Explore a selection of our essential drug information below, or:
Identification
- Generic Name
- KD3010
- DrugBank Accession Number
- DB05188
- Background
KD3010 is a small molecule peroxisome proliferator-activator receptor delta (PPAR Delta) agonist for the treatment of metabolic disorders, including obesity.
- Type
- Small Molecule
- Groups
- Investigational
- Structure
Structure for KD3010 (DB05188)
- Weight
- Average: 670.72
Monoisotopic: 670.163042868 - Chemical Formula
- C30H33F3N2O8S2
- Synonyms
- Not Available
- External IDs
- KD 3010
- KD-3010
- KD3010
Pharmacology
- Indication
Investigated for use/treatment in metabolic disease and obesity.
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By activating PPAR Delta, which regulates lipid catabolism and energy utilization in peripheral tissues, KD3010 is designed to address the underlying metabolic derangement of these disorders. KD3010 results in significant reduction of central adiposity, atherogenic lipid profiles, and improved glucose utilization/insulin sensitivity.
- Mechanism of action
KD3010 is a potent, orally administered, peroxisome proliferator-activated receptor-delta (PPARδ) agonist that exhibits ~1000-fold selectivity over PPARγ and PPARα. PPARδ regulates lipid catabolism and energy utilization in peripheral tissues. Activation of PPARδ reduces central adiposity, improves atherogenic lipid profiles, and increases glucose utilization/insulin sensitivity.
Target Actions Organism UPeroxisome proliferator-activated receptor delta 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.Not Available
- Food Interactions
- Not Available
Categories
- Drug Categories
- Classification
- Not classified
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- Not Available
- CAS number
- 934760-90-4
- InChI Key
- SUTQDFLDQUPTKX-QVLMFNNZSA-N
- InChI
- InChI=1S/C23H25F3N2O5S.C7H8O3S/c1-14-12-27(18-6-8-19(9-7-18)33-23(24,25)26)13-15(2)28(14)34(31,32)21-5-3-4-16-10-17(22(29)30)11-20(16)21;1-6-2-4-7(5-3-6)11(8,9)10/h3-9,14-15,17H,10-13H2,1-2H3,(H,29,30);2-5H,1H3,(H,8,9,10)/t14-,15+,17?;
- IUPAC Name
- 4-methylbenzene-1-sulfonic acid; 4-{[(2R,6S)-2,6-dimethyl-4-[4-(trifluoromethoxy)phenyl]piperazin-1-yl]sulfonyl}-2,3-dihydro-1H-indene-2-carboxylic acid
- SMILES
- CC1=CC=C(C=C1)S(O)(=O)=O.[H]C1(CC2=C(C1)C(=CC=C2)S(=O)(=O)N1[C@@]([H])(C)CN(C[C@@]1([H])C)C1=CC=C(OC(F)(F)F)C=C1)C(O)=O
References
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
- Solid
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source Water Solubility 0.0349 mg/mL ALOGPS logP 3.33 ALOGPS logP 4.88 Chemaxon logS -4.2 ALOGPS pKa (Strongest Acidic) 3.9 Chemaxon pKa (Strongest Basic) 2.86 Chemaxon Physiological Charge -1 Chemaxon Hydrogen Acceptor Count 6 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 87.15 Å2 Chemaxon Rotatable Bond Count 6 Chemaxon Refractivity 115.59 m3·mol-1 Chemaxon Polarizability 47.48 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
- Not Available
- Chromatographic Properties
Collision Cross Sections (CCS)
Not Available
Targets
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Ligand-activated transcription factor key mediator of energy metabolism in adipose tissues (PubMed:35675826). Receptor that binds peroxisome proliferators such as hypolipidemic drugs and fatty acids. Has a preference for poly-unsaturated fatty acids, such as gamma-linoleic acid and eicosapentanoic acid. Once activated by a ligand, the receptor binds to promoter elements of target genes. Regulates the peroxisomal beta-oxidation pathway of fatty acids. Functions as transcription activator for the acyl-CoA oxidase gene. Decreases expression of NPC1L1 once activated by a ligand
- Specific Function
- DNA binding
- Gene Name
- PPARD
- Uniprot ID
- Q03181
- Uniprot Name
- Peroxisome proliferator-activated receptor delta
- Molecular Weight
- 49902.99 Da
Drug created at October 21, 2007 22:24 / Updated at June 12, 2020 16:52