| Stereochemistry | ABSOLUTE |
| Molecular Formula | C15H23NO4 |
| Molecular Weight | 281.3474 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 5 / 5 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
[H][C@@]1(C[C@@H](CC(N)=O)CC(=O)O1)[C@]2([H])C[C@@H](C)C[C@H](C)C2=O
InChI
InChIKey=SAVFIMRLAWCZGX-UHFZAUJKSA-N
InChI=1S/C15H23NO4/c1-8-3-9(2)15(19)11(4-8)12-5-10(6-13(16)17)7-14(18)20-12/h8-12H,3-7H2,1-2H3,(H2,16,17)/t8-,9-,10-,11-,12+/m0/s1
A bone resorption inhibitor, A-75943, isolated from the fermentation broth of Streptomyces sp. SANK 61296, was found to be structurally related to cycloheximide, from which A-75943 was prepared chemically.
A-75943 inhibited in vitro bone resorption in a concentration-dependent manner, with maximal nontoxic inhibition greater than 90% at 5ug/ml and an
IC50 of 0.35uM.
Approval Year
PubMed
Sample Use Guides
Rat accelerated bone resorption model: Among three Ro-136298-treated groups, two groups received a concomitant daily subcutaneous administration of A-75943 (3 and 30mg/kg), and the remaining group received vehicle from the 4th to the 10th day following TPTX.
Route of Administration:
Other
A-75943 inhibited in vitro bone resorption in a concentration-dependent manner, with maximal nontoxic inhibition greater than 90% at 5 ug/ml and an
IC50 of 0.35 uM. At higher concentrations, A-75943 exhibited cytotoxicity and significantly decreased the survival of osteoclasts on bone slices; but at lower
concentrations it did not affect the survival or morphology of osteoclasts.
ACTIVE MOIETY
