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Art. -Nr.: HY-129591

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Paraherquamide A

Name: Paraherquamide A
Brand: MedChemExpress
SKU: HY-129591
Price: 375.00 USD
Availability: InStock
Rating: 5 (1 reviews)

(Synonyms: PNU-97333)

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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.

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Reinheit : 99.58%
CAS. Nr.: 77392-58-6
Formel: C₂₈H₃₅N₃O₅
Molecular Weight:493.59

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Paraherquamide A Chemical Structure

CAS. Nr.: 77392-58-6

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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In Vitro

Paraherquamide A (0.03-30 μM) acts as a competitive antagonist of nicotinic acetylcholine receptors in the body wall muscle of Ascaris suum. Its pK_B 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. .

In Vivo

Paraherquamide A (100 nM-1 mM) inhibits locomotor activity of wild-type *Caenorhabditis elegans*, with a pLC₅₀ of 5.02; this compound exhibits enhanced potency in N-type nAChR mutant nematodes but shows almost no efficacy in L-type nAChR mutant nematodes, confirming that it has higher selectivity for L-type nAChRs than for N-type nAChRs^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

N2 (wild-type); RB918 acr-16 (ok789) V (N-type nAChR mutant); ZZ37 unc-63 (x37) I (L-type nAChR mutant)^[2]
Dosage:

100 nM-1 mM
Administration:

solution exposure
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

CAS. Nr. 77392-58-6
Appearance Solid
Molecular Weight 493.59
Formel C₂₈H₃₅N₃O₅
Color White to off-white
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
Synonyms

PNU-97333
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
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]

[3]. Stocking E M, et al. Reverse prenyl transferases exhibit poor facial discrimination in the biosynthesis of paraherquamide A, brevianamide A, and austamide[J]. Journal of the American Chemical Society, 2000, 122(38): 9089-9098.

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

MOQ

Minimum order quantity

100 mg

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
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Paraherquamide A

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