Tinoridine hydrochloride (Y-3642 hydrochloride)
(Synonyms: 盐酸替诺立定,Y-3642 hydrochloride) 目录号 : GC31882
Tinoridine hydrochloride (Y-3642) is a non-steroidal anti-inflammatory drug with a potent antiperoxidative activity.
Cas No.:25913-34-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Kinase experiment: | CCl4 aministration produces a marked decrease in the concentrations of liver microsomal cytochrome P-450 and G6Pase, indicating that hepatic endoplasmic reticulum function is disrupted. Prior treatment of the animals with tinoridine (100 mg/kg) significantly reduces the CCl4-induced alterations in the enzyme activities, and a rapid recovery toward the normal values is observed[2]. |
Animal experiment: | Rat: Male Wistar rats (180-220 g) are used in the experiments. Drugs (Tinoridine) are given orally as a suspension in 0.5% methylcellulose solution 1 hr before CCl4, administration. Control animals receive an equivalent amount of the vehicle. CCl4 is administered ip at a dose of 0.25 ml/kg as a 5% (v/v) solution in olive oil. The animals are killed by carotid excision at different times after CCl4 administration; the livers are rapidly removed, weighed and processed for biochemical or histologic analysis[2]. |
References: [1]. O Shimada, et al. Hydroxyl radical scavenging action of tinoridine. Agents Actions. 1986 Nov;19(3-4):208-14. | |
Tinoridine hydrochloride (Y-3642) is a non-steroidal anti-inflammatory drug with a potent antiperoxidative activity.
| Cas No. | 25913-34-2 | SDF | |
| 别名 | 盐酸替诺立定,Y-3642 hydrochloride | ||
| Canonical SMILES | O=C(C1=C(N)SC2=C1CCN(CC3=CC=CC=C3)C2)OCC.Cl | ||
| 分子式 | C17H21ClN2O2S | 分子量 | 352.88 |
| 溶解度 | DMSO : ≥ 31 mg/mL (87.85 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Comprehensive degradation profiling and influence of different oxidizing reagents on tinoridine hydrochloride: Structural characterization of its degradation products using HPLC and HRMS
Rationale: Stress testing on tinoridine hydrochloride was carried out using a multidimensional approach. This included different conditions: hydrolytic (acidic, alkaline, and neutral conditions), different oxidative reagents, thermal, photolytic conditions, HPLC method development, and structural elucidation using high-resolution mass spectrometry (HRMS). It provides the basis for quality control of tinoridine hydrochloride and its derivatives during storage conditions. Methods: The tinoridine hydrochloride was subjected to a variety of stress conditions. A gradient reversed-phase HPLC method was developed on a X-Bridge C18 column (250 × 4.6 mm, 5 μm) to separate all the degradation products (DPs). HRMS studies have been performed to elucidate the structure of DPs. Results: HPLC-PDA study revealed that significant degradation products were formed in hydrolytic, AIBN (radical initiator at 40°C), thermal, and solid-state photolight stress conditions, but the drug was stable under oxidative conditions (H2 O2, Fenton's reagent at room temperature and ferric chloride at 40°C). The structure of degradation products was elucidated, and mechanism of their formation was explained. Conclusion: Stress study was successfully carried out as per ICH Q1A (R2) guideline on tinoridine hydrochloride. A total of six new degradation products were characterized, DP 2 and DP 6 formed by the effect of co-solvent. This study provides the scientifically sound basis for quality monitoring and storage conditions of tinoridine hydrochloride.
Effects of 2-(4-(2-imidazo[1,2-a]pyridyl)phenyl) propionic acid (Y-9213) and anti-inflammatory drugs on erythrocytes, polymorphonuclear leukocytes and lysosomes in vitro
2-(4-(2-Imidazo[1,2-a]pyridyl)phenyl)propionic acid (Y-9213) with analgesic, antipyretic and anti-inflammatory activities significantly inhibited hemolysis of rat erythrocytes. Activity of Y-9213 (100--500 micrometer) on hemolysis was more potent than that of phenylbutazone, and less potent than that of indomethacin. The spontaneous release of enzymes from rat liver lysosomes by incubation alone was significantly inhibited by Y-9213 (1--100 micrometer) to the same degrees as phenylbutazone or tinoridine hydrochloride. Release of enzymes from the lysosomes by addition of phospholipase C (PLC, 0.03 units/ml) was slightly inhibited by Y-9213 (10--100 micrometer) and phenylbutazone (100 micrometer). Dexamethasone, prednisolone, hydrocortisone and tinoridine hydrochloride (1--10 micrometer) inhibited more potently the PLC-induced release than the spontaneous release. Y-9213 (1--100 micrometer) inhibited considerably the release of enzymes from intact lysosomes of rabbit polymorphonuclear (PMN) leukocytes. The release of enzymes from the PMN leukocyte lysosomes preincubated at 37 degrees C for 15 min was strongly inhibited by dexamethasone, prednisolone and hydrocortisone (1--100 micrometer), but not by Y-9213, phenylbutazone and indomethacin (100 micrometer). Y-9213 (0.1--10 micrometer) also inhibited significantly the phagocytic secretion of lysosomal enzymes from PMN leukocytes without affecting phagocytosis of the particles. Activity of this agent was similar to that of phenylbutazone, and less active than that of indomethacin, dexamethasone or prednisolone. Our results suggest that Y-9213 may stabilize membranes of erythrocytes and lysosomes and inhibit phagocytic secretion of lysosomal constitutents from PMN leukocytes.