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CPT

Cat No.:V18771 Purity: ≥98%
8-Cyclopentyl-1,3-dimethylxanthine (Compound 2a) is a selective adenosine A1 receptor blocker (antagonist) with Kis of 10.9 nM and 1440 nM for A1 and A2 receptors, respectively.
CPT
CPT Chemical Structure CAS No.: 35873-49-5
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
10mg
50mg
100mg
250mg
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Product Description
8-Cyclopentyl-1,3-dimethylxanthine (Compound 2a) is a selective adenosine A1 receptor blocker (antagonist) with Kis of 10.9 nM and 1440 nM for A1 and A2 receptors, respectively.
CPT, also known as 8-cyclopentyl-1,3-dimethylxanthine, is a selective adenosine A1 receptor antagonist. It has Ki values of 10.9 nM for the A1 receptor and 1440 nM for the A2 receptor, demonstrating high selectivity for the A1 subtype. CPT is a potent antagonist of the adenosine A1 receptor and is used as a pharmacological tool to study the role of A1 receptors in various physiological processes. It has a molecular formula of C12H16N4O2 and a molecular weight of 248.28.
Biological Activity I Assay Protocols (From Reference)
Targets
CPT targets the adenosine A1 receptor. It acts as a potent and selective antagonist, binding to the receptor and preventing its activation by endogenous adenosine. It shows high selectivity for the A1 receptor over the A2 receptor, with a Ki of 10.9 nM for A1 and 1440 nM for A2. This selectivity makes it a valuable tool for studying the specific functions of the A1 receptor.
ln Vitro
In vitro, CPT is a potent and selective antagonist of the adenosine A1 receptor. It binds to the A1 receptor with high affinity (Ki = 10.9 nM) and shows much lower affinity for the A2 receptor (Ki = 1440 nM). This selectivity allows researchers to study A1 receptor-mediated effects without significant interference from A2 receptor activity.
ln Vivo
In vivo, CPT is used as a pharmacological tool to study the role of adenosine A1 receptors in various physiological processes, including cardiovascular function, neuroprotection, and renal function. Its ability to selectively block A1 receptors makes it useful for investigating the therapeutic potential of A1 receptor antagonists in conditions such as heart failure and neurodegenerative diseases. However, specific in vivo study details are not extensively documented.
Enzyme Assay
CPT is evaluated in cell-free receptor binding assays to determine its affinity for adenosine receptors. Radioligand binding displacement assays are performed using membrane preparations expressing A1 and A2 receptors. Competition binding experiments are conducted with increasing concentrations of CPT and a fixed concentration of a labeled reference ligand. Ki values are determined to quantify the potency of receptor binding.
Cell Assay
CPT is assessed in cell-based functional assays to measure its antagonist activity at the A1 receptor. Cells expressing the A1 receptor are treated with CPT, and receptor activation is measured by assessing downstream signaling pathways, such as the inhibition of adenylyl cyclase activity. The compound's ability to block agonist-induced receptor activation is evaluated.
Animal Protocol
CPT is administered in animal models to evaluate its effects on A1 receptor-mediated functions. It has been used to study the role of A1 receptors in cardiovascular and neurological disorders. Efficacy is assessed by measuring physiological parameters such as heart rate, blood pressure, and neuroprotection. However, specific animal study protocols are not extensively documented.
ADME/Pharmacokinetics
CPT has a molecular formula of C12H16N4O2 and a molecular weight of 248.28. Its CAS number is 35873-49-5. The compound is a solid. It is soluble in DMSO. It should be stored under recommended conditions. It is also known as 8-cyclopentyl-1,3-dimethylxanthine.
Toxicity/Toxicokinetics
No detailed toxicity data is available for CPT. The compound is for research use only and is not intended for human therapeutic use. It is a selective A1 receptor antagonist used as a pharmacological tool.
Additional Infomation
8-Cyclopentyl-1,3-dimethyl-7H-purine-2,6-dione is an oxopurine.
CPT is a selective adenosine A1 receptor antagonist. It is also known as 8-cyclopentyl-1,3-dimethylxanthine. It is used in research to study the role of A1 receptors in various physiological and pathological processes. The compound is not approved for clinical use.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C12H16N4O2
Molecular Weight
248.28104
Exact Mass
248.127
CAS #
35873-49-5
PubChem CID
1917
Appearance
Typically exists as solid at room temperature
Density
1.332g/cm3
Boiling Point
513.1ºC at 760mmHg
Melting Point
250-252ºC
Flash Point
264.1ºC
Index of Refraction
1.607
LogP
0.617
Hydrogen Bond Donor Count
1
Hydrogen Bond Acceptor Count
3
Rotatable Bond Count
1
Heavy Atom Count
18
Complexity
380
Defined Atom Stereocenter Count
0
SMILES
CN1C2=C(C(=O)N(C)C1=O)N=C(C3CCCC3)N2
InChi Key
SCVHFRLUNIOSGI-UHFFFAOYSA-N
InChi Code
InChI=1S/C12H16N4O2/c1-15-10-8(11(17)16(2)12(15)18)13-9(14-10)7-5-3-4-6-7/h7H,3-6H2,1-2H3,(H,13,14)
Chemical Name
8-cyclopentyl-1,3-dimethyl-7H-purine-2,6-dione
HS Tariff Code
2934.99.9001
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)
Solubility Data
Solubility (In Vitro)
DMSO : ~20 mg/mL (~80.55 mM)
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
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*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 : PEG300Tween 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).
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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)]
*Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL 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).
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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders


Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 4.0277 mL 20.1386 mL 40.2771 mL
5 mM 0.8055 mL 4.0277 mL 8.0554 mL
10 mM 0.4028 mL 2.0139 mL 4.0277 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.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
  • Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume
An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
  • To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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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