Propionyl-L-carnitine

Propionyl-L-carnitine is an orally active L-carnitine derivative. Propionyl-L-carnitine has a high affinity for muscle L-carnitine transferase. Propionyl-L-carnitine increases Apoptosis, Bax, and reduces NF-κB, VCAM-1, MCP-1, and survivin. Propionyl-L-carnitine activates Src kinase, Akt, induces p-AMPK and nitric oxide synthesis. Propionyl-L-carnitine alleviates cardiovascular disease, obesity, and colitis^{[1][2][3][4][5][6][7][8][9][10]}. IC50 & Target:IC50: muscular carnitine transferase^[1] In Vitro: Propionyl-L-carnitine (0-100 μM; 0-8 h) induces eNOS activation and nitric oxide synthesis in endothelial cells HAEC via PI3 and Akt kinases^[2].
Propionyl-L-carnitine (100 μM; 6-24 h) induces IκB-α mRNA, and inhibits p65 and p50 in intimal cells^[3].
In Vivo: Propionyl-L-carnitine (120 mg/kg; p.o.; daily; starting immediately after aortic injury and lasting for 15 days) reduces the relative aortic intimal volume, increases apoptosis, up-regulates Bax without changing the Bcl-2 level, and reduces NF-κB, VCAM-1, MCP-1, and survivin in rats^[3].
Propionyl-L-carnitine (30-120 mg/kg/day, p.o., drinking water) enhances wound healing and counteracts microvascular endothelial cell dysfunction in rats^[4].
Propionyl-L-carnitine (3.6 mg/mL, infused into the renal artery at the rate of 0.4 mL/min) prevents renal function deterioration due to ischemia/reperfusion in male Sprague-Dawley rats^[5].
Propionyl-L-carnitine (200 mg/kg/day, p.o., 4 weeks) corrects metabolic and cardiovascular alterations in diet-induced obese mice and improves liver respiratory chain activity^[6].
Propionyl-L-carnitine (25  mg/kg, intrarectal, twice daily, for 1 week; 120 mg/kg, p.o., once daily, for 1 week) reduces intestinal damage and microvascular dysfunction in rat TNBS-induced acute and reactivated colitis^[7].
Propionyl-L-carnitine (200 mg/kg, p.o., drinking water) increases NO synthesis by enhancing eNOS expression in spontaneously hypertensive rats^[8].
Propionyl-L-carnitine (500 mg/kg, i.p., 10 successive days) prevents the progression of Cisplatin (HY-17394)-induced cardiomyopathy in a carnitine-depleted rat model^[9].
Propionyl-L-carnitine (200 mg/kg per d, p.o., 20 weeks) reduces body weight and hyperinsulinaemia in obese Zucker rats^[10].