Product Name
(rel)-Asperparaline A
Synonyms
(rel)-Aspergillimide; (rel)-VM55598
Description
(rel)-Asperparaline A ((rel)-Aspergillimide), an anthelmintic metabolite, is isolated from okara that has been fermented with Aspergillus japonicas JV-23. (rel)-Asperparaline A is also a potent and selective antagonist of nAChR. (rel)-Asperparaline A exhibits paralytic activity in silk worms.
Structural Formula
(rel)-Asperparaline A
Source
Aspergillus japonicus JV-2
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Shipping
Room temperature in continental US; may vary elsewhere.
SMILES
CN(C1=O)C(C[C@@]2(CC3=O)C(N3C)=O)(CN(CC[C@@H]4C)C14C5)[C@]5([H])C2(C)C.[Rotation (-)]
In Vivo
Asperparaline A (10 μg/g; p.o.) exhibits paralysis against silk worms within 1 h and lasts for 7 to 10 h.Asperparaline A (3 μg/g; injection with a micro-syringe) exhibits paralysis activity against silk worms within 20 min and lasts for 4 to 5 h.
In Vitro
Asperparaline A (1 μM; 1 min) markedly and reversibly blocks the acetylcholine (Ach; 10 µM)-induced current in the silkworm larval neurons. Asperparaline A (1-1000 nM; 1 min) differentially blocks the peak and slowly desensitizing currents, with IC50s of 20.2 and 39.6 nM, respectively. Asperparaline A (10 μM; 1 min) reduces the peak current amplitude of the ACh (100 µM)-induced response of α3β4 nAChR by 33.4%, while barely influencing the amplitudes of the responses to ACh of the α4β2 and α7 nAChRs in X. laevis oocytes.
Datasheet 