CGS 21595
CGS 21595 is an orally active 5-lipoxygenase inhibitor that blocks the synthesis of 5-hydroxyeicosatetraenoic acid and leukotriene B4. CGS 21595 acts as a prodrug and metabolizes into CGS 19213. CGS 21595 induces lesions in the spinal nerve roots and sciatic nerves of rats, causing mild functional impairments including reduced grip strength, increased spread of the landing feet, and decreased motor activity. CGS 21595 exhibits dose-dependent neurotoxicity in rats, and induces reversible cytoplasmic hyaline droplets in the proximal renal tubules of both male and female rats. CGS 21595 can be used in studies of peripheral toxic neuropathy.
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- CAS 番号: 121412-39-3
- 分子式: C21H25NO4
- 分子量:355.43
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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5-Lipoxygenase |
CGS 21595 (1000 mg/kg; p.o.; 5 days per week; for up to 10 weeks) induces Schwann cell-targeted segmental demyelination in the peripheral segment of spinal nerve roots, and causes mild functional impairments, including reduced grip strength, increased hind paw splay, and decreased motor activity[2].
CGS 21595 (50-1000 mg/kg; p.o.; 5 days per week; for 10 weeks) induces dose-dependent peripheral segmental demyelination, with significant functional deficits and demyelinating changes occurring only at the 1000 mg/kg dose[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male, 8-week-old, 223-302 g; female, 8-week-old, 163-204 g)[1]
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Dosage:50 mg/kg; 150 mg/kg; 500 mg/kg; 1000 mg/kg
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Administration:p.o.; daily; 13 weeks
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Result:Induced peripheral neuropathy with spinal and sciatic myelin injury.
Triggered universal renal proximal tubular hyaline droplets in rats of both sexes across all test doses.
Suppressed body weight gain in a dose-dependent manner for males at ≥150 mg/kg and females at ≥500 mg/kg.
Retained attenuated neuropathic lesions in all 1000 mg/kg-dosed rats after a 4-week recovery period.
Eliminated renal lesions and weight gain deficits entirely within the 4-week recovery phase.
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Animal Model:Sprague-Dawley derived albino rats (male and female, 8 weeks old)[2]
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Dosage:1000 mg/kg
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Administration:p.o.; 5 days per week; up to 10 weeks
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Result:Observed no clinical or body weight anomalies.
Reduced grip strength starting week 4.
Increased landing foot splay at week 10.
Suppressed all male motor activity parameters at week 10.
Lowered female horizontal and vertical locomotion from week 8.
Detected early spinal root myelin swelling, lamellar damage and microvesiculation at week 4.
Identified late-stage demyelination, macrophage infiltration, thin remyelination and occasional onion bulbs.
Found lesions spread to major leg nerves by week 10, leaving distal plantar nerve unaffected.
Validated central nervous myelin remained undamaged.
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Animal Model:Sprague-Dawley derived albino rats (male, 8 weeks old)[2]
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Dosage:50 mg/kg; 200 mg/kg; 1000 mg/kg
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Administration:p.o.; 5 days per week; 10 weeks
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Result:Detected prominent limb grip strength loss at weeks 7/10 under 1000 mg/kg.
Found persistent vertical activity suppression from week 7 with mild horizontal activity decline at 1000 mg/kg.
Observed no functional deficits at 50 or 200 mg/kg.
Found 1.8% dorsal and 5.8% ventral spinal root axons demyelinated at 1000 mg/kg.
Confirmed demyelination ratio below 0.1% in control, 50 and 200 mg/kg groups.
化学情報
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CAS 番号 121412-39-3
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分子量 355.43
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分子式 C21H25NO4
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SMILES
O=C(C)OC1=C(OC(C)=O)C2=C(C=CC=C2)C(N(C3CCCCC3)C)=C1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[1]. Gunson DE, et al. Toxic peripheral neuropathy with demyelination in Sprague-Dawley rats given CGS 21595--a 5-lipoxygenase inhibitor. Veterinary pathology. 1992 Mar;29(2):145-51. [Content Brief]
[2]. Classen W, et al. Functional and morphological characterization of neuropathy induced with 5-lipoxygenase inhibitor CGS 21595. Experimental and toxicologic pathology : official journal of the Gesellschaft fur Toxikologische Pathologie. 1994 Jul;46(2):119-25. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
CGS 21595 関連分類
HY-183244 関連分類
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