Managlinat dialanetil

This drug entry is a stub and has not been fully annotated. It is scheduled to be annotated soon.

Identification

Generic Name
Managlinat dialanetil
DrugBank Accession Number
DB05518
Background

CS-917 is a novel inhibitor of fructose 1,6-bisphphosphatase (FBPase) which is one of the rate-limiting enzymes of gluconeogenesis.

Type
Small Molecule
Groups
Investigational
Structure
Thumb
Weight
Average: 500.55
Monoisotopic: 500.185842971
Chemical Formula
C21H33N4O6PS
Synonyms
  • Managlinat dialanetil
  • Managlinat dialanétil
  • Managlinat dialanetilo
  • Managlinatum dialanetilum
External IDs
  • CS 917
  • CS-917
  • CS917
  • MB 06322
  • MB-06322
  • MB06322
  • R 132917

Pharmacology

Indication

Investigated for use/treatment in diabetes mellitus type 2.

Pharmacology
Reduce drug development failure rates
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Contraindications & Blackbox Warnings
Contraindications
Avoid life-threatening adverse drug events
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Avoid life-threatening adverse drug events & improve clinical decision support.
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Pharmacodynamics

Not Available

Mechanism of action

In type 2 diabetes, the liver produces excessive amounts of glucose through the gluconeogenesis (GNG) pathway and consequently is partly responsible for the elevated glucose levels characteristic of the disease. CS-917 targets the AMP binding site of fructose 1,6-bisphosphatase (FBPase), inhibiting the GNC pathway.

TargetActionsOrganism
UFructose-1,6-bisphosphatase 1Not AvailableHumans
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
Adverseeffects
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Toxicity

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
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
3W93F83K7S
CAS number
280782-97-0
InChI Key
BYKBUQDQTLDNLE-KBPBESRZSA-N
InChI
InChI=1S/C21H33N4O6PS/c1-7-29-19(26)13(5)24-32(28,25-14(6)20(27)30-8-2)17-10-9-15(31-17)18-16(11-12(3)4)33-21(22)23-18/h9-10,12-14H,7-8,11H2,1-6H3,(H2,22,23)(H2,24,25,28)/t13-,14-/m0/s1
IUPAC Name
ethyl (2S)-2-[({5-[2-amino-5-(2-methylpropyl)-1,3-thiazol-4-yl]furan-2-yl}({[(2S)-1-ethoxy-1-oxopropan-2-yl]amino})phosphoryl)amino]propanoate
SMILES
[H][C@@](C)(NP(=O)(N[C@@]([H])(C)C(=O)OCC)C1=CC=C(O1)C1=C(CC(C)C)SC(N)=N1)C(=O)OCC

References

General References
  1. Erion MD, van Poelje PD, Dang Q, Kasibhatla SR, Potter SC, Reddy MR, Reddy KR, Jiang T, Lipscomb WN: MB06322 (CS-917): A potent and selective inhibitor of fructose 1,6-bisphosphatase for controlling gluconeogenesis in type 2 diabetes. Proc Natl Acad Sci U S A. 2005 May 31;102(22):7970-5. Epub 2005 May 23. [Article]
  2. Yoshida T, Okuno A, Izumi M, Takahashi K, Hagisawa Y, Ohsumi J, Fujiwara T: CS-917, a fructose 1,6-bisphosphatase inhibitor, improves postprandial hyperglycemia after meal loading in non-obese type 2 diabetic Goto-Kakizaki rats. Eur J Pharmacol. 2008 Dec 28;601(1-3):192-7. doi: 10.1016/j.ejphar.2008.10.050. Epub 2008 Nov 6. [Article]
ChemSpider
7987590
BindingDB
50322043
ChEMBL
CHEMBL259771

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
2CompletedTreatmentType 2 Diabetes Mellitus1

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 Solubility0.0686 mg/mLALOGPS
logP2.14ALOGPS
logP2.74ChemAxon
logS-3.9ALOGPS
pKa (Strongest Acidic)17.32ChemAxon
pKa (Strongest Basic)3.91ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area145.78 Å2ChemAxon
Rotatable Bond Count14ChemAxon
Refractivity124.82 m3·mol-1ChemAxon
Polarizability51.23 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability0ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Targets

Drugtargets2
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Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Monosaccharide binding
Specific Function
Catalyzes the hydrolysis of fructose 1,6-bisphosphate to fructose 6-phosphate in the presence of divalent cations, acting as a rate-limiting enzyme in gluconeogenesis. Plays a role in regulating gl...
Gene Name
FBP1
Uniprot ID
P09467
Uniprot Name
Fructose-1,6-bisphosphatase 1
Molecular Weight
36842.145 Da
References
  1. Erion MD, van Poelje PD, Dang Q, Kasibhatla SR, Potter SC, Reddy MR, Reddy KR, Jiang T, Lipscomb WN: MB06322 (CS-917): A potent and selective inhibitor of fructose 1,6-bisphosphatase for controlling gluconeogenesis in type 2 diabetes. Proc Natl Acad Sci U S A. 2005 May 31;102(22):7970-5. Epub 2005 May 23. [Article]

Drug created on November 18, 2007 18:25 / Updated on February 21, 2021 18:51