| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Adenosine A1 receptor (A1R) is a G protein-coupled receptor that plays important roles in the regulation of the cardiovascular system, including heart rate, contractility, and conduction. NPC 200 is a potent and selective antagonist of the adenosine A1 receptor. By binding to the A1 receptor, NPC 200 blocks the activation of the receptor by adenosine or other agonists, thereby inhibiting A1 receptor-mediated signaling pathways.
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| ln Vitro |
In vitro, NPC 200 is a potent A1 receptor-selective antagonist. It reverses NECA-induced left and right atrial depression with EC50 values of 1.08 μM (left atrium) and 2.03 μM (right atrium). In functional assays, NPC 200 inhibits A1 receptor-mediated signaling, including the inhibition of cAMP accumulation and other downstream effects in cardiac tissue.
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| ln Vivo |
In vivo, NPC 200 acts as an adenosine antagonist and has been shown to reduce high blood pressure. It reverses adenosine-mediated effects in cardiovascular models. By blocking A1 receptor activation, NPC 200 can be used to dissect the role of the A1 receptor in cardiovascular regulation, including heart rate, blood pressure, and cardiac function.
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| Enzyme Assay |
The in vitro enzyme/receptor binding (cell-free) assay for NPC 200 involves radioligand binding assays using membrane preparations from tissues or cells expressing adenosine receptors. The binding affinity and selectivity of NPC 200 for A1 versus other adenosine receptor subtypes are determined using competition binding assays with appropriate radioligands. The Ki values are calculated from competition curves using the Cheng-Prusoff equation.
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| Cell Assay |
In vitro cellular assays for NPC 200 use functional assays measuring A1 receptor-mediated signaling (e.g., cAMP inhibition or G-protein activation) in cells expressing the receptor. Cells expressing A1 receptors are treated with an A1 receptor agonist (such as NECA) in the presence or absence of NPC 200, and downstream signaling is measured. The antagonist activity of the compound is determined by its ability to reverse agonist-induced effects.
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| Animal Protocol |
In vivo studies using animal models of cardiovascular function are performed to evaluate the effects of NPC 200 on adenosine-mediated responses. Atrial depression reversal is a key measure of A1 receptor antagonism in cardiac tissue. Animal models of hypertension and cardiac arrhythmias are used to evaluate the cardiovascular effects of NPC 200.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for NPC 200 are limited. As a xanthine derivative, it is expected to have properties suitable for in vivo research applications. The compound is likely to have good oral bioavailability and distribution to target tissues. Further pharmacokinetic studies are needed to fully characterize the ADME properties of NPC 200.
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| Toxicity/Toxicokinetics |
Preclinical toxicology data for NPC 200 are limited. The compound is used for research purposes only. No significant toxicities have been reported in the literature. Further toxicological evaluation is needed to assess the safety of NPC 200 for potential therapeutic applications.
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| References | |
| Additional Infomation |
8-Phenyl-1,3-dipropyl-7H-purine-2,6-dione is an oxopurine.
NPC 200 (CAS: 85872-53-3) is a research compound used to study adenosine A1 receptor function and its role in cardiovascular regulation. The compound is also known as 1,3-Dipropyl-8-phenylxanthine. NPC 200 is a potent A1 receptor-selective antagonist that has been used in receptor binding, biochemical, and physiological assays. NPC 200 is not approved for human use and is intended for research purposes only. |
| Molecular Formula |
C17H20N4O2
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|---|---|
| Molecular Weight |
312.37
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| Exact Mass |
312.159
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| CAS # |
85872-53-3
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| PubChem CID |
128784
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.218g/cm3
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| Boiling Point |
539.1ºC at 760 mmHg
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| Flash Point |
279.8ºC
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| Index of Refraction |
1.587
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| LogP |
2.373
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
23
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| Complexity |
450
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCCN1C2=C(C(=O)N(CCC)C1=O)N=C(C3=CC=CC=C3)N2
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| InChi Key |
CLIGSMOZKDCDRZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H20N4O2/c1-3-10-20-15-13(16(22)21(11-4-2)17(20)23)18-14(19-15)12-8-6-5-7-9-12/h5-9H,3-4,10-11H2,1-2H3,(H,18,19)
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| Chemical Name |
8-phenyl-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) |
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 | 3.2013 mL | 16.0067 mL | 32.0133 mL | |
| 5 mM | 0.6403 mL | 3.2013 mL | 6.4027 mL | |
| 10 mM | 0.3201 mL | 1.6007 mL | 3.2013 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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