Echothiopate iodide
Echothiopate iodide (Echothiophate iodide) is an acetylcholinesterase (AChE) inhibitor. Echothiopate iodide irreversibly inhibits acetylcholinesterase, prevents the enzymatic hydrolysis of acetylcholine, and increases the local acetylcholine concentration in the ciliary muscle, thereby driving muscarinic receptor downregulation and regulatory hyposensitivity to Pilocarpine Hydrochloride. Echothiopate iodide can be used in the study of glaucoma.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 513-10-0
- 分子式: C9H23INO3PS
- 分子量:383.23
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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
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生物活性
製品説明
IC50 & Target
[1]|
AChE |
体外実験
Echothiopate iodide (0.1 mg/mL; 2.5-4 h) increases ACh content in resting and electrically stimulated rat isolated superior cervical ganglia, reaching 476 pM in resting ganglia and 395 pM in stimulated ganglia[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
Echothiopate iodide (30-150 μg; topical ocular administration; once daily; 42-47 weeks) reduced baseline aqueous humor outflow facility and the accommodative response to Pilocarpine Hydrochloride (HY-B0726) in cynomolgus monkeys[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Cynomolgus monkeys (Macaca fascicularis) (Group 1: two females and two males, 5, 6, 7, and 10 years old, weighing 2.8-5.6 kg)[1]
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Dosage:30 μg in 2 μL ramped up over 5 weeks to 150 μg in 5 × 2-μL drops
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Administration:topical ocular; once daily; 42-47 weeks
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Result:Increased intraocular pressure from 14.8 to 21.1 mm Hg in treated eyes after 34 weeks.
Induced cataract in two of four treated eyes.
Decreased baseline resting refraction from -2.8 to -21.8 D in treated eyes after 36 weeks.
Nearly abolished the accommodation response to pilocarpine (20, 200, and 1000 μg).
Reduced baseline outflow facility to 50% of pretreatment baseline values after 38 weeks.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 513-10-0
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分子量 383.23
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分子式 C9H23INO3PS
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SMILES
O=P(SCC[N+](C)(C)C)(OCC)OCC.[I-]
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別名
Echothiophate iodide
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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
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Echothiopate iodide 関連分類
HY-16183 関連分類
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