Paraherquamide A
Based on 1 Customer Validation
Paraherquamide A (PNU-97333) is an anthelmintic and nicotinic acetylcholine receptor (nAChR) antagonist, with pIC50 values ranging from 6.87 to 7.58 for L-type nAChR and from 4.84 to 5.54 for N-type nAChR. Paraherquamide A acts as a competitive antagonist against multiple nematode nAChR subtypes, as well as a mixed competitive-noncompetitive antagonist against nematode N-type nAChR. Paraherquamide A induces flaccid paralysis in parasitic nematodes without altering ATP levels, inhibits nematode motility, and antagonizes cholinergic agonist-induced muscle contraction in nematodes. Paraherquamide A can be used in studies related to nematode parasitic infections.
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- Reinheit: 99.58%
- CAS. Nr.: 77392-58-6
- Formel: C28H35N3O5
- Molecular Weight:493.59
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
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Biologische Aktivität
Paraherquamide A (0.03-30 μM) acts as a competitive antagonist of nicotinic acetylcholine receptors in the body wall muscle of Ascaris suum. Its pKB value (5.86) for nicotine-sensitive receptors is significantly lower than those of the levamisole (HY-A0106)-sensitive (6.61), pyrantel (HY-12641A)-sensitive (6.50), and bephenium (HY-12639)-sensitive receptor subtypes[1].
Paraherquamide A (10 μM; 1 min) acts as a mixed competitive/non-competitive antagonist of wild-type C. elegans type N (ACR-16) nAChR expressed in X. laevis oocytes, with a pIC50 value of 4.84[2].
Paraherquamide A acts as a non-competitive antagonist of the wild-type L-type (UNC-38/UNC-29/UNC-63/LEV-1/LEV-8) nAChR from *Caenorhabditis elegans* expressed in Xenopus oocytes, with a pIC50 value of 7.58[2].
Paraherquamide A (1 min) acts as an antagonist of *C. elegans* L-type 2.1 and L-type 2.2 nAChRs expressed in *X. laevis* oocytes, with pIC50 values of 6.91 and 6.94, respectively[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.
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Animal Model:N2 (wild-type); RB918 acr-16 (ok789) V (N-type nAChR mutant); ZZ37 unc-63 (x37) I (L-type nAChR mutant)[2]
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Dosage:100 nM-1 mM
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Administration:solution exposure
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Result:Suppressed thrashing of wild-type worms with a pLC50 of 5.02.
Inhibited thrashing of RB918 acr-16 (ok789) V (N-type nAChR mutant) worms with a pLC50 of 5.61, showing higher sensitivity than wild-type worms.
Failed to cause significant reduction in thrashing of ZZ37 unc-63 (x37) I (L-type nAChR mutant) worms even at tested concentrations.
Chemical Information
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CAS. Nr. 77392-58-6
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Appearance Solid
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Molecular Weight 493.59
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Formel C28H35N3O5
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Color White to off-white
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SMILES
CN1C23[C@](C[C@@]4(C1=O)N(CC[C@]4(O)C)C3)([H])C(C)([C@@]5(C6=CC=C(OC(C)(C=CO7)C)C7=C6NC5=O)C2)C
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Synonyms
PNU-97333
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Reinheit & Dokumentation
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Data Sheet (281 KB)
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SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Korean - KR (419 KB)
- Portuguese - PT (419 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Robertson AP, et al. Paraherquamide and 2-deoxy-paraherquamide distinguish cholinergic receptor subtypes in Ascaris muscle. J Pharmacol Exp Ther. 2002;302(3):853-860. [Content Brief]
[2]. Koizumi W, et al. Determinants of Subtype-Selectivity of the Anthelmintic Paraherquamide A on Caenorhabditis elegans Nicotinic Acetylcholine Receptors. Mol Pharmacol. 2023 Jun;103(6):299-310. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Paraherquamide A Related Classifications
HY-129591 Related Classifications
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