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  • 产品名称:Q-VD-OPh(GeneralCaspaseInhibitor)

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  • 产品厂商:KamiyaBiomedical
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简单介绍:
Q-VD-OPh(GeneralCaspaseInhibitor)
详情介绍:
Purpose Irreversible calpain I, II / Cathepsin L inhibitor 
Sequence Quinolyl-Val-Asp-OPh
Purity > 95 %
Chemical Name (3S)-5-(2,6-Difluorophenoxy)-3-[[(2S)-3-methyl-1-oxo-2-[(2-quinolinylcarbonyl)amino]butyl]amino]-4-oxo-pentanoic acid hydrate
Formula C26H25F2N3O6 · xH2O
Solubility DMSO
Molecular Weight 513 Da
Comment

The novel Q-VD-OPH (Quinoline-Val-Asp-CH2-OPh) compound is an irreversible caspase inhibitor specifically designed for animal in vivo research. The Q-VD-OPH irreversibly binds to activated caspases to block apoptosis. Q-VD-OPH penetrates the bloodbrain barrier. The “OPH” trap with its superior potency, proven cell permeability and minimal toxicity provides an exceptional alternative to the fluoromethyl ketone family of inhibitors. The improvements derive from significant changes in structural design and replacement of the putatively toxic fluoromethyl ketone (FMK) with the non-toxic 2,6-difluorophenoxy (OPH) group. The mechanism of action involves the formation of an irreversible thioether bond between the aspartic acid derivative in the inhibitor and the active site cysteine of the caspase with the displacement of the 2,6-difluorophenoxy leaving group.
The “OPH” trap features:
- Non-toxic: A preliminary study showed no evidence of toxicity in mice injected with >1,000 mg/kg
- Potency: IC50 values against purified caspases are in the nanomolar range, over 90% inhibition of apoptosis when used in an in vitro cell-based assay
Prepare desired concentrated stocks solutions as follows: For each mg of Q-VD-OPH
20 mM - add 97 µL DMSO.
10 mM - add 194 µL DMSO.
5 mM - add 388 µL DMSO.

Restrictions For Research Use only
Format Solid
Reconstitution Soluble in DMSO (stock solutions in DMSO up to 200 mg/mL may be prepared). For solubility in water at concentrations above 1 mg/mL, 80% DMSO is suggested. Solubility may be improved in the presence of carrier proteins such as albumin or whole serum. A concentration of 0.5 mg/mL in serum has been shown to be obtained by direct dilution (1:400) of DMSO stock solution of 200 mg/mL Q-VD- OPH.
Storage -20 °C