| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
| Targets |
(±)-5'-Chloro-5'-deoxy-ENBA targets the adenosine A1 receptor. It is a potent and highly selective agonist of the human adenosine A1 receptor. Activation of A1 receptors inhibits adenylate cyclase, reduces neuronal excitability, and has analgesic and tremorolytic effects. It alleviates neuropathic pain through functional glial and microglial changes. It inhibits excessive glutamatergic transmission in the ventral thalamic nuclei.
|
|---|---|
| ln Vitro |
In vitro, (±)-5'-Chloro-5'-deoxy-ENBA is a potent and highly selective adenosine A1 receptor agonist. It inhibits adenylate cyclase activity and reduces neuronal excitability. It is used as a research tool for studying A1 receptor biology. Exact EC50 values vary by assay.
|
| ln Vivo |
In vivo, (±)-5'-Chloro-5'-deoxy-ENBA alleviates thermal hyperalgesia and mechanical allodynia in a mouse model of neuropathic pain (Spared Nerve Injury) through functional glial and microglial changes without affecting motor or cardiovascular functions. It also has tremorolytic effects in the harmaline-induced model of essential tremor in rats.
|
| Enzyme Assay |
For non-cell receptor binding assays, membranes from cells expressing adenosine A1 receptors are incubated with radiolabeled A1 receptor agonist (e.g., [3H]CCPA) and (±)-5'-Chloro-5'-deoxy-ENBA at serial dilutions. Bound radioligand is separated by filtration and counted. Ki values are calculated from competition curves.
|
| Cell Assay |
In cell assays, cells expressing adenosine A1 receptors are treated with (±)-5'-Chloro-5'-deoxy-ENBA. cAMP accumulation is measured by radioimmunoassay or ELISA. Calcium flux is measured using fluorescent dyes. Receptor binding is assessed by radioligand binding.
|
| Animal Protocol |
In vivo animal protocols use mice with Spared Nerve Injury (SNI) or rats with harmaline-induced tremor. (±)-5'-Chloro-5'-deoxy-ENBA is dissolved in saline and administered intraperitoneally or intrathecally. Thermal hyperalgesia and mechanical allodynia are assessed. Tremor is measured by electromyography. Microglial activation is assessed by immunohistochemistry.
|
| References |
| Molecular Formula |
C17H22N5O3CL
|
|---|---|
| Molecular Weight |
379.84128
|
| Exact Mass |
379.141
|
| CAS # |
103626-26-2
|
| PubChem CID |
42636897
|
| Appearance |
Typically exists as solid at room temperature
|
| LogP |
1.357
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
26
|
| Complexity |
531
|
| Defined Atom Stereocenter Count |
4
|
| SMILES |
C1CC2CC1CC2NC3=C4C(=NC=N3)N(C=N4)C5C(C(C(O5)CCl)O)O
|
| 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 (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
|
|---|---|
| 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 | 2.6327 mL | 13.1634 mL | 26.3269 mL | |
| 5 mM | 0.5265 mL | 2.6327 mL | 5.2654 mL | |
| 10 mM | 0.2633 mL | 1.3163 mL | 2.6327 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
