| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 100mg | |||
| Other Sizes |
| Targets |
Carboxy-PTIO acts as a direct nitric oxide (NO) scavenger. Its primary mechanism of action is to chemically react with and neutralize NO, thereby inhibiting NO-mediated signaling pathways. By removing NO from the system, it can block downstream effects that are dependent on the NO-cGMP-PKG signaling pathway. This makes it a useful tool for studying the role of NO in various biological systems, including its effects on vascular tone, neurotransmission, and inflammation.
|
|---|---|
| ln Vitro |
The enhancement of NO expression generated by Physalin A treatment was greatly decreased by Carboxy-PTIO k (200 μM; 1 hour before Physalin A; 24 hours); however, Carboxy-PTIO therapy alone did not cause any alterations [1]. μM; Physalin A 1 hour; 24 hours) decreases internal procaspase-3 and PARP caused by physalin A, impairs the expression of ICAD, and lessens nucleus DNA fragmentation [1]. Carboxy-PTIO Potassium (200 μM; Physalin A 1 hour ago) did not affect iNOS expression, but it did reverse the downregulation of mTOR and p-mTOR levels in A375-S2 cells caused by Physalin A. It also inhibited LC3 in I to LC3; 24 hr.
Carboxy-PTIO has been shown to block in vitro vascular relaxation stimulated by NO. In cellular models, pretreatment with Carboxy-PTIO has been used to study the role of NO in various processes. For example, in A375-S2 cells, pretreatment with Carboxy-PTIO (200 μM for 1 hour) has been employed to investigate the effects of other compounds, such as Physalin A, helping to determine if their actions are mediated through NO pathways. Its primary in vitro function is as a reliable tool for scavenging NO in cell culture and biochemical assays. |
| ln Vivo |
In LPS treatment, carboxy-PTIO (intravenous; 0.056-1.70 mg/kg/min; administered for 1 hour beginning 90 minutes after LPS injection) reduces newborn rates, hypotension, and renal failure.
In vivo, Carboxy-PTIO is primarily used to study the effects of NO in animal models. In lipopolysaccharide (LPS)-induced rat models of endotoxic shock, Carboxy-PTIO has been shown to prevent hypotension and renal dysfunction through its direct scavenging action on NO. This treatment has also been reported to increase survival in these models. These in vivo effects confirm the compound's ability to counteract the pathophysiological effects of excessive NO production during systemic inflammation. |
| Enzyme Assay |
Carboxy-PTIO is a chemical NO scavenger, and its activity is typically confirmed in cell-free systems by demonstrating its ability to react with and neutralize NO. A common experimental protocol involves incubating Carboxy-PTIO with a known NO donor in a suitable buffer at room temperature or 37°C. The reaction stoichiometry and kinetics can be monitored spectrophotometrically or by using an NO-sensitive electrode. The disappearance of NO or the formation of the reaction products (NO2 and carboxy-PTI derivatives) confirms the scavenging activity.
|
| Cell Assay |
Western Blot Analysis[1]
Cell Types: A375-S2 Cell Tested Concentrations: 200 μM Incubation Duration: 1 h before conversion of physalin A; II[1]. 24-hour Experimental Results: Physalin A-induced cleavage of procaspase-3 and PARP was diminished. The primary in vitro cellular experimental protocol for Carboxy-PTIO involves treating cells with the compound prior to or concurrently with an NO donor or a stimulus that induces NO production. For instance, cells such as A375-S2 are pretreated with Carboxy-PTIO potassium salt at a concentration of 200 μM for 1 hour. This is followed by the addition of the test compound or stimulus. The subsequent cellular responses are then measured and compared to control groups to determine the contribution of NO to the observed effects. |
| Animal Protocol |
Animal/Disease Models: SD rats [3]
Doses: 0.056-1.70 mg/kg/min Route of Administration: intravenous (iv) (iv)injection; it does not affect the parameters of normal mice [3]. 0.056-1.70 mg/kg/min; Infusion started 90 minutes after LPS injection for 1 hour and 90 minutes. Experimental Results: Through the direct scavenging effect of NO, it demonstrated effective therapeutic value in endotoxic shock. Dosing in animal models is typically based on the specific model and route of administration. While detailed standard protocols are not universally published, a common application is in LPS-induced endotoxic shock models in rats. In these studies, Carboxy-PTIO is often administered via intravenous injection. The dosage and timing are optimized to counteract the hypotensive effects of LPS. A typical approach involves administering Carboxy-PTIO either before or shortly after LPS challenge to assess its protective effects on blood pressure and renal function. |
| ADME/Pharmacokinetics |
As a small molecule NO scavenger, Carboxy-PTIO is expected to have a rapid distribution and a short half-life in vivo due to its reaction with NO and subsequent clearance. Specific pharmacokinetic parameters (e.g., half-life, volume of distribution, clearance) are not typically the focus of its use as a research tool. The compound is known to be water-soluble, which facilitates its administration in biological systems. Its primary route of elimination is likely through renal excretion after its reaction with NO.
|
| Toxicity/Toxicokinetics |
Carboxy-PTIO is generally considered a safe research tool for in vitro and in vivo use at standard concentrations. However, as with any chemical, it should be handled with appropriate laboratory safety precautions. The compound's toxicity profile is not extensively documented, but as it is a radical scavenger, its effects are primarily related to its pharmacological action of neutralizing NO. In animal models, it is used at doses that are effective for scavenging NO without causing overt toxicity.
|
| References |
|
| Additional Infomation |
Carboxy-PTIO is a research-grade biochemical tool and is not a therapeutic drug for human use. It has not been approved for clinical applications. Its primary value lies in its ability to selectively scavenge NO, making it a critical reagent for studying nitric oxide biology. Common synonyms for Carboxy-PTIO include 2-(4-Carboxyphenyl)-4,4,5,5-tetramethylimidazoline-1-oxyl-3-oxide and its potassium salt form, cPTIO. It is often used in combination with other pharmacological tools to dissect complex signaling pathways involving NO.
|
| Molecular Formula |
C14H16KN2O4
|
|---|---|
| Molecular Weight |
315.39
|
| Exact Mass |
315.074
|
| CAS # |
148819-94-7
|
| Related CAS # |
Carboxy-PTIO;145757-47-7
|
| Appearance |
Brown to black solid powder
|
| Boiling Point |
456.3ºC at 760 mmHg
|
| Melting Point |
141-143°C
|
| Flash Point |
229.7ºC
|
| LogP |
1.756
|
| 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 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)
|
| Solubility (In Vitro) |
H2O : ~25 mg/mL (~79.27 mM)
DMSO : ~10 mg/mL (~31.71 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 50 mg/mL (158.53 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1707 mL | 15.8534 mL | 31.7068 mL | |
| 5 mM | 0.6341 mL | 3.1707 mL | 6.3414 mL | |
| 10 mM | 0.3171 mL | 1.5853 mL | 3.1707 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
