Bioactivity | S-MGB-234 is a minor groove binder of Animal African Trypanosomiasis (AAT). S-MGB-234 displays excellent in vitro activities against the principal causative organisms of AAT; Trypanosoma congolense, and Trypanosoma vivax. S-MGB-234 does not show cross-resistance with the current diamidine drugs and are not internalized via the transporters used by diamidines[1]. |
Invitro | S-MGB-234 (compound 7) (69 hours) shows nontoxic to L6 cells with an EC50 of 20.39 μM[1]. |
In Vivo | S-MGB-234 (compound 7) provides total cure and no relapses in mice (cured/infected, 4/4), when treated with 2 applications of 50 mg/kg i.p.. Partial cure (1/4) is seen in mice treated with four daily applications of 10 mg/kg i.p., whilst only two applications of S-MGB-234 (compound 7) at 10 mg/kg i.p. gives no cure but prolongs survival relative to the untreated control[1]. |
Name | S-MGB-234 |
CAS | 1970223-53-0 |
Formula | C30H32N8O4 |
Molar Mass | 568.63 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Giordani F, et al. Novel Minor Groove Binders Cure Animal African Trypanosomiasis in an in Vivo Mouse Model [published correction appears in J Med Chem. 2021 Dec 23;64(24):18236]. J Med Chem. 2019;62(6):3021-3035. |