SLX-4090

Investigational

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)

HIDE SMILES / InChI

Molecular Formula	C31H25F3N2O4
Molecular Weight	546.5364
Charge	0
Count	MOL RATIO 1 MOL RATIO (average)

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Approval Year

Targets

Targets

Primary Target	Pharmacology	Condition	Potency
Microsomal triglyceride transfer protein large subunit 4	Inhibitor 8,297		8.0 nM [IC50]

Substance Class	Chemical
Record UNII	F84YQX13FV
Record Status	`Validated (UNII)`
Record Version

Show entries

Name

Type

Language

SLX-4090

Common Name

English

2(1H)-ISOQUINOLINECARBOXYLIC ACID, 3,4-DIHYDRO-6-(((6-METHOXY-4'-(TRIFLUOROMETHYL)(1,1'-BIPHENYL)-2-YL)CARBONYL)AMINO)-, PHENYL ESTER

Systematic Name

English

KD-026

Code

English

PHENYL 6-((3-METHOXY-2-(4-(TRIFLUOROMETHYL)PHENYL)BENZOYL)AMINO)-3,4-DIHYDRO-1H-ISOQUINOLINE-2-CARBOXYLATE

Systematic Name

English

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Code System

Code

Type

Description

CAS

913541-47-6

PRIMARY

PUBCHEM

53497429

PRIMARY

FDA UNII

F84YQX13FV

PRIMARY

CLINICAL_TRIALS.GOV

SLX-4090

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.

DRUG BANK

DB05678

PRIMARY

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Related Record

Type

Details


					F84YQX13FV

SLX-4090

ACTIVE MOIETY

Comments:

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.


					F84YQX13FV

SLX-4090

ACTIVE MOIETY

Comments:

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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