Clozic (ICI 55897)
(Synonyms: 氯丁扎利,ICI 55897; Clobuzarit) 目录号 : GC31931Clozic (ICI 55897) 是一种潜在的抗关节炎剂。
Cas No.:22494-47-9
Sample solution is provided at 25 µL, 10mM.
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Cell experiment: | Approximately 3×104 to 5×104 cells/mL medium are seeded into 24-well plates and incubated at 37°C in a humidified atmosphere of 95% air/5% CO2. Medium is replaced with fresh medium containing 20% foetal calf serum and methanol or Clozic under investigation. Cell numbers are determined in replicate wells on various days during culture growth[1]. |
References: [1]. Foster SJ, et al. Anti-proliferative properties of Clozic, a disease-modifying anti-arthritic agent. Biochem Pharmacol. 1983 Feb 1;32(3):461-7. |
Clozic is a potential anti-arthritic agent.
Clozic is a potential anti-arthritic agent. Concentrations of Clozic greater than 50 μM cause a dose-dependent decrease in the amount of matrix protein synthesized by RHMC cell cultures. Inhibition of RHMC cell culture growth by Clozic occurs in a dose-dependent manner. The anti-proliferative effect of Clozic on RHMC cell growth is reversible. Lactate dehydrogenase (LDH) levels in media taken from RHMC cell cultures exposed to 500 μM Clozic for 3 days do not significantly differ from LDH levels in control cell culture media[1].
[1]. Foster SJ, et al. Anti-proliferative properties of Clozic, a disease-modifying anti-arthritic agent. Biochem Pharmacol. 1983 Feb 1;32(3):461-7.
Cas No. | 22494-47-9 | SDF | |
别名 | 氯丁扎利,ICI 55897; Clobuzarit | ||
Canonical SMILES | CC(C)(OCC1=CC=C(C2=CC=C(Cl)C=C2)C=C1)C(O)=O | ||
分子式 | C17H17ClO3 | 分子量 | 304.77 |
溶解度 | Soluble in DMSO | 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。 |
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1 mg | 5 mg | 10 mg | |
1 mM | 3.2812 mL | 16.4058 mL | 32.8116 mL |
5 mM | 0.6562 mL | 3.2812 mL | 6.5623 mL |
10 mM | 0.3281 mL | 1.6406 mL | 3.2812 mL |
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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 | |||
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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。
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Anti-proliferative properties of Clozic, a disease-modifying anti-arthritic agent
Cytostatic drugs have been used in the treatment of rheumatoid arthritis but are of limited clinical application due to their severe toxic side-effects. We have discovered that 'Clozic' (ICI 55897), an agent with disease-modifying properties in rheumatoid arthritis patients, inhibits the growth of a variety of mammalian cell types including a matrix-secreting cell culture derived from neonatal rat hearts. The inhibition of growth was reversible and no loss of cell viability occurred when measured by lactate dehydrogenase released into the medium or by vital staining, suggesting a cytostatic rather than a cytotoxic mechanism. Cytostatic activity was observed at ICI 55897 concentrations within the reported therapeutic plasma concentration range and was related to the concentration of unbound compound, since the effect could be reduced by increasing the albumin concentration in the medium. Other oxyalkanoic acids inhibited cell growth. Their inhibitory potency correlated with lipophilicity. The anti-proliferative potencies of R and S enantiomers of two oxyalkanoic acids containing asymmetric centres were similar. These observations suggest that the anti-proliferative effect of the oxyalkanoic acids is due to their interaction with lipophilic cell target sites.
The effect of drugs on serum histidine levels in rheumatoid arthritis
Groups of 15 patients with active rheumatoid arthritis were treated for 24 weeks with zinc sulphate, trien, captopril, clozic in two doses or a combination of D-penicillamine and hydroxychloroquine. Serum histidine levels were monitored along with measures of disease activity including C-reactive protein, plasma viscosity, articular index, grip strength and early morning stiffness. Zinc sulphate and trien were found to be ineffective while the other drugs all showed evidence of second-line action. Serum histidine was found to improve during successful therapy. The possible cause of low serum histidine and its response to therapy is discussed.
Effects of antirheumatoid drugs on the production and action of porcine catabolin
We report the effects of some common antirheumatic drugs on the production of catabolin from synovium and on its action on cartilage. A method is described to generate reproducible amounts of catabolin from synovial mince. Aspirin, Clozic (ICI 55,897), and gold were without effect on the catabolin system. Penicillamine at high doses enhanced the action of catabolin, while chloroquine inhibited catabolin's effect on cartilage. Prednisolone inhibited the production of catabolin without affecting its action. This inhibition was produced by very low doses of prednisolone (25 ng/ml) and was dose-dependent.
Clozic (ICI 55,897) in rheumatoid arthritis--a controlled comparison with gold
A clinical and biochemical evaluation of Clozic, a novel disease modifying drug in rheumatoid arthritis
We have compared two dose levels of Clozic, a novel agent with potential anti-rheumatoid activity, to D-penicillamine and aspirin in an observer blind randomised parallel group study of 56 patients with active rheumatoid arthritis. Eight clinical assessments and 26 laboratory assessments were performed on each patient at each visit over a six month period. Results were analysed by conventional methods and also by correlation matrices constructed between clinical and laboratory variables. Patients treated with D-penicillamine (500 mg/day) responded adequately and the control group on aspirin (up to 3.6 g of enteric coated formulation/day) performed well, though the withdrawal rate from this latter group was high, predominantly because of continued disease activity. Patients receiving Clozic (100 mg/day or 300 mg/day) improved more than patients receiving penicillamine, particularly at the higher dose. Comparison of methods of analysis validates the use of correlation matrices both for detecting anti-rheumatoid activity and for determining the optimum dose of a novel compound. This trial illustrates the problems of a study of this nature, with the powerful effect on patients of being enrolled in such a closely monitored investigation. It emphasises the greater value of biochemical changes in following disease changes.