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.
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- CAS. Nr.: 513-10-0
- Formel: C9H23INO3PS
- Molecular Weight:383.23
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
AChE |
In Vitro
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. .
In Vivo
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.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 513-10-0
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Molecular Weight 383.23
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Formel C9H23INO3PS
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SMILES
O=P(SCC[N+](C)(C)C)(OCC)OCC.[I-]
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Synonyms
Echothiophate iodide
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Echothiopate iodide Related Classifications
HY-16183 Related Classifications
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