Emamectin B1a

Emamectin B1a (L-656,748) is a semisynthetic derivative of avermectin B1a that binds to GABA receptors (Ki=17.6 nM in rat brain membranes) and enhances GABA responses. Emamectin B1a acitivates GABAA receptors α1β1γ2, α1β2γ2, and α1β3γ2 with IC50s of 57, 210, and 49.8 nM, respectively. Emamectin B1a also binds to glycine receptors, inhibiting glycine receptors with an IC50=218 nM in rat spinal cord. Emamectin B1a (1.067 ng/mL) caused 90% mortality of S. exigua larvae in foliar spray bioassays and topical application, making it more toxic than avermectin B1.

Product Specifications

CAS Number

[121124-29-6]

Product Name Alternative

L-656,748

UNSPSC

12352005

Target

GABA Receptor

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel; Neuronal Signaling

Applications

COVID-19-immunoregulation

Field of Research

Infection

Assay Protocol

https://www.medchemexpress.com/emamectin-b1a.html

Smiles

CC[C@@H]([C@@H]1[C@@H](C)C=C[C@]2(C[C@@H]3C[C@@H](C/C=C(C)/[C@@H](O[C@H]4C[C@H](OC)[C@@H](O[C@H]5C[C@H](OC)[C@H](NC)[C@H](C)O5)[C@H](C)O4)[C@@H](C)/C=C/C=C6CO[C@H]7[C@]\6(O)[C@H](C(O3)=O)C=C(C)[C@H]7O)O2)O1)C

Molecular Formula

C49H75NO13

Molecular Weight

886.12

References & Citations

[1]Dawson, et al. Anticonvulsant and adverse effects of avermectin analogs in mice are mediated through the g-aminobutyric acidA receptor. J. Pharmacol. Exp. Ther. 295 (3), 1051-1060 (2000) .