SSR69071
Based on 1 Customer Validation
SSR69071 is a potent, orally active and selective inhibitor of neutrophil elastase. SSR69071 reduces myocardial infarct size following ischemia-reperfusion injury. SSR69071 displays a higher affinity for human elastase (Ki=0.0168 nM) than for rat (Ki=3 nM), mouse (Ki=1.8 nM), and rabbit (Ki= 58 nM) elastases.
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- Pureté: 98.4%
- CAS No.: 344930-95-6
- Formule: C27H32N4O7S
- Masse moléculaire:556.63
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Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Metabolism/Protease Compound Library
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Anti-Cardiovascular Disease Compound Library
HY-L046
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Orally Active Compound Library
HY-L061
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Heterocyclic Compound Library
HY-L138
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Protease Inhibitor Library
HY-L147
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Highly Selective Inhibitors Library
HY-L158
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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High-Throughput Bioactive Compound Library
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RNA Binding Bioactive Compound Library
HY-L248
Activité biologique
SSR69071 is a potent inhibitor of human leukocyte elastase (HLE), with the inhibition constant (Ki) and the constant for inactivation process (kon) being 0.0168±0.0014 nM and 0.183±0.013 106/mol sr, respectively[2].
SSR69071 is a potent, competitive and slow tight binding inhibitor of HLE in vitro with a Ki value of 16.8 pM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Treatment with SSR69071 (3 mg/kg i.v.) just prior to reperfusion significantly reduces cardiac elastase activity[1].
Bronchoalveolar lavage fluid from mice orally treated with SSR69071 inhibits HLE (ex vivo), and in this model, SSR69071 has a dose-dependent efficacy with an ED50=10.5 mg/kg p.o. SSR69071 decreases significantly the acute lung hemorrhage induced by HLE (ED50=2.8 mg/kg p.o.) in mice[2]. SSR69071 prevents carrageenan- (ED30=2.2 mg/kg) and HLE-induced (ED30=2.7 mg/kg) paw edema in rats after p.o. administration[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male New Zealand white rabbits weighing 2-3 kg[1]
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Dosage:3 mg/kg (dissolved in methane sulphonic acid before being diluted in 0.9% saline)
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Administration:Administered i.v.
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Result:Treatment just prior to reperfusion significantly reduced cardiac elastase activity.
Chemical Information
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CAS No. 344930-95-6
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Appearance Solid
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Masse moléculaire 556.63
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Formule C27H32N4O7S
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Color Off-white to light yellow
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SMILES
O=C1C=C(OCN(C(C2=C3C=C(OC)C=C2C(C)C)=O)S3(=O)=O)N=C4N1C=CC=C4OCCN5CCCCC5
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 52 mg/mL (93.42 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (275 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Jean-Pierre Bidouard, et al. SSR69071, an elastase inhibitor, reduces myocardial infarct size following ischemia-reperfusion injury. Eur J Pharmacol. 2003 Feb 7;461(1):49-52. [Content Brief]
[2]. Zoltan Kapui, et al. Biochemical and pharmacological characterization of 2-(9-(2-piperidinoethoxy)-4-oxo-4H-pyrido[1,2-a]pyrimidin-2-yloxymethyl)-4-(1-methylethyl)-6-methoxy-1,2-benzisothiazol-3(2H)-one-1,1-dioxide (SSR69071), a novel, orally active elast [Content Brief]
[3]. Márton Varga, et al. A novel orally active inhibitor of HLE. Eur J Med Chem. 2003 Apr;38(4):421-5. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7965 mL | 8.9826 mL | 17.9653 mL | 44.9131 mL |
| 5 mM | 0.3593 mL | 1.7965 mL | 3.5931 mL | 8.9826 mL | |
| 10 mM | 0.1797 mL | 0.8983 mL | 1.7965 mL | 4.4913 mL | |
| 15 mM | 0.1198 mL | 0.5988 mL | 1.1977 mL | 2.9942 mL | |
| 20 mM | 0.0898 mL | 0.4491 mL | 0.8983 mL | 2.2457 mL | |
| 25 mM | 0.0719 mL | 0.3593 mL | 0.7186 mL | 1.7965 mL | |
| 30 mM | 0.0599 mL | 0.2994 mL | 0.5988 mL | 1.4971 mL | |
| 40 mM | 0.0449 mL | 0.2246 mL | 0.4491 mL | 1.1228 mL | |
| 50 mM | 0.0359 mL | 0.1797 mL | 0.3593 mL | 0.8983 mL | |
| 60 mM | 0.0299 mL | 0.1497 mL | 0.2994 mL | 0.7486 mL | |
| 80 mM | 0.0225 mL | 0.1123 mL | 0.2246 mL | 0.5614 mL |
SSR69071 Related Classifications
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