1. Metabolic Enzyme/Protease
  2. Elastase
  3. SSR69071

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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SSR69071 Chemical Structure

SSR69071 Chemical Structure

CAS No. : 344930-95-6

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Based on 1 publication(s) in Google Scholar

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Description

SSR69071 is a potent, orally active and selective inhibitor of neutrophil elastase. SSR69071 reduces myocardial infarct size following ischemia-reperfusion injury[1]. 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[2].

In Vitro

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.

In Vivo

SSR69071 (3 mg/kg i.v.) reduces cardiac infarct size when administered before ischemia or just prior to reperfusion[1].

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.

Animal Model: Male New Zealand white rabbits weighing 2-3 kg[1]
Dosage: 3 mg/kg (dissolved in methane sulphonic acid before being diluted in 0.9% saline)
Administration: Administered i.v.
Result: Treatment just prior to reperfusion significantly reduced cardiac elastase activity.
Molecular Weight

556.63

Formula

C27H32N4O7S

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C1C=C(OCN(C(C2=C3C=C(OC)C=C2C(C)C)=O)S3(=O)=O)N=C4N1C=CC=C4OCCN5CCCCC5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7965 mL 8.9826 mL 17.9653 mL
5 mM 0.3593 mL 1.7965 mL 3.5931 mL
View the 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.

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Working solution concentration: mg/mL
Purity & Documentation

Purity: ≥98.0%

References

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
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SSR69071 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
SSR69071
Cat. No.:
HY-103445
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