SLx-4090

Identification

Name
SLx-4090
Accession Number
DB05678
Description

SLx-4090 is a microsomal triglyceride transfer protein (MTTP) inhibitor potentially for the treatment of type 2 diabetes. 1

Type
Small Molecule
Groups
Investigational
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Structure
Thumb
Weight
Average: 546.546
Monoisotopic: 546.176641782
Chemical Formula
C31H25F3N2O4
Synonyms
Not Available
External IDs
  • KD-026
  • KD026
  • SLx 4090
  • SLx-4090
  • SLx4090

Pharmacology

Indication

Investigated for use/treatment in hyperlipidemia.

Contraindications & Blackbox Warnings
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Pharmacodynamics
Not Available
Mechanism of action

SLx-4090 inhibits Microsomal Triglyceride Transfer Protein (MTP). It acts selectively in the enterocytes lining the gastrointestinal tract, preventing the formation of chylomicrons which are used to transport triglyceride (TG) and cholesterol into the systemic circulation.

TargetActionsOrganism
UMicrosomal triglyceride transfer protein large subunit
inhibitor
Humans
Absorption
Not Available
Volume of distribution
Not Available
Protein binding
Not Available
Metabolism
Not Available
Route of elimination
Not Available
Half-life
Not Available
Clearance
Not Available
Adverse Effects
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Toxicity
Not Available
Affected organisms
Not Available
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Not Available
Food Interactions
Not Available

Categories

Drug Categories
Classification
Not classified

Chemical Identifiers

UNII
F84YQX13FV
CAS number
913541-47-6
InChI Key
AZUIUVJESCFSLJ-UHFFFAOYSA-N
InChI
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)
IUPAC Name
phenyl 6-[6-methoxy-4'-(trifluoromethyl)-[1,1'-biphenyl]-2-amido]-1,2,3,4-tetrahydroisoquinoline-2-carboxylate
SMILES
COC1=CC=CC(C(=O)NC2=CC3=C(CN(CC3)C(=O)OC3=CC=CC=C3)C=C2)=C1C1=CC=C(C=C1)C(F)(F)F

References

General References
  1. Kim E, Campbell S, Schueller O, Wong E, Cole B, Kuo J, Ellis J, Ferkany J, Sweetnam P: A small-molecule inhibitor of enterocytic microsomal triglyceride transfer protein, SLx-4090: biochemical, pharmacodynamic, pharmacokinetic, and safety profile. J Pharmacol Exp Ther. 2011 Jun;337(3):775-85. doi: 10.1124/jpet.110.177527. Epub 2011 Mar 15. [PubMed:21406547]
ChemSpider
58540436
ZINC
ZINC000072316409

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
2CompletedTreatmentHyperlipidemias1
2CompletedTreatmentHypertriglyceridemias1
2CompletedTreatmentType 2 Diabetes Mellitus2
2TerminatedTreatmentType 1 Hyperlipoproteinemia1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.000197 mg/mLALOGPS
logP5.24ALOGPS
logP6.92ChemAxon
logS-6.4ALOGPS
pKa (Strongest Acidic)15.11ChemAxon
pKa (Strongest Basic)-3.8ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area67.87 Å2ChemAxon
Rotatable Bond Count7ChemAxon
Refractivity146.69 m3·mol-1ChemAxon
Polarizability55.02 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability0ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Targets

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Protein heterodimerization activity
Specific Function
Catalyzes the transport of triglyceride, cholesteryl ester, and phospholipid between phospholipid surfaces (PubMed:23475612, PubMed:8939939, PubMed:26224785, PubMed:25108285, PubMed:22236406). Requ...
Gene Name
MTTP
Uniprot ID
P55157
Uniprot Name
Microsomal triglyceride transfer protein large subunit
Molecular Weight
99350.255 Da
References
  1. Kim E, Campbell S, Schueller O, Wong E, Cole B, Kuo J, Ellis J, Ferkany J, Sweetnam P: A small-molecule inhibitor of enterocytic microsomal triglyceride transfer protein, SLx-4090: biochemical, pharmacodynamic, pharmacokinetic, and safety profile. J Pharmacol Exp Ther. 2011 Jun;337(3):775-85. doi: 10.1124/jpet.110.177527. Epub 2011 Mar 15. [PubMed:21406547]

Drug created on November 18, 2007 11:26 / Updated on June 12, 2020 10:52

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