GPCR antagonist-2
GPCR antagonist-2 is a GPCR antagonist with macrofilaricidal activity. GPCR antagonist-2 shows inhibitory effects on Brugia pahangi adult females and males (IC50 = 3.9 μM and 2.8 μM, respectively) and Onchocerca ochengi adult females and males (IC50 = 0.35 μM and 1.7 μM, respectively). GPCR antagonist-2 reduces B. pahangi worm burden and affects female fecundity and embryogenesis, downregulates GPCR expression in surviving adult female worms and can be used for the study of filarial infections, including onchocerciasis (river blindness).
For research use only. We do not sell to patients.
- Formula: C25H23F2N3
- Molecular Weight:403.47
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Biological Activity
Description
In Vitro
GPCR antagonist-2 (30 μM; 3 days) inhibits the motility of adult female and male Brugia pahangi with IC50 values of 3.9 μM and 2.8 μM, respectively[1].
GPCR antagonist-2 (30 μM; 5-7 days) inhibits the motility of adult female and male Onchocerca ochengi with IC50 values of 0.35 μM and 1.7 μM, respectively[1].
GPCR antagonist-2 (30 μM; 6 days) inhibits the molting of Onchocerca volvulus L3 larvae with an IC50 of 3.2 μM[1].
GPCR antagonist-2 (30 μM; 3 days) exhibits larvicidal activity against Brugia pahangi L4 larvae in both sexes[1].
GPCR antagonist-2 (30 μM; 3 days) induces ultrastructural alterations including vacuolated embryos and destroyed hypodermal chords in adult female Brugia pahangi[1].
GPCR antagonist-2 (1-50 μM; 24 h) shows cytotoxicity in HepG2 cells with a CC50 of 17.7 μM[1].
GPCR antagonist-2 shows reduced off-target binding to human α2B and 5-HT2B receptors[1].
GPCR antagonist-2 (100 μM; 48 h) shows significantly reduced developmental inhibition in C. elegans ser-7 mutants[1].
GPCR antagonist-2 shows reduced developmental inhibition in C. elegans gar-3 mutants[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2 cells
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Concentration:1, 3, 10, 30, 50 μM
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Incubation Time:24 h
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Result:Showed cytotoxicity with CC50 of 17.7 μM; female selectivity index (F-SI) = 4.5 and male selectivity index (M-SI) = 6.3.
In Vivo
GPCR antagonist-2 (50 mg/kg; p.o.; b.i.d 6 h apart; for 10 days) significantly increases the proportion of deformed embryos while decreasing normal embryos and eggs in adult female Brugia pahangi in vivo[1].
GPCR antagonist-2 downregulates GPCR expression in surviving adult female Brugia pahangi after in vivo treatment[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mongolian gerbils (Meriones unguiculatus), infected with 200 B. pahangi L3 larvae[1]
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Dosage:50 mg/kg
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Administration:p.o.; b.i.d 6 h apart; for 10 days
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Result:Reduced total worm burden by 50.8%.
Significantly reduced mf secretion by 57.1%, gonad content by 36.1%, and increased the percentage of deformed embryos by 49.0%.
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Animal Model:Mongolian gerbils, infected with 200 B. pahangi L3 larvae[1]
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Dosage:25 mg/kg
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Administration:p.o.; b.i.d 6 h apart; for 10 days
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Result:Did not significantly reduce worm burden but significantly affected female fecundity (increased deformed embryos by 13.7%).
Chemical Information
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Molecular Weight 403.47
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Formula C25H23F2N3
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SMILES
FC1=CC(C2=CC=C(CN3C(CN4CCCC4)=NC5=CC=CC=C53)C=C2)=CC(F)=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GPCR antagonist-2 Related Classifications
HY-187528 Related Classifications
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