Difelikefalin
CAS No. : 1024828-77-0
(Synonyms: CR-845; FE-202845)
| Size | Price | Stock |
|---|---|---|
| 5mg | $320 | In-stock |
| 10mg | $510 | In-stock |
| 25mg | $950 | In-stock |
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| Cat. No. : | HY-17609 |
| M.Wt: | 679.85 |
| Formula: | C36H53N7O6 |
| Purity: | >98 % |
| Solubility: | DMSO : 100 mg/mL (ultrasonic);H2O : ≥ 100 mg/mL |
Difelikefalin (CR-845; FE-202845) is an orally active peripherally acting kappa opioid receptor agonist. Difelikefalin reduces acute kidney injury, decreases oliguria, maintains urine flow, inhibits cytokine expression, and improves survival in endotoxemia after ischemia/reperfusion. Difelikefalin suppresses pruritus signals and exhibits neuromodulatory antipruritic activity. Difelikefalin can be used in research related to acute kidney injury, chronic kidney disease-associated pruritus, and atopic dermatitis[1][2][3].
In Vitro:Difelikefalin 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 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].
In Vivo:Difelikefalin (1 mg/kg; i.v.; continuous infusion; 2 hours) produces a transient diuretic effect without altering blood pressure or pulse rate in normal anesthetized rats[1].
Difelikefalin (0.3-1.0 mg/kg; i.v.; single injection; 1 hour pre-LPS) 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) 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) 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) improves tubular flow rate in LPS-induced septic acute kidney injury in mice, independent of renal innervation[1].
Difelikefalin 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) suppresses atopic dermatitis-associated itch in mice[3].
Difelikefalin (1.0 mg/kg; i.p.; single dose) rapidly reduces atopic dermatitis-associated scratching behavior in mice[3].
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