| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Targets |
The primary target of NF023 hexasodium is the P2X1 purinergic receptor. It acts as a selective and competitive antagonist at this receptor. NF023 displays high selectivity for P2X1 over other P2X receptor subtypes, with IC50 values of 0.21 μM for human P2X1, 28.9 μM for P2X3, and >50 μM and >100 μM for P2X2 and P2X4, respectively. It is also selective over adrenoceptors, histamine, and P2Y receptors.
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| ln Vitro |
Recombinant Go alpha and Gi alpha-1 are the only substances for which NF023 is selective (EC50 value of about 300 nM)[2]. P2X1 receptor inhibition by NF023 is voltage-insensitive. The concentration-response curve is shifted to the right by NF023 (5 and 30 μM), but it has no effect on the peak response to ATP (KB=1.190.2 μM)[4].
In vitro, NF023 is a potent antagonist at the P2X1 receptor, with an IC50 of 0.21 μM for human P2X1-mediated responses. It inhibits P2X1 receptors in a voltage-insensitive manner. At concentrations of 5 and 30 μM, NF023 causes a rightward shift of the ATP concentration-response curve without affecting the maximal response, yielding a KB value of 1.19 μM. Additionally, it selectively inhibits the α-subunit of Go/i proteins with an EC50 of approximately 300 nM. |
| ln Vivo |
In rats with pitting anatomies, NF023 (100 µmol/kg iv) inhibits vasopressor responses to α,β-mATP but not noradrenaline[3].
In vivo, NF023 has been shown to antagonize vasopressor responses in pithed rats. Intravenous administration of NF023 at 100 μmol/kg inhibits the pressor responses induced by the P2X receptor agonist α,β-methylene ATP (α,β-mATP), but does not affect responses to noradrenaline. This demonstrates its functional antagonism of P2X1 receptor-mediated vascular effects in a whole-animal model. |
| Enzyme Assay |
In vitro binding and functional assays for NF023 typically involve cell lines heterologously expressing human P2X receptors. The compound's antagonistic properties are assessed by measuring its ability to inhibit ATP-evoked calcium influx or ion currents using techniques like fluorometric imaging or patch-clamp electrophysiology. IC50 values are determined from concentration-response curves.
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| Cell Assay |
In vitro cellular assays for NF023 are performed using cell lines that recombinantly express P2X1 or other P2X receptor subtypes. Cells are pre-incubated with varying concentrations of NF023, and then stimulated with a P2X receptor agonist like ATP or α,β-mATP. The inhibition of the agonist-induced response, such as calcium mobilization or membrane depolarization, is measured to quantify the antagonist activity.
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| Animal Protocol |
In vivo animal studies for NF023 have been conducted in pithed rats. In this model, the compound is administered intravenously at a dose of 100 μmol/kg. The compound's ability to antagonize P2X1 receptor-mediated vasopressor responses is then assessed by measuring the change in blood pressure in response to the agonist α,β-mATP.
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| ADME/Pharmacokinetics |
NF023 hexasodium has a molecular weight of 1162.88 g/mol and a molecular formula of C35H20N4Na6O21S6. It is highly soluble in water, with a solubility of at least 116.3 mg/mL (100 mM). For storage, the powder should be kept at 4°C in a sealed container, protected from moisture. Solutions can be stored at -80°C for up to 6 months or at -20°C for up to 1 month.
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| Toxicity/Toxicokinetics |
There is no specific toxicity data reported for NF023 hexasodium in the provided literature. As a research chemical, it is intended for laboratory use only and should be handled with standard safety precautions. It is not approved for human therapeutic use.
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| References |
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| Additional Infomation |
NF023 hexasodium is a selective, competitive, and reversible P2X1 receptor antagonist. It is a suramin analog and serves as a key pharmacological tool for studying P2X1 receptor function in various physiological systems, including the cardiovascular, nervous, and immune systems. Its high selectivity for P2X1 over other P2X receptor subtypes makes it particularly valuable for dissecting the specific roles of this receptor.
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| Molecular Formula |
C35H20N4NA6O21S6
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| Molecular Weight |
1162.88
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| Exact Mass |
1161.83
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| CAS # |
104869-31-0
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| PubChem CID |
4466
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| Appearance |
White to off-white solid powder
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| LogP |
8.343
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| Hydrogen Bond Donor Count |
10
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| Hydrogen Bond Acceptor Count |
21
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| Rotatable Bond Count |
12
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| Heavy Atom Count |
66
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| Complexity |
2350
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC(=CC(=C1)NC(=O)NC2=CC=CC(=C2)C(=O)NC3=C4C(=CC(=CC4=C(C=C3)S(=O)(=O)[O-])S(=O)(=O)[O-])S(=O)(=O)[O-])C(=O)NC5=C6C(=CC(=CC6=C(C=C5)S(=O)(=O)[O-])S(=O)(=O)[O-])S(=O)(=O)[O-].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+]
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| InChi Key |
JMONOAYAUIIKMS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C35H26N4O21S6/c40-33(38-25-7-9-27(63(49,50)51)23-13-21(61(43,44)45)15-29(31(23)25)65(55,56)57)17-3-1-5-19(11-17)36-35(42)37-20-6-2-4-18(12-20)34(41)39-26-8-10-28(64(52,53)54)24-14-22(62(46,47)48)16-30(32(24)26)66(58,59)60/h1-16H,(H,38,40)(H,39,41)(H2,36,37,42)(H,43,44,45)(H,46,47,48)(H,49,50,51)(H,52,53,54)(H,55,56,57)(H,58,59,60)
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| Chemical Name |
8-[[3-[[3-[(4,6,8-trisulfonaphthalen-1-yl)carbamoyl]phenyl]carbamoylamino]benzoyl]amino]naphthalene-1,3,5-trisulfonic acid
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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) |
H2O: ≥ 116.3 mg/mL (100.01 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 | 0.8599 mL | 4.2997 mL | 8.5993 mL | |
| 5 mM | 0.1720 mL | 0.8599 mL | 1.7199 mL | |
| 10 mM | 0.0860 mL | 0.4300 mL | 0.8599 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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