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| 25mg |
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Purity: ≥98%
Tinoridine HCl (also known as Y-3642 HCl), the hydrochloride of tinoridine (Y-3642), is a nonsteroidal anti-inflammatory drug (NSAID) that also has potent radical scavenger and antiperoxidative activity. At concentrations from 5 μM to 100 μM, tinoridine can produce a concentration-dependent inhibition on the simultaneous increases in lipid peroxide formation and renin release induced by 50 μM ascorbic acid in the renin granule fraction. While other NSAIDs and steroids such as indomethacin, hydrocortisone and prednisolone do not inhibit the lipid peroxidation in the renin granule fraction, did not influence the release of renin from the granules, suggesting that tinoridine suppresses renin release by inhibiting the oxidative disintegration of membranes of renin granules.
| ln Vitro |
Tinoridine's capacity to scavenge free radicals is demonstrated by its reduction of diphenyl-p-picrylhydrazyl, a stable free radical, at a molar ratio of roughly 1:2. In the presence of ADP and Fe2+, tinoridine prevents the formation of hydroxyl radicals during lipid peroxidation in rat liver microsomes caused by the xanthine-xanthine oxidase system. It is shown that tinoridine is oxidized during lipid peroxidation by monitoring the fluorescence that results from tinoridine's oxidation product. When Fe2+ is present, the xanthine-xanthine oxidase system oxidizes it as well; when Fe2+ is not present, catalase almost entirely inhibits its oxidation, which is sluggish. Superoxide radical-induced cytochrome c reduction is unaffected by tinoridine oxidation, which is also mediated by the H2O2-Fe2+ system and produces OH (Fenton reaction) [1].
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| ln Vivo |
Liver microsomal cytochrome P-450 and G6Pase concentrations are significantly reduced upon CCl4 aministration, suggesting a disruption in hepatic endoplasmic reticulum function. When animals are given 100 mg/kg of tinoridine beforehand, the alterations in enzyme activities caused by CCl4 are significantly reduced, and the animals quickly return to their normal values[2].
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| References |
[1]. O Shimada, et al. Hydroxyl radical scavenging action of tinoridine. Agents Actions. 1986 Nov;19(3-4):208-14.
[2]. Yasuda H, et al. The protective effect of tinoridine against carbon tetrachloride hepatotoxicity. Toxicol Appl Pharmacol. 1980 Mar 15;52(3):407-13 |
| Molecular Formula |
C17H21CLN2O2S
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| Molecular Weight |
352.88
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| CAS # |
25913-34-2
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| Related CAS # |
24237-54-5;25913-34-2 (HCl);
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| SMILES |
O=C(C1=C(N)SC2=C1CCN(CC3=CC=CC=C3)C2)OCC.Cl
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| Chemical Name |
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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. |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.67 mg/mL (4.73 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.67 mg/mL (4.73 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8338 mL | 14.1691 mL | 28.3382 mL | |
| 5 mM | 0.5668 mL | 2.8338 mL | 5.6676 mL | |
| 10 mM | 0.2834 mL | 1.4169 mL | 2.8338 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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