This drug entry is a stub and has not been fully annotated. It is scheduled to be annotated soon.
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Identification
- Generic Name
- AMG-222
- DrugBank Accession Number
- DB06011
- Background
Not Available
- Type
- Small Molecule
- Groups
- Investigational
- Structure
Structure for AMG-222 (DB06011)
- Weight
- Average: 597.724
Monoisotopic: 597.317586152 - Chemical Formula
- C32H39N9O3
- Synonyms
- Not Available
- External IDs
- ALS 2-0426
- ALS-2-0426
- AMG-222
Pharmacology
- Indication
Investigated for use/treatment in diabetes mellitus type 2.
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Not Available
- Mechanism of action
AMG-222 is an orally active, small molecule inhibitor of Dipeptidyl Peptidase IV (DPP-IV). DPP-IV inactivates glucagon-like peptide-1 (GLP-1), an important mediator of blood glucose levels following meals. DPP-IV inhibitors have been clinically shown to provide long term improvement of glucose control without the risk of hypoglycemia, and to improve the function of pancreatic beta cells, the cells responsible for the production of insulin. DPP-IV inhibitors represent a novel approach to the treatment of type II diabetes.
Target Actions Organism UDipeptidyl peptidase 4 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
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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.
Drug Interaction Integrate drug-drug
interactions in your softwareAcarbose The risk or severity of hypoglycemia can be increased when Acarbose is combined with AMG-222. Acebutolol The therapeutic efficacy of AMG-222 can be increased when used in combination with Acebutolol. Acetazolamide The therapeutic efficacy of AMG-222 can be increased when used in combination with Acetazolamide. Acetohexamide AMG-222 may increase the hypoglycemic activities of Acetohexamide. Acetyl sulfisoxazole The therapeutic efficacy of AMG-222 can be increased when used in combination with Acetyl sulfisoxazole. - Food Interactions
- Not Available
Categories
- Drug Categories
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as dibenzocycloheptenes. These are compounds containing a dibenzocycloheptene moiety, which consists of two benzene rings connected by a cycloheptene ring.
- Kingdom
- Organic compounds
- Super Class
- Benzenoids
- Class
- Dibenzocycloheptenes
- Sub Class
- Not Available
- Direct Parent
- Dibenzocycloheptenes
- Alternative Parents
- Alpha amino acid amides / N-acylpyrrolidines / Aralkylamines / Tetrazoles / Tertiary carboxylic acid amides / Heteroaromatic compounds / Nitriles / Dialkylamines / Azacyclic compounds / Organic oxides show 2 more
- Substituents
- Alpha-amino acid amide / Alpha-amino acid or derivatives / Amine / Amino acid or derivatives / Aralkylamine / Aromatic heteropolycyclic compound / Azacycle / Azole / Carbonitrile / Carbonyl group show 19 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- Not Available
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- GH23A7L3EL
- CAS number
- 913978-37-7
- InChI Key
- NVSWJKWHLUTHLP-CPJSRVTESA-N
- InChI
- InChI=1S/C32H39N9O3/c1-20(34-19-28(42)41-14-6-7-25(41)18-33)17-32(31-35-37-38-36-31)26-12-10-23(29(43)39(2)3)15-21(26)8-9-22-16-24(11-13-27(22)32)30(44)40(4)5/h10-13,15-16,20,25,34H,6-9,14,17,19H2,1-5H3,(H,35,36,37,38)/t20-,25-/m0/s1
- IUPAC Name
- 2-[(2S)-2-({2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl}amino)propyl]-N6,N6,N13,N13-tetramethyl-2-(2H-1,2,3,4-tetrazol-5-yl)tricyclo[9.4.0.0^{3,8}]pentadeca-1(15),3,5,7,11,13-hexaene-6,13-dicarboxamide
- SMILES
- [H][C@](C)(CC1(C2=NNN=N2)C2=CC=C(C=C2CCC2=CC(=CC=C12)C(=O)N(C)C)C(=O)N(C)C)NCC(=O)N1CCC[C@@]1([H])C#N
References
- General References
- Not Available
- External Links
- ChemSpider
- 10151331
Clinical Trials
- Clinical Trials
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package Phase Status Purpose Conditions Count Start Date Why Stopped 100+ additional columns Unlock 175K+ rows when you subscribe.View sample data
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 0.0336 mg/mL ALOGPS logP 2.31 ALOGPS logP 0.56 Chemaxon logS -4.2 ALOGPS pKa (Strongest Acidic) 6.44 Chemaxon pKa (Strongest Basic) 7.77 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 8 Chemaxon Hydrogen Donor Count 2 Chemaxon Polar Surface Area 151.21 Å2 Chemaxon Rotatable Bond Count 8 Chemaxon Refractivity 170.86 m3·mol-1 Chemaxon Polarizability 64.53 Å3 Chemaxon Number of Rings 5 Chemaxon Bioavailability 1 Chemaxon Rule of Five No Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule Yes Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Not Available
Targets
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Cell surface glycoprotein receptor involved in the costimulatory signal essential for T-cell receptor (TCR)-mediated T-cell activation (PubMed:10900005, PubMed:10951221, PubMed:11772392, PubMed:17287217). Acts as a positive regulator of T-cell coactivation, by binding at least ADA, CAV1, IGF2R, and PTPRC (PubMed:10900005, PubMed:10951221, PubMed:11772392, PubMed:14691230). Its binding to CAV1 and CARD11 induces T-cell proliferation and NF-kappa-B activation in a T-cell receptor/CD3-dependent manner (PubMed:17287217). Its interaction with ADA also regulates lymphocyte-epithelial cell adhesion (PubMed:11772392). In association with FAP is involved in the pericellular proteolysis of the extracellular matrix (ECM), the migration and invasion of endothelial cells into the ECM (PubMed:10593948, PubMed:16651416). May be involved in the promotion of lymphatic endothelial cells adhesion, migration and tube formation (PubMed:18708048). When overexpressed, enhanced cell proliferation, a process inhibited by GPC3 (PubMed:17549790). Acts also as a serine exopeptidase with a dipeptidyl peptidase activity that regulates various physiological processes by cleaving peptides in the circulation, including many chemokines, mitogenic growth factors, neuropeptides and peptide hormones such as brain natriuretic peptide 32 (PubMed:10570924, PubMed:16254193). Removes N-terminal dipeptides sequentially from polypeptides having unsubstituted N-termini provided that the penultimate residue is proline (PubMed:10593948)
- Specific Function
- aminopeptidase activity
- Gene Name
- DPP4
- Uniprot ID
- P27487
- Uniprot Name
- Dipeptidyl peptidase 4
- Molecular Weight
- 88277.935 Da
Drug created at November 18, 2007 18:29 / Updated at June 12, 2020 16:52