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.
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- CAS No.: 2803411-76-7
- 화학식: C38H57N7O8
- 분자량:739.90
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Publications Citing Use of MedChemExpress (MCE) Difelikefalin acetate
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Biological Activity
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κ Opioid Receptor/KOR |
IL-10 |
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.
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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분자량 739.90
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화학식 C38H57N7O8
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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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
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
순도&문서
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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Difelikefalin acetate Related Classifications
HY-17609C Related Classifications
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- 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