An inhibitor of parasitic PKG
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MBP146-78

Item No. 41083

Technical Information
Formal Name
4-[2-(4-fluorophenyl)-5-(1-methyl-4-piperidinyl)-1H-pyrrol-3-yl]-pyridine
CAS Number
188343-77-3
Molecular Formula
C21H22FN3
Formula Weight
Purity
≥98%
A solid
DMSO: Slightly Soluble: 0.1-1 mg/mlEthanol: Slightly Soluble: 0.1-1 mg/ml
SMILES
FC(C=C1)=CC=C1C2=C(C3=CC=NC=C3)C=C(C4CCN(C)CC4)N2
InChi Code
InChI=1S/C21H22FN3/c1-25-12-8-16(9-13-25)20-14-19(15-6-10-23-11-7-15)21(24-20)17-2-4-18(22)5-3-17/h2-7,10-11,14,16,24H,8-9,12-13H2,1H3
InChi Key
RBWNFHXBUDPAIO-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    MBP146-78 is an inhibitor of parasitic cGMP-dependent protein kinases (PKGs; IC50s = 1.9 and 1 nM for the E. tenella and T. gondii enzymes, respectively).1 It inhibits P. berghei sporozoite development into liver-stage parasites in HepG2 cells in a concentration-dependent manner.2 MBP146-78 (50 mg/kg) prevents P. yoelii liver infection in P. yoelii-infected mice. It increases survival time in P. berghei-infected mice when administered at a dose of 50 mg/kg twice per day for eight days.1 MBP146-78 (50 mg/kg two times per day) increases survival in T. gondii-infected mice and prevents secondary reinfection in the same mice.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Diaz, C.A., Allocco, J., Powles, M.A., et alCharacterization of Plasmodium falciparum cGMP-dependent protein kinase (PfPKG): Antiparasitic activity of a PKG inhibitor. Mol. Biochem. Parasitol. 146(1), 78-88 (2006).

    2. Panchal, D., and Bhanot, P. Activity of a trisubstituted pyrrole in inhibiting sporozoite invasion and blocking malaria infection. Antimicrob. Agents Chemother. 54(10), 4269-4274 (2010).

    3. Nare, B., Allocco, J.J., Liberator, P.A., et alEvaluation of a cyclic GMP-dependent protein kinase inhibitor in treatment of murine toxoplasmosis: Gamma interferon is required for efficacy. Antimicrob. Agents Chemother. 46(2), 300-307 (2002).