p-APMSF hydrochloride
Based on 1 Customer Validation
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.
For research use only. We do not sell to patients.
- Purity: 95.0%
- CAS No.: 74938-88-8
- Formula: C8H10ClFN2O2S
- Molecular Weight:252.69
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Storage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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; 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.
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Animal Model:Sprague-Dawley Rat (SD) (male, 8 weeks old, 250-300 g)[2]
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Dosage:10 mM
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Administration:intratracheal; single coadministered dose
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Result:Increased plasma rhG-CSF concentration about 3-fold, from 3.9 to 11.7 ng/mL, at 30 minutes post-administration.
Increased AUC0-8 of rhG-CSF by more than 1.5-fold compared to intratracheal control.
When combined with Laureth-9, increased plasma rhG-CSF concentration at 30 minutes post-administration about 123-fold to 481.5 ng/mL.
Achieved a relative bioavailability of rhG-CSF of 73.6% versus intravenous administration and 172.8% versus subcutaneous administration.
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Animal Model:Sprague-Dawley Rat (SD) (male, 8 weeks old, 250-300 g)[3]
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Dosage:10 mM (in combination with rhG-CSF at 100 μg/kg)
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Administration:intranasal
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Result:Did not produce a significant increase in the AUC for the increase ratio of total leukocyte numbers compared to rhG-CSF administered alone.
Did not significantly increase plasma rhG-CSF concentrations relative to rhG-CSF administered alone.
Chemical Information
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CAS No. 74938-88-8
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Appearance Solid
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Molecular Weight 252.69
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Formula C8H10ClFN2O2S
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Color White to off-white
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SMILES
O=S(CC1=CC=C(C(N)=N)C=C1)(F)=O.[H]Cl
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Synonyms
p-Amidinophenylmethylsulfonylfluoride hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Purity & Documentation
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Data Sheet (273 KB)
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SDS (476 KB)
- English - EN (476 KB)
- Français - FR (476 KB)
- Deutsch - DE (476 KB)
- Norwegian - NO (476 KB)
- Español - ES (476 KB)
- Swedish - SV (476 KB)
- Italian - IT (476 KB)
- Korean - KR (476 KB)
- Portuguese - PT (476 KB)
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Handling Instructions (2659 KB)
References
[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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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