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Cipemastat

Catalog No. T10817   CAS 190648-49-8
Synonyms: Ro 32-3555

Cipemastat is a competitive inhibitor of human collagenases 1, 2, and 3 (Kis: 3.0, 4.4, and 3.4 nM).

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Cipemastat Chemical Structure
Cipemastat, CAS 190648-49-8
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25 mg 8-10 weeks $ 1,390.00
50 mg 8-10 weeks $ 1,810.00
100 mg 8-10 weeks $ 2,750.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Cipemastat is a competitive inhibitor of human collagenases 1, 2, and 3 (Kis: 3.0, 4.4, and 3.4 nM).
Targets&IC50 stromelysins 1:527 nM (ki), collagenases 3:3.4 nM (ki), collagenases 2:4.4 nM (ki), gelatinase B:59.1 nM (ki), gelatinase A:154 nM (ki), collagenases 1:3.0 nM (ki)
In vitro Cipemastat (Ro 32-3555) is also a potent inhibitor of rat collagenase (IC50: 44.7 nM). In vitro cartilage degradation ± inhibited IL-1a induced cartilage degradation in vitro in a concentration-dependent manner (IC50: 60 nM). The inhibition is not mediated by a cytotoxic action on explant chondrocytes. Cipemastat, at all concentrations tested, fails to modify glucose utilization when compared to explants cultured in the presence of IL-La alone.
In vivo The amount of hydroxyproline in non-implanted cartilage is 119.3 nM/mg and this decreases in cartilages implanted in vehicle-dosed animals to 53.6 nM/mg over a fourteen-day period. Animals administered Cipemastat orally at doses of 2.5, 5, 10, and 25 mg/kg showed statistically increased levels of implanted cartilage hydroxyproline. Fourteen days after the second challenge injection of P. acnes, the area of cartilage most consistently affected by pannus is the lateral femoral condyle, which is the area analyzed. In arthritic animals, there is a significant decrease to a mean area of 0.086±0.01 mm2 (n=10). In non-arthritic animals, the mean cartilage area is 0.17±0.02 mm2 (n=5). The group of animals dosed with Cipemastat (50 mg/kg, p.o.) show a significantly greater area of cartilage with a mean value of 0.126±0.012 mm2 (n=9). The pannus area in vehicle-dosed animals is 0.099±0.017 mm2 and in Cipemastat dosed animals 0.102 mm2. Adjuvant arthritis injection of adjuvant-induced two phases of swelling of the injected paw in vehicle-dosed rats. The primary swelling phase occurred between days 0 to 5 and induced an increase in paw volume of 1.9±0.1 mL; the second phase occurs between days 9 to 14 and there was an increase in paw swelling of 0.98±0.08 mL. The group of animals dosed with dexamethasone (0.1 mg/kg) shows a significant reduction in both primary (0.2±0.03 mL) and secondary inflammation (0.07±0.08 mL) paw swelling as well as total inhibition of the lesion score.
Synonyms Ro 32-3555
Molecular Weight 436.55
Formula C22H36N4O5
CAS No. 190648-49-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

1. E J Lewis, et al. Ro 32-3555, an orally active collagenase inhibitor, prevents cartilage breakdown in vitro and in vivo. Br J Pharmacol. 1997 May; 121(3): 540–546.

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Keywords

Cipemastat 190648-49-8 Others Ro 32-3555 inhibitor inhibit

 

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