Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C31H25F3N2O4 |
| Molecular Weight | 546.5364 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
COC1=CC=CC(C(=O)NC2=CC=C3CN(CCC3=C2)C(=O)OC4=CC=CC=C4)=C1C5=CC=C(C=C5)C(F)(F)F
InChI
InChIKey=AZUIUVJESCFSLJ-UHFFFAOYSA-N
InChI=1S/C31H25F3N2O4/c1-39-27-9-5-8-26(28(27)20-10-13-23(14-11-20)31(32,33)34)29(37)35-24-15-12-22-19-36(17-16-21(22)18-24)30(38)40-25-6-3-2-4-7-25/h2-15,18H,16-17,19H2,1H3,(H,35,37)
| Molecular Formula | C31H25F3N2O4 |
| Molecular Weight | 546.5364 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
Approval Year
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 01:41:13 GMT 2023
by
admin
on
Sat Dec 16 01:41:13 GMT 2023
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| Record UNII |
F84YQX13FV
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| Record Status |
Validated (UNII)
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| Record Version |
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913541-47-6
Created by
admin on Sat Dec 16 01:41:13 GMT 2023 , Edited by admin on Sat Dec 16 01:41:13 GMT 2023
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53497429
Created by
admin on Sat Dec 16 01:41:13 GMT 2023 , Edited by admin on Sat Dec 16 01:41:13 GMT 2023
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F84YQX13FV
Created by
admin on Sat Dec 16 01:41:13 GMT 2023 , Edited by admin on Sat Dec 16 01:41:13 GMT 2023
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SLX-4090
Created by
admin on Sat Dec 16 01:41:13 GMT 2023 , Edited by admin on Sat Dec 16 01:41:13 GMT 2023
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PRIMARY | Funding Source - FDA OOPDPurpose: This study is being done to find out whether an investigational (not approved by FDA ) drug called SLx-4090 or Orlistat (FDA approved medication for weight loss) when given alone or in combination can treat the high blood fat (elevated triglycerides)levels found in the condition Type 1 Hyperlipoproteinemia (T1HLP) better or more safely than low fat diet alone, the current standard medical care.It is also not clear whether Orlistat, that is FDA approved for weight loss, is effective in lowering blood fat levels in patients with Type 1 hyperlipoproteinemia (T1HLP). The researchers are interested in learning whether any one of these drugs when given alone or in combination is more effective and safe in treating T1HLP. | ||
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DB05678
Created by
admin on Sat Dec 16 01:41:13 GMT 2023 , Edited by admin on Sat Dec 16 01:41:13 GMT 2023
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| Related Record | Type | Details | ||
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ACTIVE MOIETY |
6-(4'-Trifluoromethyl-6-methoxy-biphenyl-2-ylcarboxamido)-1,2,3,4-tetrahydroisoquinoline-2-carboxylic acid phenyl ester (SLx-4090) (IC(50) value 8 nM) was designed to inhibit only MTP localized to enterocytes. In Caco-2 cells SLx-4090 inhibited apolipoprotein B (IC(50) value 9.6 nM) but not apolipoprotein A1 secretion. Administered orally to rats SLx-4090 reduced postprandial lipids by >50% with an ED(50) value 7 mg/kg. SLx-4090 was not detected in the systemic or portal vein serum of the animals (lower limit of quantitation 5 ng/ml) after single or multiple oral doses in fasted rodents. When coadministered with tyloxapol, SLx-4090 did not inhibit the secretion of hepatic triglycerides (TG), consistent with the absence of systemic exposure. Chronic treatment with SLx-4090 in mice maintained on a high-fat diet decreased LDL-C and TG and resulted in weight loss without the elevation of liver enzymes or an increase in hepatic fat.
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ACTIVE MOIETY |
Class: Antihyperglycaemic, Antihyperlipidaemic, Benzamide, Isoquinoline, Obesity therapy, Small molecule; Mechanism of Action: Microsomal triglyceride transfer protein inhibitor; Highest Development Phase: Phase II for Type 2 diabetes mellitus, No development reported for Dyslipidaemia, Obesity; Most Recent Events: 01 Mar 2016 Kadmon Pharmaceuticals completes a phase II trial for Type 2 diabetes mellitus (Combination therapy) in USA (NCT02434744), 20 Aug 2015 No recent reports on development identified - Phase-II for Dyslipidaemias in USA and Germany (PO), 20 Aug 2015 No recent reports on development identified - Phase-II for Obesity in USA (PO)
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