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.

Physicochemical Properties

Molecular Formula	C17H21CLN2O2S
Molecular Weight	352.88
Exact Mass	352.101
CAS #	25913-34-2
Related CAS #	24237-54-5;25913-34-2 (HCl);
PubChem CID	134896
Appearance	White to yellow solid powder
Density	1.256g/cm3
Boiling Point	493.5ºC at 760mmHg
Melting Point	234-235° (dec)
Flash Point	252.3ºC
Vapour Pressure	7E-10mmHg at 25°C
LogP	4.386
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	5
Rotatable Bond Count	5
Heavy Atom Count	23
Complexity	387
Defined Atom Stereocenter Count	0
InChi Key	LMAQHEGFQZGATE-UHFFFAOYSA-N
InChi Code	InChI=1S/C17H20N2O2S.ClH/c1-2-21-17(20)15-13-8-9-19(11-14(13)22-16(15)18)10-12-6-4-3-5-7-12;/h3-7H,2,8-11,18H2,1H3;1H
Chemical Name	2-Amino-3-ethoxycarbonyl-6-benzyl-4,5,6,7-tetrahydrothieno(2,3-c)pyridine monohydrochloride
Synonyms	Y3642; Y-3642 hydrochloride;Tinoridine hydrochloride; Tinoridine HCl; Y-3642; Y3642 HCl; Y3642 hydrochloride
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)

Biological Activity

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].
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].
Animal Protocol	Formulated in 0.5% methylcellulose solution; p.o. Male Wistar rats
References	[1]. Hydroxyl radical scavenging action of tinoridine. Agents Actions. 1986 Nov;19(3-4):208-14. [2]. The protective effect of tinoridine against carbon tetrachloride hepatotoxicity. Toxicol Appl Pharmacol. 1980 Mar 15;52(3):407-13.
Additional Infomation	Tinoridine hydrochloride is a thienopyridine.

Solubility Data

Solubility (In Vitro)

DMSO:10 mM Water:N/A Ethanol:N/A

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.