| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
Selectively and competitively targets the rat P2X2 receptor. It exhibits a competitive mechanism of action with a pA2 value of 7.49.
|
|---|---|
| ln Vitro |
PSB-1011 sodium demonstrates a Ki value of 79 nM for the rat P2X2 receptor. It is >100-fold selective versus P2X4, P2X7, and several investigated P2Y receptor subtypes.
|
| ln Vivo |
No detailed in vivo activity data for PSB-1011 sodium is available in the provided search results. It is primarily described as an in vitro research tool for studying purinergic signaling.
|
| Enzyme Assay |
Non-cell-based binding assays are performed to determine the compound's affinity for the P2X2 receptor. Competitive binding studies are conducted using radiolabeled ligands and membrane preparations from cells expressing the rat P2X2 receptor to calculate the Ki value.
|
| Cell Assay |
In vitro cell-based assays are conducted using cell lines expressing the rat P2X2 receptor. The compound's antagonist activity is evaluated by measuring its ability to inhibit ATP-gated ion flux, typically using electrophysiological techniques or fluorescent-based calcium influx assays.
|
| Animal Protocol |
In vivo animal studies for PSB-1011 sodium are not described in the provided literature, as the compound is predominantly utilized as a research tool for in vitro investigations of P2X2 receptor function and purinergic signaling pathways.
|
| References |
| Molecular Formula |
C23H14CL2N6O8S2.2NA
|
|---|---|
| Molecular Weight |
681.39200
|
| Exact Mass |
679.933
|
| CAS # |
4499-01-8
|
| Related CAS # |
4499-01-8 (sodium);13324-20-4 (free acid);
|
| PubChem CID |
78253
|
| Appearance |
Typically exists as solid at room temperature
|
| LogP |
5.72
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
14
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
43
|
| Complexity |
1200
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C1=CC=C2C(=C1)C(=O)C3=C(C(=C(C=C3NC4=CC(=C(C=C4)S(=O)(=O)O)N=C5NC(=NC(=N5)Cl)Cl)S(=O)(=O)O)N)C2=O.[Na].[Na].[H].[H]
|
| InChi Key |
DHHMYWVFMSHEIP-UHFFFAOYSA-L
|
| InChi Code |
InChI=1S/C23H14Cl2N6O8S2.2Na/c24-21-29-22(25)31-23(30-21)28-12-7-9(5-6-14(12)40(34,35)36)27-13-8-15(41(37,38)39)18(26)17-16(13)19(32)10-3-1-2-4-11(10)20(17)33;;/h1-8,27H,26H2,(H,34,35,36)(H,37,38,39)(H,28,29,30,31);;/q;2*+1/p-2
|
| Chemical Name |
disodium;1-amino-4-[3-[(4,6-dichloro-1,3,5-triazin-2-yl)amino]-4-sulfonatoanilino]-9,10-dioxoanthracene-2-sulfonate
|
| 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 | 1.4676 mL | 7.3379 mL | 14.6759 mL | |
| 5 mM | 0.2935 mL | 1.4676 mL | 2.9352 mL | |
| 10 mM | 0.1468 mL | 0.7338 mL | 1.4676 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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