Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C17H31NO12 |
| Molecular Weight | 441.4275 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 13 / 13 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
C[C@H]1O[C@@H](O[C@@H]2[C@@H](CO)O[C@H](O[C@H]3[C@H](O)CN[C@@H]3CO)[C@H](O)[C@H]2O)[C@H](O)[C@@H](O)[C@@H]1O
InChI
InChIKey=WLDBVPWSCOUGQI-ZMMVPWHFSA-N
InChI=1S/C17H31NO12/c1-5-9(22)10(23)12(25)16(27-5)30-15-8(4-20)28-17(13(26)11(15)24)29-14-6(3-19)18-2-7(14)21/h5-26H,2-4H2,1H3/t5-,6-,7-,8-,9-,10+,11-,12-,13-,14-,15-,16+,17-/m1/s1
| Molecular Formula | C17H31NO12 |
| Molecular Weight | 441.4275 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 13 / 13 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
Approval Year
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 11:32:09 GMT 2023
by
admin
on
Sat Dec 16 11:32:09 GMT 2023
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| Record UNII |
P6XAY84W8G
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| Record Status |
Validated (UNII)
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| Record Version |
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9846130
Created by
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736967-62-7
Created by
admin on Sat Dec 16 11:32:09 GMT 2023 , Edited by admin on Sat Dec 16 11:32:09 GMT 2023
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P6XAY84W8G
Created by
admin on Sat Dec 16 11:32:09 GMT 2023 , Edited by admin on Sat Dec 16 11:32:09 GMT 2023
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PRIMARY |
| Related Record | Type | Details | ||
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ACTIVE MOIETY |
A concentration-dependent and saturable plasma protein binding of CS-1036 was observed in rats and monkeys with the dissociation rate constant (KD) of 8.95 and 27.2 nM, and maximal binding capacity (Bmax) of 52.8 and 22.1 nM, respectively. By the assessments of the recombinant amylase and
immunoprecipitation, the major binding protein of CS-1036 in rats was identified as salivary amylase (KD 5.64 nM). CS-1036 also showed concentration-dependent and saturable binding to human
salivary and pancreatic amylase, with similar binding affinity in rats.
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ACTIVE MOIETY |
Originator: Daiichi Sankyo Company; Class: Anti-hyperglycaemic; Highest Development Phase: Discontinued for Diabetes mellitus; Most Recent Events: 26 May 2011 Discontinued - Phase-II for Diabetes mellitus in Asia (PO), 26 May 2011 Discontinued - Phase-II for Diabetes mellitus in Japan (PO), 21 May 2010 Phase-II clinical trials in Diabetes mellitus in Asia (PO)
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ACTIVE MOIETY |
(2R,3R,4R)-4-hydroxy-2-(hydroxymethyl)pyrrolidin-3-yl 4-O-(6-deoxy-.BETA.-D-glucopyranosyl)-.ALPHA.-D-glucopyranoside (CS-1036), which is an .ALPHA.-amylase inhibitor, exhibited biphasic and sustained elimination with a long t1/2 (18.4-30.0 hours) in rats and monkeys, but exhibited a short t1/2 (3.7-7.9 hours) in humans. To clarify the species differences in the t1/2, the plasma protein binding of CS-1036 was evaluated by ultrafiltration. A concentration-dependent and saturable plasma protein binding of CS-1036 was observed in rats and monkeys with the dissociation rate constant (KD) of 8.95 and 27.2 nM, and maximal binding capacity (Bmax) of 52.8 and 22.1 nM, respectively.
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