RP 59794
RP 59794 is a potent collagenase (collagenase) and broad-spectrum matrix metalloproteinase (MMP) inhibitor. The active stereoisomer of RP 59794 has a Ki of 13 nM against MMP-1 (with native collagen as substrate) and 45 nM (with a synthetic octapeptide as substrate). RP 59794 blocks and partially dissociates TIMP by binding to the active site of collagenase, specifically inhibits the collagen-transmigrating migration of osteoclasts and bone resorption on collagen-coated surfaces, but exerts no effect on cell migration in collagen-free environments, and acts in a time-dependent manner in bone tissues. RP 59794 can be used in studies of arthritis, periodontal disease, corneal ulcers and tumor invasion.
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- CAS No.: 132259-06-4
- Formule: C20H31N3O4
- Masse moléculaire:377.48
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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MMP-1 13 nM (Ki, with native collagen as substrate) |
MMP-1 45 nM (Ki, with a synthetic octapeptide as substrate) |
RP 59794 form A (18 h) potently inhibits purified porcine synovial cell collagenase (using [14C]-collagen as substrate) with a Ki of 13 nM, and exhibits 500-fold higher activity than form B[1].
RP 59794 Form A inhibits purified porcine synovial cell collagenase (using a synthetic octapeptide substrate) with a Ki value of 45 nM, while Form B is approximately 67-fold less potent[1].
Crystal form RP 59794 A exhibits selective inhibitory activity against porcine synovial cell collagenase compared with other metalloproteinases; in contrast, crystal form RP 59794 B potently inhibits neprilysin (Ki ~10 nM) with low activity against collagenase[1].
RP 59794 (5 min) stereoselectively inhibits the formation of TIMP-collagenase complexes. Among its stereoisomers, form A completely blocks complex formation at a concentration of 10-3 M, which is consistent with the stereoselectivity of its collagenase inhibition[1].
RP 59794 (0.001 M; 3 h) at a 1000-fold molar excess can partially dissociate preformed TIMP-collagenase complexes, achieving a dissociation rate of 20%-30% at 36°C[1].
RP 59794 (0.1-10 μM; overnight) inhibits resorption pit formation by non-separated rabbit osteocytes in a dose-dependent manner on collagen-coated, but not uncoated, dentine slices[2].
RP 59794 (10 μM; overnight) inhibits the formation of bone resorption lacunae by purified rabbit osteoclasts on collagen-coated dentine slices (but fails to exert this effect on uncoated dentine slices)[2].
RP 59794 (0.1-10 μM; overnight) dose-dependently inhibits the invasive ability of purified rabbit osteoclasts through collagen-coated membranes (but exerts no such effect on uncoated membranes)[2].
RP 59794 (25 μM; 4-24 h) induces extensive demineralized but undigested bone matrix within osteoclast resorption lacunae in mouse calvarial explants, with its maximal effect observed at 16-24 h[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Purified rabbit osteoclasts
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Concentration:0.1, 1 and 10 μM
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Incubation Time:overnight
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Result:Dose-dependently inhibited the invasive ability of purified rabbit osteoclasts through collagen-coated membranes (but showed no such effect on uncoated membranes), with significant inhibition observed at 1 μM and 10 μM.
Chemical Information
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CAS No. 132259-06-4
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Masse moléculaire 377.48
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Formule C20H31N3O4
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SMILES
O=C(NCC1=CC=CC=C1)[C@@H](C(C)C)NC([C@@H](CC(C)C)CC(NO)=O)=O
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Structure Classification
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Initial Source
Cladosporium cladosporioide
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Lelièvre Y, et al. Low molecular weight, sequence based, collagenase inhibitors selectively block the interaction between collagenase and TIMP (tissue inhibitor of metalloproteinases). Matrix (Stuttgart, Germany). 1990 Oct;10(5):292-9. [Content Brief]
[2]. Sato T, et al. The migration of purified osteoclasts through collagen is inhibited by matrix metalloproteinase inhibitors. Journal of bone and mineral research : the official journal of the American Society for Bone and Mineral Research. 1998 Jan;13(1):59-66. [Content Brief]
[3]. Everts V, et al. Cysteine proteinases and matrix metalloproteinases play distinct roles in the subosteoclastic resorption zone. Journal of bone and mineral research : the official journal of the American Society for Bone and Mineral Research. 1998 Sep;13(9):1420-30. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
RP 59794 Related Classifications
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