| Identification | Back Directory | [Name]
APSTATIN TRIFLUOROACETATE SALT | [CAS]
160470-73-5 | [Synonyms]
Apstatin (HPLC)
Apstatin, 95% (HPLC)
APSTATIN HYDROCHLORIDE
APSTATIN TRIFLUOROACETATE SALT
N-(2S,3R)-AHPBA-Pro-Pro-Ala-NH2
N-((2S,3R)-3-Amino-2-hydroxy-4-phenylbutanoyl)-Pro-Pro-Ala-NH2
N-[(2S,3R)-3-Amino-2-hydroxy-4-phenylbutanoyl]-L-prolyl-L-prolyl-L-alaninamide
L-Alaninamide, 1-[(2S,3R)-3-amino-2-hydroxy-1-oxo-4-phenylbutyl]-L-prolyl-L-prolyl- | [Molecular Formula]
C23H33N5O5 | [MDL Number]
MFCD01310909 | [MOL File]
160470-73-5.mol | [Molecular Weight]
459.54 |
| Chemical Properties | Back Directory | [Boiling point ]
864.3±65.0 °C(Predicted) | [density ]
1.320±0.06 g/cm3(Predicted) | [storage temp. ]
−20°C | [form ]
Solid. | [pka]
11.26±0.45(Predicted) |
| Hazard Information | Back Directory | [Uses]
Apstatin is a potent aminopeptidase P (APP) inhibitor with Ki values of 2.6, 0.64 μM for rat and human APP, respectively. Apstatin shows cardioprotection[1][2]. | [in vivo]
Apstatin (1 mg/kg; i.v.; 5?min before ischaemia) reduces myocardial infarct size (IS) in acute myocardial ischaemia model[1]. | Animal Model: | 270-310 g, Male Wistar rats[1] | | Dosage: | 1 mg/kg | | Administration: | I.v.; 5?min before ischaemia | | Result: | Significantly reduced infarct size (IS) in acute myocardial ischaemia. |
| [References]
[1] Wolfrum S, et al. Apstatin, a selective inhibitor of aminopeptidase P, reduces myocardial infarct size by a kinin-dependent pathway. Br J Pharmacol. 2001 Sep;134(2):370-4. DOI:10.1038/sj.bjp.0704236
[2] Maggiora LL, et al. Apstatin analogue inhibitors of aminopeptidase P, a bradykinin-degrading enzyme. J Med Chem. 1999 Jul 1;42(13):2394-402. DOI:10.1021/jm9805642 |
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