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Ac-Tyr-Val-Ala-Asp-aldehyde (pseudo acid)

Names

[ CAS No. ]:
143313-51-3

[ Name ]:
Ac-Tyr-Val-Ala-Asp-aldehyde (pseudo acid)

[Synonym ]:
pase inhibitor i
acetyl-yvad-aldehyde
ice inhibitor
ac-yvad-aldehyde
N-Acetyl-L-tyrosyl-L-valyl-N-[(2S)-1-carboxy-3-oxopropan-2-yl]-L-alaninamide
L-Alaninamide, N-acetyl-L-tyrosyl-L-valyl-N-((1S)-2-carboxy-1-formylethyl)-
tyr-val-ala-asp-cho
N-Acetyl-L-tyrosyl-L-valyl-N-[(2S)-1-carboxy-3-oxo-2-propanyl]-L-alaninamide
yvad-cho
L-Alaninamide, N-acetyl-L-tyrosyl-L-valyl-N-[(1S)-2-carboxy-1-formylethyl]-
ice inhibitor i

Biological Activity

[Description]:

Ac-YVAD-CHO (L-709049) is a potent, reversible, specific tetrapeptide interleukin-lβ converting enzyme (ICE) inhibitor with mouse and human Ki values of 3.0 and 0.76 nM. Ac-YVAD-CHO can suppress the production of mature IL-lβ[1].

[Related Catalog]:

Signaling Pathways >> Immunology/Inflammation >> Interleukin Related
Research Areas >> Inflammation/Immunology

[Target]

IL-1β:3 nM (Ki)

IL-1β:0.76 nM (Ki)


[In Vitro]

Ac-YVAD-CHO inhibits IL-1β in a dose-dependent manner, with mouse and human IC50 values of 2.5 and 0.7 μM. Ac-YVAD-CHO (0.01~100 μM) reduces the elevations of IL-lβ in the plasma and peritoneal fluid treated with LPS in a dose-related manner[1].

[In Vivo]

Ac-YVAD-CHO (10 mg/kg; i.p.; 1 hour) is absorbed from the peritoneal cavity, as well as cleared from the blood rapidly[1]. Ac-YVAD-CHO (50 mg/kg; i.p.; 1 hour) drops precipitously to approximately 1 and 0.2 μM at 30 and 60 minutes after injection[1]. Ac-YVAD-CHO (30 mg/kg; i.p.; 6 hours) suppresses IL-1β levels[1]. Animal Model: CD1 female mice Dosage: 10 mg/kg (Pharmacokinetic Analysis) Administration: I.p.; 1 hour Result: Absorbed from the peritoneal cavity, as well as cleared from the blood rapidly. Animal Model: CD1 female mice Dosage: 50 mg/kg (Pharmacokinetic Analysis) Administration: I.p.; 1 hour Result: Dropped precipitously to approximately 1 and 0.2 μM at 30 and 60 minutes after injection. Animal Model: P. acnes-sensitized mice Dosage: 30 mg/kg Administration: I.p.; 6 hours Result: Suppressed IL-1β levels.

[References]

[1]. Fletcher DS, et al. A synthetic inhibitor of interleukin-1 beta converting enzyme prevents endotoxin-induced interleukin-1 beta production in vitro and in vivo. J Interferon Cytokine Res. 1995;15(3):243-248.

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
937.7±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C23H32N4O8

[ Molecular Weight ]:
492.522

[ Flash Point ]:
520.9±34.3 °C

[ Exact Mass ]:
492.222015

[ PSA ]:
191.00000

[ LogP ]:
0.79

[ Vapour Pressure ]:
0.0±0.3 mmHg at 25°C

[ Index of Refraction ]:
1.552

[ Storage condition ]:
−20°C

Safety Information

[ WGK Germany ]:
3


Related Compounds