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.
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
製品説明
体外実験
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. .
体内実験
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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