Paraherquamide A
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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.
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。
- 純度: 99.58%
- CAS 番号: 77392-58-6
- 分子式: C28H35N3O5
- 分子量:493.59
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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
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.
化学情報
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CAS 番号 77392-58-6
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性状 Solid
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分子量 493.59
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分子式 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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別名
PNU-97333
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
純度とドキュメンテーション
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データシート (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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取扱説明書 (2659 KB)
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Paraherquamide A 関連分類
HY-129591 関連分類
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