL-10 mRNA expression in isolated KOR1-positive renal interstitial cells from C57Bl/6J mouse kidneys[1].
Difelikefalin acetate preferentially activates medium-to-large diameter mouse dorsal root ganglia neurons with no direct alteration of neuronal responses to pruritogens like Histamine (HY-B1204) or Chloroquine (HY-17589A)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Difelikefalin (0.3-1.0 mg/kg; i.v.; single injection; 1 hour pre-LPS) acetate improves tubular flow rate, and the 1.0 mg/kg dose preserves urine volume, in LPS-induced septic acute kidney injury in mice[1].
Difelikefalin (0.3-1.0 mg/kg; i.v.; single injection; 1 hour pre-CLP) acetate improves tubular flow rate in CLP-induced polymicrobial sepsis-associated acute kidney injury in mice[1].
Difelikefalin (0.3 mg/kg; i.v.; single injections; days 1-5 post-ischemia/reperfusion) acetate increases survival rate to over 80% in subsequent LPS-induced septic acute kidney injury in mice[1].
Difelikefalin (1.0 mg/kg; i.v.; single injection; 1 hour pre-LPS) acetate improves tubular flow rate in LPS-induced septic acute kidney injury in mice, independent of renal innervation[1].
Difelikefalin acetate significantly increases plasma IL-10 levels in LPS-induced septic acute kidney injury in mice[1].
Difelikefalin (0.5 mg/kg; i.p.; twice daily; 14 days) acetate suppresses atopic dermatitis-associated itch in mice[3].
Difelikefalin (1.0 mg/kg; i.p.; single dose) acetate rapidly reduces atopic dermatitis-associated scratching behavior in mice[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2803411-76-7
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Appearance Solid
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Molecular Weight 739.90
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Formula C38H57N7O8
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Color White to off-white
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SMILES
CC(O)=O.O=C(C1(N)CCN(C([C@@H](CCCCN)NC([C@@H](CC(C)C)NC([C@@H](CC2=CC=CC=C2)NC([C@@H](CC3=CC=CC=C3)N)=O)=O)=O)=O)CC1)O
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Synonyms
CR-845 acetate; FE-202845 acetate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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Cell
In vivo transcriptomic, functional, circuit-based, and translational analyses of enteric neurons. [Abstract]2025 Dec 24;188(26):7547-7570.e45 PMID: 41406962
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (135.15 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (3.38 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (3.38 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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]. Sawanobori Y, et al. A kappa opioid receptor agonist, difelikefalin, improves acute kidney injury in experimental sepsis models. PloS one. 2026;21(4):e0343693. [Content Brief]
[2]. Viscusi ER, et al. Effect of difelikefalin, a selective kappa opioid receptor agonist, on respiratory depression: A randomized, double-blind, placebo-controlled trial. Clinical and translational science. 2021 Sep;14(5):1886-1893. [Content Brief]
[3]. Tamari M, et al. Difelikefalin suppresses itch and reduces scratching independent of inflammation in a murine model of atopic dermatitis. The Journal of allergy and clinical immunology. 2023 Oct;152(4):927-932. [Content Brief]
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 (sealed storage, away from moisture). 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 | 1.3515 mL | 6.7577 mL | 13.5153 mL | 33.7883 mL |
| 5 mM | 0.2703 mL | 1.3515 mL | 2.7031 mL | 6.7577 mL | |
| 10 mM | 0.1352 mL | 0.6758 mL | 1.3515 mL | 3.3788 mL | |
| 15 mM | 0.0901 mL | 0.4505 mL | 0.9010 mL | 2.2526 mL | |
| 20 mM | 0.0676 mL | 0.3379 mL | 0.6758 mL | 1.6894 mL | |
| 25 mM | 0.0541 mL | 0.2703 mL | 0.5406 mL | 1.3515 mL | |
| 30 mM | 0.0451 mL | 0.2253 mL | 0.4505 mL | 1.1263 mL | |
| 40 mM | 0.0338 mL | 0.1689 mL | 0.3379 mL | 0.8447 mL | |
| 50 mM | 0.0270 mL | 0.1352 mL | 0.2703 mL | 0.6758 mL | |
| 60 mM | 0.0225 mL | 0.1126 mL | 0.2253 mL | 0.5631 mL | |
| 80 mM | 0.0169 mL | 0.0845 mL | 0.1689 mL | 0.4224 mL | |
| 100 mM | 0.0135 mL | 0.0676 mL | 0.1352 mL | 0.3379 mL |
Difelikefalin acetate Related Classifications
HY-17609C Related Classifications
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Keywords
- Difelikefalin
- 2803411-76-7
- CR-845
- FE-202845
- CR845
- CR 845
- FE202845
- FE 202845
- Opioid Receptor
- Interleukin Related
- dorsal root ganglia neurons
- histamine
- atopic dermatitis
- renal interstitial cells
- C57Bl/6J mouse
- chloroquine
- acute kidney injury
- chronic kidney disease-associated pruritus
- central nervous system
- kappa opioid receptor
- Inhibitor
- inhibitor
- inhibit