| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 100mg | |||
| 250mg | |||
| Other Sizes |
| Targets |
Adenosine A1 receptor (central).
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|---|---|
| ln Vitro |
FR-194921 is a potent antagonist of the central adenosine A1 receptor with a Ki of 6.6 nM. It shows high selectivity for the A1 receptor over the A2A receptor (Ki = 5400 nM). The compound exerts cognitive-enhancing and anxiolytic activity. It penetrates the blood-brain barrier.
|
| ln Vivo |
The stent exhibits good oral bioavailability for FR194921 (32 mg/kg; po), as evidenced by its AUC of 6.91 µg·h/mL, Cmax of 2.13 µg/mL, Tmax of 0.63 h, and BA of 60.6% [1]. The lowest dosages of FR194921 (0.032, 0.1, and 0.32 mg/kg) are required to restrict CPA-induced hypomotility [2]. Scopolamine-induced memory impairments are greatly improved by FR194921 (0.1–10 mg/kg; intraperitoneal administration) [2].
In vivo, FR-194921 exerts both cognitive-enhancing and anxiolytic activity. The compound is orally active and penetrates the BBB. It has been suggested for the therapeutic potential in dementia and anxiety disorders. |
| Enzyme Assay |
Adenosine A1 receptor binding affinity is assessed using in vitro radioligand binding assays. Membrane preparations from cells expressing the recombinant human A1 receptor or from brain tissue are incubated with a selective radioligand (e.g., [3H]DPCPX) and varying concentrations of FR-194921. Ki values are calculated from displacement curves. Selectivity is assessed against A2A and other adenosine receptor subtypes.
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| Cell Assay |
Cellular activity is evaluated in cells expressing the A1 receptor. Cells are treated with FR-194921, and the inhibition of A1 receptor-mediated signaling, such as the decrease in cAMP accumulation, is measured. The compound's antagonist activity is confirmed by blocking the effects of an A1 agonist.
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| Animal Protocol |
Animal/Disease Models: SD rats [2]
Doses: 0.032, 0.1, 0.32 mg/kg Route of Administration: Po; . Oral administration of CPA (0.056 mg/kg; ip) 25 minutes before intraperitonealadministration Experimental Results: Dose-dependent attenuation of CPA-induced hypokinesia with an ED50 value of 0.08 mg/kg, statistically significant at 0.32 mg/kg Attachment. Animal/Disease Models: SD rat [2] Doses: 0.1, 0.32, 1, 3.2, 10 mg/kg Route of Administration: intraperitoneal (ip) injection; Scopolamine (1 mg/kg, intraperitoneal (ip) injection) Experimental Results: After scopolamine-induced memory deficit in rats Cognitive abilities are Dramatically enhanced. In vivo efficacy is studied in animal models of cognitive impairment and anxiety, such as the Morris water maze, passive avoidance, or elevated plus maze tests. FR-194921 is administered orally, and its effects on cognition and anxiety-related behaviors are assessed. The compound's ability to penetrate the brain is confirmed by measuring its concentration in brain tissue. |
| ADME/Pharmacokinetics |
FR-194921 has a molecular formula of C23H23N5O and a molecular weight of 385.46 g/mol. It is an orally active compound that penetrates the blood-brain barrier. The compound is a potent and selective adenosine A1 receptor antagonist.
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| Toxicity/Toxicokinetics |
Specific toxicological data for FR-194921 are not extensively published. As a CNS-active compound, it should be handled with appropriate safety precautions. The compound is for research use only.
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| References |
[1]. Kuroda S, et al. Design, synthesis and biological evaluation of a novel series of potent, orally active adenosine A1 receptor antagonists with high blood-brain barrier permeability. Chem Pharm Bull (Tokyo). 2001 Aug;49(8):988-98.
[2]. Maemoto T, et al. Pharmacological characterization of FR194921, a new potent, selective, and orally active antagonist for central adenosine A1 receptors. J Pharmacol Sci. 2004 Sep;96(1):42-52. |
| Additional Infomation |
FR-194921 is a research tool compound for studying the role of adenosine A1 receptors in cognition and anxiety. It is not approved for clinical use. The compound is a potent, selective, and orally active A1 antagonist with Ki values of 6.6 nM for A1 and 5400 nM for A2A.
|
| Molecular Formula |
C23H23N5O
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|---|---|
| Molecular Weight |
385.46
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| Exact Mass |
385.19
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| CAS # |
202646-80-8
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| PubChem CID |
9821511
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| Appearance |
Off-white to light yellow solid powder
|
| LogP |
3.429
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
|
| Heavy Atom Count |
29
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| Complexity |
662
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| Defined Atom Stereocenter Count |
0
|
| SMILES |
CN1CCC(CC1)N2C(=O)C=CC(=N2)C3=C4C=CC=CN4N=C3C5=CC=CC=C5
|
| InChi Key |
YHDRUTMZCJZJAL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H23N5O/c1-26-15-12-18(13-16-26)28-21(29)11-10-19(24-28)22-20-9-5-6-14-27(20)25-23(22)17-7-3-2-4-8-17/h2-11,14,18H,12-13,15-16H2,1H3
|
| Chemical Name |
2-(1-methylpiperidin-4-yl)-6-(2-phenylpyrazolo[1,5-a]pyridin-3-yl)pyridazin-3-one
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| Synonyms |
FR194921; FR 194921; FR-194921
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.5943 mL | 12.9715 mL | 25.9430 mL | |
| 5 mM | 0.5189 mL | 2.5943 mL | 5.1886 mL | |
| 10 mM | 0.2594 mL | 1.2972 mL | 2.5943 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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