Acoltremon
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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
- Acoltremon
- DrugBank Accession Number
- DB19202
- Background
Acoltremon is under investigation in clinical trial NCT05493111 (A Long-term Safety Study Evaluating the Safety and Systemic Exposure of AR-15512).
- Type
- Small Molecule
- Groups
- Investigational
- Structure
- Weight
- Average: 289.419
Monoisotopic: 289.204179113 - Chemical Formula
- C18H27NO2
- Synonyms
- Cyclohexanecarboxamide, n-(4-methoxyphenyl)-5-methyl-2-(1-methylethyl)-, (1r,2s,5r)-
- N-(4-methoxyphenyl)-5-methyl-2- (1-methylethyl)cyclohexanecarboxamide, (1r,2s,5r)-
- N-(4-methoxyphenyl)-p-menthanecarboxamide
- External IDs
- AR-15512
- FEMA NO. 4681
- WS-12
Pharmacology
- Indication
Not Available
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- Pharmacodynamics
Not Available
- Mechanism of action
Target Actions Organism ATransient receptor potential cation channel subfamily M member 8 activatorHumans - 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. View sample adverse effects data in our new Data Library!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
- Not Available
Chemical Identifiers
- UNII
- 1L7BVT4Z4Z
- CAS number
- 68489-09-8
- InChI Key
- HNSGVPAAXJJOPQ-XOKHGSTOSA-N
- InChI
- InChI=1S/C18H27NO2/c1-12(2)16-10-5-13(3)11-17(16)18(20)19-14-6-8-15(21-4)9-7-14/h6-9,12-13,16-17H,5,10-11H2,1-4H3,(H,19,20)/t13-,16-,17-/m1/s1
- IUPAC Name
- SMILES
- COC1=CC=C(NC(=O)[C@@H]2C[C@H](C)CC[C@H]2C(C)C)C=C1
References
- General References
- Not Available
- External Links
- ChemSpider
- 9441255
- BindingDB
- 50442649
- ChEMBL
- CHEMBL2441929
- ZINC
- ZINC000034499085
- PDBe Ligand
- KXS
- PDB Entries
- 6nr2
Clinical Trials
- Clinical Trials
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Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
- Not Available
- Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Not Available
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Not Available
- Chromatographic Properties
Collision Cross Sections (CCS)
Not Available
Targets
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Activator
- General Function
- Receptor-activated non-selective cation channel involved in detection of sensations such as coolness, by being activated by cold temperature below 25 degrees Celsius. Activated by icilin, eucalyptol, menthol, cold and modulation of intracellular pH. Involved in menthol sensation. Permeable for monovalent cations sodium, potassium, and cesium and divalent cation calcium. Temperature sensing is tightly linked to voltage-dependent gating. Activated upon depolarization, changes in temperature resulting in graded shifts of its voltage-dependent activation curves. The chemical agonist menthol functions as a gating modifier, shifting activation curves towards physiological membrane potentials. Temperature sensitivity arises from a tenfold difference in the activation energies associated with voltage-dependent opening and closing. In prostate cancer cells, shows strong inward rectification and high calcium selectivity in contrast to its behavior in normal cells which is characterized by outward rectification and poor cationic selectivity. Plays a role in prostate cancer cell migration (PubMed:25559186). Isoform 2 and isoform 3 negatively regulate menthol- and cold-induced channel activity by stabilizing the closed state of the channel
- Specific Function
- Calcium channel activity
- Gene Name
- TRPM8
- Uniprot ID
- Q7Z2W7
- Uniprot Name
- Transient receptor potential cation channel subfamily M member 8
- Molecular Weight
- 127684.035 Da
References
- Zhou Y, Zhang Y, Zhao D, Yu X, Shen X, Zhou Y, Wang S, Qiu Y, Chen Y, Zhu F: TTD: Therapeutic Target Database describing target druggability information. Nucleic Acids Res. 2024 Jan 5;52(D1):D1465-D1477. doi: 10.1093/nar/gkad751. [Article]
Drug created at July 08, 2024 21:31 / Updated at August 27, 2024 19:17