This product is for research use only, not for human use. We do not sell to patients.
| Size | Price | Stock |
|---|---|---|
| 5mg | $55 | 3-6 Days |
| 10mg | $80 | 3-6 Days |
| 25mg | $110 | 3-6 Days |
| 50mg | $160 | 3-6 Days |
| 100mg | $240 | 3-6 Days |
| 250mg | $420 | 3-6 Days |
| 500mg | $720 | 3-6 Days |
: Cat #: V2638 CAS #: 127373-66-4 Purity ≥ 98%
Description: Sivelestat (also known as ONO5046; LY544349; EI546) is a novel, potent and competitive inhibitor of human neutrophil elastase (HNE) with IC50 value of 44 nM and Ki of 200 nM; it also inhibited leukocyte elastase obtained from rabbit, rat, hamster and mouse. ONO-5046 did not inhibit trypsin, thrombin, plasmin, plasma kallikrein, pancreas kallikrein, chymotrypsin and cathepsin G even at 100 microM. In in vivo studies, ONO-5046 suppressed lung hemorrhage in hamster by intratracheal administration and increase of skin capillary permeability in guinea pig by intravenous administration. It is used in the treatment of acute respiratory failure. Preliminary studies show Sivelestat may also improve neuropathic pain.
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| Molecular Weight (MW) | 434.46 |
|---|---|
| Molecular Formula | C20H22N2O7S |
| CAS No. | 127373-66-4 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 86 mg/mL (197.9 mM) |
| Water: <1 mg/mL | |
| Ethanol: 86 mg/mL (197.9 mM) | |
| Solubility In Vivo | 5% DMSO+40% PEG 300+5% Tween 80+ddH2O: 23mg/mL |
| Synonyms | ONO5046, LY544349, EI546; ONO 5046; ONO5046; ONO-5046; LY544349; LY-544349; LY 544349; EI 546 sodium salt hydrate, Elaspol sodium salt hydrate, LY 544349 sodium salt hydrate, Trade name: Elaspol. |
| Protocol | In Vitro | In vitro activity: Sivelestat suppresses both adhesion and transmigration of neutrophils to the endothelium Kinase Assay: Sivelestat(ONO5046; LY544349; EI546) is a competitive inhibitor of human neutrophil elastase(IC50 = 44 nM; Ki=200 nM); also inhibited leukocyte elastase obtained from rabbit, rat, hamster and mouse. Cell Assay: HUVEC are grown to confluence on fibronectin (25 μg/mL) coated Falcon cell culture inserts. Neutrophils stimulated by PAF (0.1 mM) are added to the HUVEC monolayers (upper chamber). The upper chamber is exposed to 2 mL of HUMEDIA and rehydrated at 37 ℃ for 1 h in the absence or the presence (50 μg/mL) of sivelestat. Subsequently, the upper chamber is removed and the fluid in the lower chamber is collected. |
|---|---|---|
| In Vivo | Intraoperative administration of sivelestat effectively reduced neutrophil induction and activation in the lung and improved oxygenation after cardiopulmonary bypass in a piglet model.By inhibiting neutrophil elastase, sivelestat has a direct action to the accumulated and activated leucocytes, offering efficient protection against the production of oxygen radicals and cytokines. | |
| Animal model | Neonatal piglets |
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.3017 mL | 11.5085 mL | 23.0171 mL | 46.0342 mL |
| 5mM | 0.4603 mL | 2.3017 mL | 4.6034 mL | 9.2068 mL |
| 10mM | 0.2302 mL | 1.1509 mL | 2.3017 mL | 4.6034 mL |
| 20mM | 0.1151 mL | 0.5754 mL | 1.1509 mL | 2.3017 mL |
This equation is commonly abbreviated as: C1 V1 = C2 V2
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.