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 No.: 513-10-0
- Formule: C9H23INO3PS
- Masse moléculaire:383.23
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Activité biologique
Description
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.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 513-10-0
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Masse moléculaire 383.23
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Echothiopate iodide Related Classifications
HY-16183 Related Classifications
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