p-APMSF hydrochloride  (Synonyms: p-Amidinophenylmethylsulfonylfluoride hydrochloride)

p-APMSF (p-Amidinophenylmethylsulfonylfluoride) hydrochloride is a serine protease and trypsin inhibitor with the characteristic of rapid onset of action. p-APMSF hydrochloride reduces the enzymatic hydrolysis of recombinant human G-CSF in rat pulmonary mucosa. Combined intratracheal treatment with p-APMSF hydrochloride and Laureth-9 significantly enhances its absorption efficiency in rat lungs. Following intranasal administration, p-APMSF hydrochloride does not increase the concentration of recombinant human G-CSF in rat plasma, nor does it alter the effect of G-CSF on inducing an increase in total white blood cell count^[1][2][3].

p-APMSF (4 mg/mL; 2 h) hydrochloride effectively inhibits trypsin activity in a cell-free system after 2 hours of incubation at room temperature, enabling the isolation of α₂M-cytochrome c conjugates^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

p-APMSF hydrochloride (10 mM; intratracheal; single coadministered dose) enhances the pulmonary absorption of rhG-CSF in rats, increasing early plasma rhG-CSF concentrations 3-fold and AUC_0-8 by over 1.5-fold, and when combined with Laureth-9, increases 30-minute plasma rhG-CSF concentrations 123-fold and achieves a relative bioavailability of 73.6% versus intravenous rhG-CSF^[2].
p-APMSF hydrochloride (10 mM; intranasal) does not enhance rhG-CSF-induced increases in total leukocyte numbers or plasma rhG-CSF concentrations following intranasal co-administration in healthy rats^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

252.69

C₈H₁₀ClFN₂O₂S

74938-88-8

Solid

White to off-white

O=S(CC1=CC=C(C(N)=N)C=C1)(F)=O.[H]Cl

Room temperature in continental US; may vary elsewhere.

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

• [1]. Mitsuda S, et al. A receptor-mediated antigen delivery and incorporation system: administration of α2-macroglobulin-cytochrome c conjugate induced high concentrations of antibodies against cytochrome c in mice[J]. Biochemical and biophysical research communications, 1993, 191(3): 1326-1331.

  [2]. Machida M, et al. The effects of absorption enhancers on the pulmonary absorption of recombinant human granulocyte colony-stimulating factor (rhG-CSF) in rats. Biol Pharm Bull. 2000;23(1):84-86.

  [3]. Machida M, et al. Effects of surfactants and protease inhibitors on nasal absorption of recombinant human granulocyte colony-stimulating factor (rhG-CSF) in rats. Biol Pharm Bull. 1994;17(10):1375-1378.