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
Structure for Managlinat dialanetil (DB05518)
- 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.
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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.
Target Actions Organism UFructose-1,6-bisphosphatase 1 Not Available 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
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates.Improve decision support & research outcomes with our structured adverse effects data.- 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
- 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]
- 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]
- External Links
- ChemSpider
- 7987590
- BindingDB
- 50322043
- ChEMBL
- CHEMBL259771
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 2 Completed Treatment Type 2 Diabetes Mellitus 1
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
Property Value Source Water Solubility 0.0686 mg/mL ALOGPS logP 2.14 ALOGPS logP 2.74 Chemaxon logS -3.9 ALOGPS pKa (Strongest Acidic) 17.32 Chemaxon pKa (Strongest Basic) 3.91 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 5 Chemaxon Hydrogen Donor Count 3 Chemaxon Polar Surface Area 145.78 Å2 Chemaxon Rotatable Bond Count 14 Chemaxon Refractivity 124.82 m3·mol-1 Chemaxon Polarizability 51.23 Å3 Chemaxon Number of Rings 2 Chemaxon Bioavailability 0 Chemaxon Rule of Five No Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Not Available
Targets
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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
- 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 at November 18, 2007 18:25 / Updated at February 21, 2021 18:51