Derquantel
Based on 1 Customer Validation
Derquantel, a spirocyclic anthelmintic, is a competitive, orally active nicotinic acetylcholine receptor (nAChR) antagonist. Derquantel inhibits ACh-induced depolarization with an IC50 of 0.22 μM. By selectively antagonizing nAChRs on the somatic muscles of nematodes, Derquantel causes flaccid paralysis of muscles, thereby dislodging parasites from the host's gastrointestinal tract. Derquantel is applicable to research related to Haemonchus contortus infection and Ascaris suum infection.
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- Purity: 98.4%
- CAS No.: 187865-22-1
- 화학식: C28H37N3O4
- 분자량:479.61
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보관:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Biological Activity
Derquantel (1 μM) acts as a competitive antagonist of acetylcholine-induced contractions in Ascaris suum somatic muscle strips, shifting the acetylcholine EC50 from 7 μM to 52 μM[2].
Derquantel (0.1-30 μM; 0-4 min) potently and reversibly inhibits acetylcholine-induced depolarizations in Ascaris suum somatic muscle flap preparations with an IC50 of 200 nM, acting as a competitive antagonist[2].
Derquantel (1 μM; 30 min pre-incubation) shifts the acetylcholine EC50 from 4.5 μM to 10.2 μM and reduces the maximum depolarization response in Ascaris suum somatic muscle flap preparations, consistent with competitive antagonism[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 187865-22-1
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Appearance Solid
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분자량 479.61
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화학식 C28H37N3O4
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Color White to off-white
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SMILES
CN([C@]12[C@](C[C@@]34N(CC[C@]3(O)C)C2)([H])C(C)([C@@]5(C6=CC=C(OC(C)(C=CO7)C)C7=C6NC5)C1)C)C4=O
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Synonyms
PF-00520904
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
순도&문서
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Data Sheet (273 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Sager H, et al. Efficacy of monepantel, derquantel and abamectin against adult stages of a multi-resistant Haemonchus contortus isolate. Parasitol Res. 2012;111(5):2205-2207. [Content Brief]
[2]. Puttachary S, et al. Derquantel and abamectin: effects and interactions on isolated tissues of Ascaris suum. Mol Biochem Parasitol. 2013;188(2):79-86. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Derquantel Related Classifications
HY-125159 Related Classifications
Powered by Bioz
- Derquantel
- 187865-22-1
- PF-00520904
- PF00520904
- PF 00520904
- Parasite
- nAChR
- acetylcholine
- GABA
- nematode species
- somatic muscle nicotinic acetylcholine receptor
- Ascaris suum
- multi-resistant Haemonchus contortus isolates
- Haemonchus contortus
- sheep
- abamectin
- pharyngeal glutamate-gated chloride receptors
- Inhibitor
- inhibitor
- inhibit