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Benzomalvin A 

Cat. No. M28611
Benzomalvin A  Structure
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Biological Activity

Benzomalvin A is a potent antagonist of neurokinin receptor isolated from Penicillium sp. Benzomalvin A shows inhibitory activity against substance P with Ki values of 12, 42 and 43 μM at the guinea pig, rat and human neurokinin NK1 receptors, respectively.

Chemical Information
Molecular Weight 381.43
Formula C24H19N3O2
CAS Number 157047-96-6
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Kenneth D Clevenger, et al. Biochemistry. Interrogation of Benzomalvin Biosynthesis Using Fungal Artificial Chromosomes with Metabolomic Scoring (FAC-MS): Discovery of a Benzodiazepine Synthase Activity

[2] Kenneth D Clevenger, et al. Nat Chem Biol. A scalable platform to identify fungal secondary metabolites and their gene clusters

[3] Paulina Del Valle, et al. Planta Med. Alkaloids from the Fungus Penicillium spathulatum as α-Glucosidase Inhibitors

[4] Jens C Frisvad, et al. FEMS Microbiol Lett. Two new Penicillium species Penicillium buchwaldii and Penicillium spathulatum, producing the anticancer compound asperphenamate

[5] H H Sun, et al. J Antibiot (Tokyo). Benzomalvins, new substance P inhibitors from a Penicillium sp

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Keywords: Benzomalvin A  supplier, Neurokinin Receptor, inhibitors, activators


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