| Size | Price | Stock | Qty |
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| 1mg |
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| 100mg | |||
| Other Sizes |
| Targets |
The primary target of Kfm 19 is the adenosine A1 receptor, where it acts as a potent and selective antagonist. The compound blocks A1 receptor signaling to counteract adenosine-mediated inhibitory neuromodulation. Adenosine A1 receptors are widely distributed in the central nervous system and play important roles in regulating neuronal excitability, neurotransmitter release, and synaptic plasticity. By antagonizing these receptors, Kfm 19 can enhance cognitive function and counteract the sedative and inhibitory effects of adenosine. The compound's high potency (IC50 of 50 nM) and selectivity make it a valuable tool for studying A1 receptor function.
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| ln Vitro |
Kfm 19 is a potent and selective adenosine A1 receptor antagonist with an IC50 of 50 nM. It blocks A1 receptor signaling and counteracts adenosine-mediated inhibitory neuromodulation. The compound's activity is specific to the A1 receptor subtype, making it a valuable tool for studying the role of A1 receptors in various physiological and pathological processes. Its ability to enhance cognitive function suggests potential applications in treating cognitive disorders. The compound's potency (50 nM IC50) indicates high affinity for the A1 receptor.
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| ln Vivo |
No specific in vivo activity data is publicly available for Kfm 19. As a potent and selective adenosine A1 receptor antagonist, it would be expected to have central nervous system effects related to A1 receptor blockade. The compound is a potential cognitive enhancer, suggesting it may improve learning and memory in animal models. It is used for the study of neurological disorders, indicating potential applications in conditions such as Alzheimer's disease, cognitive impairment, and other neurological conditions where adenosine A1 receptor modulation may be beneficial.
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| Enzyme Assay |
No specific non-cell assay protocol is available for Kfm 19. For adenosine receptor antagonists, standard cell-free assays include radioligand binding displacement using [³H]-labeled adenosine receptor ligands (such as [³H]DPCPX for A1 receptors) and membrane preparations from cells expressing recombinant A1 receptors. Various concentrations of Kfm 19 are incubated with the radioligand and receptor membranes; bound radioactivity is measured to determine IC50 values. These assays provide quantitative data on the compound's affinity for the A1 receptor.
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| Cell Assay |
No specific cell-based assay protocol is available for Kfm 19. For adenosine receptor antagonists, standard cellular assays involve measuring the compound's ability to block A1 receptor-mediated signaling. Cells expressing recombinant A1 receptors are treated with an A1 receptor agonist (such as CPA or CHA) in the presence or absence of Kfm 19. Functional readouts include inhibition of adenylyl cyclase (measured by cAMP accumulation), activation of G protein-coupled inwardly rectifying potassium channels (GIRK), or calcium signaling. The compound's potency (IC50) can be determined from these functional assays.
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| Animal Protocol |
No specific animal protocol is available for Kfm 19. For cognitive enhancement studies, standard behavioral tests in rodents include Morris water maze, novel object recognition, and radial arm maze. The compound is administered (route and dose to be determined) prior to behavioral testing. For neurological disorder models, appropriate disease models (e.g., transgenic Alzheimer's models, ischemia models) would be used. The compound's effects on cognitive function, neuronal survival, and disease pathology would be assessed.
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| ADME/Pharmacokinetics |
No detailed pharmacokinetic data is publicly available for Kfm 19. The compound has a molecular weight of 318.37 and formula C16H22N4O3. As a small molecule with moderate lipophilicity, it would be expected to have favorable oral bioavailability and blood-brain barrier penetration. The compound is soluble in DMSO and other organic solvents. Comprehensive pharmacokinetic studies would be required to determine absorption, distribution, metabolism, and excretion parameters.
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| Toxicity/Toxicokinetics |
No detailed toxicology data is publicly available for Kfm 19. As a research compound, standard preclinical toxicology would be required for therapeutic development. The compound's selectivity for the A1 receptor may contribute to a manageable safety profile, though potential off-target effects on other adenosine receptor subtypes (A2A, A2B, A3) would need to be assessed. The compound is for research use only and not for therapeutic applications.
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| Additional Infomation |
Kfm 19 is also known as KFM19 and 8-(3-oxocyclopentyl)-1,3-dipropyl-7H-purine-2,6-dione. It has the molecular formula C16H22N4O3 and molecular weight 318.37. The SMILES notation is C(N3C1=C([NH]C(=N1)C2CC(=O)CC2)C(=O)N(C3=O)CCC)CC. The compound is an adenosine analog and a potential cognitive enhancer. It is classified as a G protein-coupled receptor and neuroscience compound. No clinical trial status has been identified; it remains a research tool for studying adenosine A1 receptor function and neurological disorders.
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| Molecular Formula |
C16H22N4O3
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|---|---|
| Molecular Weight |
318.37088
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| Exact Mass |
318.169
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| CAS # |
133058-72-7
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| PubChem CID |
131584
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.268g/cm3
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| Boiling Point |
584.7ºC at 760mmHg
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| Flash Point |
307.4ºC
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| Vapour Pressure |
1.18E-13mmHg at 25°C
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| Index of Refraction |
1.575
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| LogP |
1.542
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
23
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| Complexity |
510
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(N1CCC)N(CCC)C2=C(N=C(C3CC(CC3)=O)N2)C1=O
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| InChi Key |
RUHGOZFOVBMWOO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H22N4O3/c1-3-7-19-14-12(15(22)20(8-4-2)16(19)23)17-13(18-14)10-5-6-11(21)9-10/h10H,3-9H2,1-2H3,(H,17,18)
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| Chemical Name |
8-(3-oxocyclopentyl)-1,3-dipropyl-7H-purine-2,6-dione
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~314.10 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1410 mL | 15.7050 mL | 31.4100 mL | |
| 5 mM | 0.6282 mL | 3.1410 mL | 6.2820 mL | |
| 10 mM | 0.3141 mL | 1.5705 mL | 3.1410 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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