C5347-10mg | Calpain Inhibitor XII [181769-57-3] Clinisciences

Background

Ki: 19 nM for μ-calpain

Calpain Inhibitor XII is a reversible and selective inhibitor of calpain I.

Calpain is a protein belonging to the family of calcium-dependent, non-lysosomal cysteine proteases expressed ubiquitously in mammals and many other organisms. Calpain inhibitors have been used to study the role of calpains in diverse processes, including neutrophil chemotaxis, neuronal signaling, and cardiac response to injury.

In vitro: A series of new dipeptidyl alpha-keto amides of the general structure R1-L-Leu-D,L-AA-CONH-R2 including Calpain Inhibitor XII were synthesized and evaluated as inhibitors for the cysteine proteases calpain I, calpain II, and cathepsin B. Calpain II was more sensitive to these inhibitors Calpain Inhibitor XII than calpain I. Calpain I was also effectively inhibited by Calpain Inhibitor XII, but lower Ki values than with calpain II. Cathepsin B was weakly inhibited by Calpain Inhibitor XII. The best calpain I inhibitor in this study was Calpain Inhibitor XII with Ki value of 19 nM [1].

In vivo: Up to now, there is no animal in vivo data reported.

Clinical trial: So far, no clinical study has been conducted.

Reference:
[1] Li, Z. ,Ortega-Vilain, A.C.,Patil, G.S., et al. Novel peptidyl α-keto amide inhibitors of calpains and other cysteine proteases. Journal of Medicinal Chemistry 39(20), 4089-4098 (1996).

Chemical Properties

Physical Appearance	A crystalline solid
Storage	Store at -20°C
M.Wt	482.6
Cas No.	181769-57-3
Formula	C₂₆H₃₄N₄O₅
Synonyms	Z-L-Nva-CONH-CH2-2-Py
Solubility	≤16mg/ml in ethanol;16mg/ml in DMSO;20mg/ml in dimethyl formamide
Chemical Name	[3-methyl-1-[[[1-[oxo[(2-pyridinylmethyl)amino]acetyl]butyl]amino]carbonyl]butyl]-carbamic acid, phenylmethyl ester
SDF	Download SDF
Canonical SMILES	O=C(NC(CC(C)C)C(NC(CCC)C(C(NCC1=NC=CC=C1)=O)=O)=O)OCC2=CC=CC=C2
Shipping Condition	Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips	We do not recommend long-term storage for the solution, please use it up soon.

Protocol

Cell experiment:[1]
Cell lines	Aplysia neurons
Reaction Conditions	200 μM calpain inhibitor XII
Applications	Calpain inhibitor XII inhibited voltage-gated potassium conductance and moderately reduced the sodium conductance, which consequently led to spike broadening and increased calcium influx. Such alterations of the excitable membrane properties may alter the normal patterns of neuronal and muscle electrical activities.
Note	The technical data provided above is for reference only.
	References: 1. Khoutorsky A, Spira ME. Calpain inhibitors alter the excitable membrane properties of cultured aplysia neurons. Journal of Neurophysiology, 2008, 100(5): 2784-2793.

Quality Control

Purity ≥ 90.00%

COA (Certificate Of Analysis)
MSDS (Material Safety Data Sheet)

Chemical structure

Calpain Inhibitor XII [181769-57-3]

Cat# C5347-10mg

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Brand : ApexBio Technology