AN11251

Product NameAN11251
CAS2130750-59-1
MFC29H38BFO7
MW528.42
EINECS
MOL File2130750-59-1.mol

Usage And Synthesis

Description

AN11251 is a potenet Anti-Wolbachia Agent with Potential for Treatment of Onchocerciasis and Lymphatic Filariasis (EC50 = 1.5nM for LDW1 cell lines and 15 nM for C6/36 cell lines). AN11251 showed in vitro anti-Wolbachia activity and physicochemical and pharmacokinetic properties providing high exposure in plasma.

Uses

AN11251 is a potent and oral active anti-Wolbachia agent with potential for treatment of onchocerciasis and lymphatic filariasis, with EC50 values of 1.5 nM in LDW1 cell lines and 15 nM in C6/36 cell lines[1].

in vivo

AN11251 (25 mg/kg, PO, BID for 7 or 14 days) reduces the Wolbachia load in the B. malayi larvae by 75.4% and 98.8% in the 7- and 14-day treatment groups, respectively^[1].

Animal Model:	CB.17 SCID mice inoculated with 50 L3-stage B. malayi larvae^[1].
Dosage:	25 mg/kg.
Administration:	Orally, BID for 7 or 14 days.
Result:	Reduced the Wolbachia load in the B. malayi larvae by 75.4% and 98.8% in the 7- and 14-day treatment groups, respectively.

References

[1] Jacobs RT, et al. Boron-Pleuromutilins as Anti- Wolbachia Agents with Potential for Treatment of Onchocerciasis and Lymphatic Filariasis. J Med Chem. 2019 Mar 14;62(5):2521-2540. DOI:10.1021/acs.jmedchem.8b01854