Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | 2C29H33ClFNO4.H2O4S |
| Molecular Weight | 1126.135 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 4 / 4 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
OS(O)(=O)=O.C[C@@H](OC[C@H](O)CNC(C)(C)CC1=CC(F)=C(Cl)C=C1)C2=C(C=CC=C2)C3=CC(C)=C(C=C3)C(O)=O.C[C@@H](OC[C@H](O)CNC(C)(C)CC4=CC(F)=C(Cl)C=C4)C5=C(C=CC=C5)C6=CC(C)=C(C=C6)C(O)=O
InChI
InChIKey=WSNVXWWLBYSQIM-DMHHVDOYSA-N
InChI=1S/2C29H33ClFNO4.H2O4S/c2*1-18-13-21(10-11-23(18)28(34)35)25-8-6-5-7-24(25)19(2)36-17-22(33)16-32-29(3,4)15-20-9-12-26(30)27(31)14-20;1-5(2,3)4/h2*5-14,19,22,32-33H,15-17H2,1-4H3,(H,34,35);(H2,1,2,3,4)/t2*19-,22-;/m11./s1
Encaleret (JTT-305 or MK-5442) is a potent oral short-acting calcium-sensing receptor (CaSR) antagonist and transiently stimulates endogenous parathyroid hormone (PTH) secretion.
CaSR antagonists stimulate endogenous PTH secretion through CaSR on the surface of parathyroid cells and thereby may be anabolic agents for osteoporosis. Japan Tobacco and Merck were developing encaleret for the treatment of osteoporosis however development has been discontinued.
Originator
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| A semimechanistic model of the time-course of release of PTH into plasma following administration of the calcilytic JTT-305/MK-5442 in humans. | 2013-08 |
|
| Pharmacodynamic responses to combined treatment regimens with the calcium sensing receptor antagonist JTT-305/MK-5442 and alendronate in osteopenic ovariectomized rats. | 2012-06 |
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| JTT-305, an orally active calcium-sensing receptor antagonist, stimulates transient parathyroid hormone release and bone formation in ovariectomized rats. | 2011-10-01 |
|
| [Antagonist for calcium-sensing receptor. JTT-305/MK-5442]. | 2011-01 |
Patents
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DTXSID40229278
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49855308
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100000175006
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T3L2G43IWK
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787584-79-6
Created by
admin on Mon Mar 31 21:11:04 GMT 2025 , Edited by admin on Mon Mar 31 21:11:04 GMT 2025
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ACTIVE MOIETY
SUBSTANCE RECORD
