Identification
- Generic Name
- Pimagedine
- DrugBank Accession Number
- DB05383
- Background
Pimagedine has been developed by Synvista Therapeutics, Inc for the treatment of diabetic kidney disease. It is an advanced glycation end product inhibitor which manages diabetic nephropathy, either alone or in combination with other therapies. It is beneficial in treating patients with diabetic nephropathy.
- Type
- Small Molecule
- Groups
- Investigational
- Structure
Structure for Pimagedine (DB05383)
- Weight
- Average: 74.0851
Monoisotopic: 74.059246212 - Chemical Formula
- CH6N4
- Synonyms
- Aminate base
- Aminoguanidine
- Guanyl hydrazine
- Hydrazinecarboximidamide
- Monoaminoguanidine
- Pimagedine
Pharmacology
- Indication
Investigated for use/treatment in diabetic kidney disease.
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Not Available
- Mechanism of action
Pimagedine reportedly inhibits the formation of glycosylated proteins (advanced glycosylation end-products) and has other actions including inhibition of aldose reductase.
Target Actions Organism UNitric oxide synthase, inducible inhibitorHumans UAldose reductase Not Available Humans UMetalloproteinase inhibitor 3 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.
Drug Interaction Integrate drug-drug
interactions in your softwareAmantadine The serum concentration of Amantadine can be increased when it is combined with Pimagedine. Choline The serum concentration of Choline can be increased when it is combined with Pimagedine. Choline salicylate The serum concentration of Choline salicylate can be increased when it is combined with Pimagedine. Cisplatin The serum concentration of Cisplatin can be increased when it is combined with Pimagedine. Clofarabine The serum concentration of Clofarabine can be increased when it is combined with Pimagedine. Dalfampridine The serum concentration of Dalfampridine can be increased when it is combined with Pimagedine. Dofetilide The serum concentration of Dofetilide can be increased when it is combined with Pimagedine. Dopamine The serum concentration of Dopamine can be increased when it is combined with Pimagedine. Epinephrine The serum concentration of Epinephrine can be increased when it is combined with Pimagedine. Gentamicin The serum concentration of Gentamicin can be increased when it is combined with Pimagedine. 
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- Not Available
Products
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Ingredient UNII CAS InChI Key Pimagedine hydrochloride A2Z7G2RGAH 1937-19-5 UBDZFAGVPPMTIT-UHFFFAOYSA-N
Categories
- Drug Categories
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as guanidines. These are compounds containing a guanidine moiety, with the general structure (R1R2N)(R3R4N)C=N-R5.
- Kingdom
- Organic compounds
- Super Class
- Organic nitrogen compounds
- Class
- Organonitrogen compounds
- Sub Class
- Guanidines
- Direct Parent
- Guanidines
- Alternative Parents
- Hydrazones / Organopnictogen compounds / Hydrocarbon derivatives
- Substituents
- Aliphatic acyclic compound / Guanidine / Hydrazone / Hydrocarbon derivative / Organopnictogen compound
- Molecular Framework
- Aliphatic acyclic compounds
- External Descriptors
- one-carbon compound, guanidines (CHEBI:40618)
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- SCQ4EZQ113
- CAS number
- 79-17-4
- InChI Key
- HAMNKKUPIHEESI-UHFFFAOYSA-N
- InChI
- InChI=1S/CH6N4/c2-1(3)5-4/h4H2,(H4,2,3,5)
- IUPAC Name
- N-aminoguanidine
- SMILES
- NNC(N)=N
References
- General References
- External Links
- PubChem Compound
- 2146
- PubChem Substance
- 175426990
- ChemSpider
- 2061
- BindingDB
- 50207159
- 1311670
- ChEBI
- 40618
- ChEMBL
- CHEMBL225304
- ZINC
- ZINC000008034829
- PDBe Ligand
- AGU
- Wikipedia
- Pimagedine
- PDB Entries
- 2nos / 5neq / 5ny8
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 1 Completed Basic Science Diabetic Retinopathy (DR) 1 1 Completed Prevention Endotoxaemia 1 Not Available Completed Treatment Asthma 1 Not Available Completed Treatment Chronic Obstructive Pulmonary Disease (COPD) 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 8.36 mg/mL ALOGPS logP -1.8 ALOGPS logP -1.5 ChemAxon logS -0.95 ALOGPS pKa (Strongest Basic) 12.01 ChemAxon Physiological Charge 1 ChemAxon Hydrogen Acceptor Count 4 ChemAxon Hydrogen Donor Count 4 ChemAxon Polar Surface Area 87.92 Å2 ChemAxon Rotatable Bond Count 0 ChemAxon Refractivity 40.84 m3·mol-1 ChemAxon Polarizability 6.88 Å3 ChemAxon Number of Rings 0 ChemAxon Bioavailability 1 ChemAxon Rule of Five Yes ChemAxon Ghose Filter No ChemAxon Veber's Rule No ChemAxon MDDR-like Rule No ChemAxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9153 Blood Brain Barrier + 0.8347 Caco-2 permeable - 0.5826 P-glycoprotein substrate Non-substrate 0.7501 P-glycoprotein inhibitor I Non-inhibitor 0.9597 P-glycoprotein inhibitor II Non-inhibitor 0.9903 Renal organic cation transporter Non-inhibitor 0.8183 CYP450 2C9 substrate Non-substrate 0.8968 CYP450 2D6 substrate Non-substrate 0.8024 CYP450 3A4 substrate Non-substrate 0.8143 CYP450 1A2 substrate Non-inhibitor 0.9045 CYP450 2C9 inhibitor Non-inhibitor 0.913 CYP450 2D6 inhibitor Non-inhibitor 0.9231 CYP450 2C19 inhibitor Non-inhibitor 0.944 CYP450 3A4 inhibitor Non-inhibitor 0.9056 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9771 Ames test Non AMES toxic 0.5884 Carcinogenicity Carcinogens 0.5 Biodegradation Not ready biodegradable 0.9842 Rat acute toxicity 2.5602 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9236 hERG inhibition (predictor II) Non-inhibitor 0.9791
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS Not Available Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available
Targets
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Tetrahydrobiopterin binding
- Specific Function
- Produces nitric oxide (NO) which is a messenger molecule with diverse functions throughout the body. In macrophages, NO mediates tumoricidal and bactericidal actions. Also has nitrosylase activity ...
- Gene Name
- NOS2
- Uniprot ID
- P35228
- Uniprot Name
- Nitric oxide synthase, inducible
- Molecular Weight
- 131116.3 Da
References
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
- Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
- Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Glyceraldehyde oxidoreductase activity
- Specific Function
- Catalyzes the NADPH-dependent reduction of a wide variety of carbonyl-containing compounds to their corresponding alcohols with a broad range of catalytic efficiencies.
- Gene Name
- AKR1B1
- Uniprot ID
- P15121
- Uniprot Name
- Aldose reductase
- Molecular Weight
- 35853.125 Da
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Protease binding
- Specific Function
- Complexes with metalloproteinases (such as collagenases) and irreversibly inactivates them by binding to their catalytic zinc cofactor. May form part of a tissue-specific acute response to remodeli...
- Gene Name
- TIMP3
- Uniprot ID
- P35625
- Uniprot Name
- Metalloproteinase inhibitor 3
- Molecular Weight
- 24144.83 Da
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Quaternary ammonium group transmembrane transporter activity
- Specific Function
- Mediates tubular uptake of organic compounds from circulation. Mediates the influx of agmatine, dopamine, noradrenaline (norepinephrine), serotonin, choline, famotidine, ranitidine, histamin, creat...
- Gene Name
- SLC22A2
- Uniprot ID
- O15244
- Uniprot Name
- Solute carrier family 22 member 2
- Molecular Weight
- 62579.99 Da
References
- Kimura N, Masuda S, Katsura T, Inui K: Transport of guanidine compounds by human organic cation transporters, hOCT1 and hOCT2. Biochem Pharmacol. 2009 Apr 15;77(8):1429-36. doi: 10.1016/j.bcp.2009.01.010. Epub 2009 Jan 29. [Article]
- Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [Article]
Drug created at November 18, 2007 18:24 / Updated at February 21, 2021 18:51