| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
hA3 1.65 nM (Ki)
Adenosine A3 receptor (A3AR) is a G protein-coupled receptor that plays important roles in inflammation, immune responses, and other physiological processes. DPTN dihydrochloride is a potent and selective A3AR antagonist with Ki values of 1.65 nM (human), 9.61 nM (mouse), and 8.53 nM (rat). By binding to the A3 receptor, DPTN blocks the activation of the receptor by adenosine or other agonists, thereby inhibiting A3 receptor-mediated signaling pathways. |
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| ln Vitro |
A strong antagonist of rat, mouse, and human A3AR is DPTN. On mice and rats, however, DPTN has less of an impact than human A3AR, and its selectivity is lower (about 20 times lower than that of A2BAR). [1]. The DNPT (10 μM) binding affinity test on the transfected HEK293 cell membrane revealed that, for hA1, hA2A, hA2B, and hA3, the corresponding Ki values were 162±49, 121±42, 230±40, and 1.65±0.57 nM[1]. For mice, the Ki values of DPTN on A1, A2A, A2B, and A3 receptors are 411, 830, 189, and 9.61 nM; for rats, they are 333, 1147, 163, and 8.53 nM.
In vitro, DPTN dihydrochloride is a potent antagonist of human, mouse, and rat A3AR. It exhibits high affinity across species with Ki values of 1.65 nM (human), 9.61 nM (mouse), and 8.53 nM (rat). DPTN is selective for A3AR over A1 and A2A receptors. In functional assays, DPTN inhibits A3 receptor-mediated signaling, including cAMP inhibition and other downstream pathways. |
| ln Vivo |
In vivo, DPTN is used to study A3 receptor-mediated effects in various physiological and pathological processes. It is a validated tool for A3AR research. On mice and rats, DPTN has less of an impact than on human A3AR, and its selectivity is lower (about 20 times lower than that of A2BAR). Despite these species differences, DPTN remains a valuable tool for studying A3 receptor function in animal models.
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| Enzyme Assay |
The in vitro enzyme/receptor binding (cell-free) assay for DPTN dihydrochloride involves radioligand binding assays using membrane preparations from cells expressing human, mouse, or rat A3 receptors. The binding affinity (Ki) and selectivity of DPTN 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 DPTN dihydrochloride use functional assays measuring A3 receptor-mediated signaling (e.g., cAMP inhibition or calcium mobilization) in cells expressing the receptor. Cells expressing A3 receptors are treated with an A3 receptor agonist in the presence or absence of DPTN, 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 are performed to evaluate the pharmacological effects of DPTN on A3 receptor-mediated responses. The compound is used to validate A3AR involvement in various disease models, including inflammation, pain, and cancer. DPTN is administered via various routes, and pharmacodynamic endpoints are measured to assess A3 receptor antagonism.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for DPTN dihydrochloride are limited. As a small molecule, it is suitable for research applications. The compound has a molecular weight appropriate for small-molecule drugs. Further pharmacokinetic studies are needed to fully characterize the absorption, distribution, metabolism, and excretion (ADME) properties of DPTN dihydrochloride.
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| Toxicity/Toxicokinetics |
Preclinical toxicology data for DPTN dihydrochloride 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 DPTN dihydrochloride for potential therapeutic applications.
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| References |
[1]. Zhan-Guo Gao, et al. Pharmacological characterization of DPTN and other selective A3 adenosine receptor antagonist. Purinergic Signal. 2021 Dec;17(4):737-746.
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| Additional Infomation |
DPTN dihydrochloride (CAS: 325767-87-1) is a validated research tool for studying A3 adenosine receptor function and its role in various physiological and disease processes. The compound is also known as N-[4-(3,5-dimethylphenyl)-5-(4-pyridinyl)-2-thiazolyl]-3-pyridinecarboxamide dihydrochloride. DPTN dihydrochloride is a potent and selective A3AR antagonist with Ki values in the range of 0.36 - 1.65 nM for human A3AR and 1.6 - 8.53 nM for rat A3AR. The compound is not approved for human use and is intended for research purposes only.
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| Molecular Formula |
C22H20CL2N4OS
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|---|---|
| Molecular Weight |
459.39
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| Exact Mass |
458.073
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| CAS # |
325767-87-1
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| PubChem CID |
168301117
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| Appearance |
Typically exists as solid at room temperature
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
30
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| Complexity |
517
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl.Cl.S1C(NC(C2C=NC=CC=2)=O)=NC(=C1C1C=CN=CC=1)C1C=C(C)C=C(C)C=1
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| InChi Key |
GTWKWBXTCBUKTR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H18N4OS.2ClH/c1-14-10-15(2)12-18(11-14)19-20(16-5-8-23-9-6-16)28-22(25-19)26-21(27)17-4-3-7-24-13-17;;/h3-13H,1-2H3,(H,25,26,27);2*1H
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| Chemical Name |
N-[4-(3,5-dimethylphenyl)-5-pyridin-4-yl-1,3-thiazol-2-yl]pyridine-3-carboxamide;dihydrochloride
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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: 5 mg/mL (10.88 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 | 2.1768 mL | 10.8840 mL | 21.7680 mL | |
| 5 mM | 0.4354 mL | 2.1768 mL | 4.3536 mL | |
| 10 mM | 0.2177 mL | 1.0884 mL | 2.1768 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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