Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C28H36N2O4 |
Molecular Weight | 464.5964 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CCOC(=O)CCC1=CC(C#N)=C(OC[C@H](O)CNC(C)(C)CC2CC3=C(C2)C=CC=C3)C=C1
InChI
InChIKey=WOOHSVAEAZCDLR-RUZDIDTESA-N
InChI=1S/C28H36N2O4/c1-4-33-27(32)12-10-20-9-11-26(24(13-20)17-29)34-19-25(31)18-30-28(2,3)16-21-14-22-7-5-6-8-23(22)15-21/h5-9,11,13,21,25,30-31H,4,10,12,14-16,18-19H2,1-3H3/t25-/m1/s1
Molecular Formula | C28H36N2O4 |
Molecular Weight | 464.5964 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
Approval Year
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 11:32:46 GMT 2023
by
admin
on
Sat Dec 16 11:32:46 GMT 2023
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Record UNII |
VQF6R9B69W
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Record Status |
Validated (UNII)
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Record Version |
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-
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351490-26-1
Created by
admin on Sat Dec 16 11:32:46 GMT 2023 , Edited by admin on Sat Dec 16 11:32:46 GMT 2023
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121596630
Created by
admin on Sat Dec 16 11:32:46 GMT 2023 , Edited by admin on Sat Dec 16 11:32:46 GMT 2023
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VQF6R9B69W
Created by
admin on Sat Dec 16 11:32:46 GMT 2023 , Edited by admin on Sat Dec 16 11:32:46 GMT 2023
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PRIMARY |
Related Record | Type | Details | ||
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METABOLITE ACTIVE -> PRODRUG |
Here we describe two novel, short-acting calcium-sensing receptor antagonists (SB-423562 and its orally bioavailable precursor, SB-423557) that elicit transient PTH release from the parathyroid gland in several preclinical species and in humans. In an ovariectomized rat model of bone loss, daily oral administration of SB-423557 promoted bone formation and improved parameters of bone strength at lumbar spine, proximal tibia and midshaft femur. Chronic administration of SB-423557 did not increase parathyroid cell proliferation in rats. In healthy human volunteers, single doses of intravenous SB-423562 and oral SB-423557 elicited transient elevations of endogenous PTH concentrations in a profile similar to that observed with subcutaneously administered PTH. Both agents were well tolerated in humans. Transient increases in serum calcium, an expected effect of increased parathyroid hormone concentrations, were observed post-dose at the higher doses of SB-423557 studied.
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