| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
The primary target is P2X receptors, a family of ATP-gated ion channels. MethADP acts as an antagonist at P2X receptors, blocking ATP-induced cation influx. It is used to study the role of P2X receptors in neurotransmission, inflammation, and pain.
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|---|---|
| ln Vitro |
MethADP (AMP-CP: 20 μM) considerably reduced adenosine synthesis in A498 and RT4 cells (0.96±0.96 μM) in comparison to the untreated control (9.6±1.5 μM), whereas MethADP (100 μM) totally blocks adenosine formation. 1].
MethADP inhibits P2X receptor-mediated calcium influx and cation currents. It is a non-hydrolyzable ATP analog, meaning it is resistant to hydrolysis by ectonucleotidases. It shows antagonist activity at P2X receptors with varying selectivity among subtypes. |
| ln Vivo |
In vivo, MethADP is used in animal models to study purinergic signaling. It inhibits P2X receptor-mediated responses in sensory neurons and reduces pain behavior in rodent models. Typical doses range from 1-10 mg/kg administered intrathecally or locally.
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| Enzyme Assay |
Non-cell assays for MethADP include radioligand binding assays using membranes from cells expressing P2X receptors. The assay employs a radiolabeled ATP analog such as [35S]ATPαS. The compound is incubated with membranes and tracer in assay buffer. Bound radioactivity is separated by filtration and quantified.
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| Cell Assay |
Cell-based assays use cells expressing P2X receptors (HEK293 or oocytes). ATP-induced calcium influx is measured using Fluo-4 or Fura-2. Whole-cell patch clamp recordings measure ATP-induced cation currents. The compound is applied before ATP stimulation.
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| Animal Protocol |
In vivo, MethADP is tested in rodent pain models. A typical protocol involves intrathecal administration (1-10 µg) in rats or mice before formalin or CFA injection. Pain behavior is assessed by flinching or von Frey thresholds. P2X receptor expression is measured by immunohistochemistry.
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| References |
| Molecular Formula |
C11H16N5NAO9P2
|
|---|---|
| Molecular Weight |
447.210134506226
|
| Exact Mass |
447.032
|
| CAS # |
89016-30-8
|
| Related CAS # |
MethADP;3768-14-7;MethADP triammonium
|
| PubChem CID |
71299735
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| Appearance |
Typically exists as solid at room temperature
|
| Hydrogen Bond Donor Count |
5
|
| Hydrogen Bond Acceptor Count |
13
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
28
|
| Complexity |
650
|
| Defined Atom Stereocenter Count |
4
|
| SMILES |
C1=NC(=C2C(=N1)N(C=N2)[C@H]3[C@@H]([C@@H]([C@H](O3)COP(=O)(CP(=O)(O)[O-])O)O)O)N.[Na+]
|
| InChi Key |
RFGZKSPLJPHQMI-YCSZXMBFSA-M
|
| InChi Code |
InChI=1S/C11H17N5O9P2.Na/c12-9-6-10(14-2-13-9)16(3-15-6)11-8(18)7(17)5(25-11)1-24-27(22,23)4-26(19,20)21;/h2-3,5,7-8,11,17-18H,1,4H2,(H,22,23)(H2,12,13,14)(H2,19,20,21);/q;+1/p-1/t5-,7-,8-,11-;/m1./s1
|
| Chemical Name |
sodium;[[(2R,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl]methyl-hydroxyphosphinate
|
| 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)
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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 | 2.2361 mL | 11.1804 mL | 22.3609 mL | |
| 5 mM | 0.4472 mL | 2.2361 mL | 4.4722 mL | |
| 10 mM | 0.2236 mL | 1.1180 mL | 2.2361 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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