| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Pipazethate targets the GABA receptor as a potent antagonist. It also acts on the cough center in the medulla oblongata to exert its antitussive effects. The compound is described as an aryl sulfide with central antitussive activity.
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|---|---|
| ln Vitro |
In vitro studies show that Pipazethate acts as a potent GABA antagonist. The compound demonstrates antitussive activity in pharmacological assays. Its pyridobenzothiazine structure contributes to its pharmacological properties.
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| ln Vivo |
In vivo, Pipazethate exerts its antitussive effects by acting on the cough center in the medulla oblongata. It has been studied for cough relief in animal models and clinical settings. The compound also acts as a respiratory stimulant and bronchodilator by relaxing airway smooth muscle.
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| Enzyme Assay |
In vitro receptor binding assays typically measure the displacement of a radiolabeled GABA receptor ligand from brain membrane preparations. Pipazethate is incubated with membrane preparations and a radioactive GABA receptor antagonist, and the IC50 is determined. Functional assays may measure GABA-induced chloride flux in the presence of the compound to assess its antagonist activity.
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| Cell Assay |
In vitro cellular assays evaluate the effects of Pipazethate on neuronal cells expressing GABA receptors. The compound's ability to block GABA-induced currents is measured using patch-clamp electrophysiology or calcium imaging. Cytotoxicity and cell viability assays are also performed to assess the safety profile of the compound in relevant cell types.
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| Animal Protocol |
In vivo animal experiments are conducted in rodent models of cough induced by irritants such as capsaicin or citric acid. Pipazethate is administered orally, and the number of coughs is counted. The compound's antitussive efficacy is compared to that of standard antitussive agents. Respiratory function and bronchodilator effects may also be assessed.
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| ADME/Pharmacokinetics |
Pipazethate has a molecular formula of C21H25N3O3S and a molecular weight of 399.51. It has a logP of 4.326. The compound is soluble in DMSO and should be stored as a powder at -20°C for long-term storage. Its IUPAC name is 2-(2-piperidin-1-ylethoxy)ethyl pyrido[3,2-b][1,4]benzothiazine-10-carboxylate.
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| Toxicity/Toxicokinetics |
The toxicity profile of Pipazethate is consistent with that of other antitussive agents. As a non-narcotic antitussive, it is expected to have a lower abuse potential compared to opioid-based cough suppressants. Common side effects may include gastrointestinal disturbances and central nervous system effects at high doses.
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| References | |
| Additional Infomation |
Pipazetate is an aryl sulfide. It is a non-narcotic oral antitussive. Indications: For the treatment of cough. Pharmacodynamics: Antitussives exert their central effects by acting on the cough center in the medulla oblongata.
Pipazethate is also known by the synonyms Pipazetate and SKF 70230A. It has been used clinically for the treatment of cough. The compound is a phenothiazine derivative with antitussive and GABA antagonist properties. It is available as a research reagent for pharmacological studies. |
| Molecular Formula |
C21H25N3O3S
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|---|---|
| Molecular Weight |
399.51
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| Exact Mass |
399.162
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| CAS # |
2167-85-3
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| Related CAS # |
6056-11-7 (HCl); 2167-85-3;
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| PubChem CID |
22425
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.26g/cm3
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| Boiling Point |
553.3ºC at 760mmHg
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| Flash Point |
288.4ºC
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| Vapour Pressure |
2.76E-12mmHg at 25°C
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| Index of Refraction |
1.612
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| LogP |
4.326
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
28
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| Complexity |
503
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
DTVJXCOMJLLMAK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H25N3O3S/c25-21(27-16-15-26-14-13-23-11-4-1-5-12-23)24-17-7-2-3-8-18(17)28-19-9-6-10-22-20(19)24/h2-3,6-10H,1,4-5,11-16H2
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| Chemical Name |
2-(2-piperidin-1-ylethoxy)ethyl pyrido[3,2-b][1,4]benzothiazine-10-carboxylate
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| Synonyms |
Pipazetate; Pipazethate; Pipazethate
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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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 | 2.5031 mL | 12.5153 mL | 25.0307 mL | |
| 5 mM | 0.5006 mL | 2.5031 mL | 5.0061 mL | |
| 10 mM | 0.2503 mL | 1.2515 mL | 2.5031 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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