GPCR antagonist-1
GPCR antagonist-1 is an orally active G protein-coupled receptor (GPCR) antagonist as well as an insecticide. GPCR antagonist-1 induces intestinal microvillus destruction, reduces microfilarial secretion, increases the proportion of malformed embryos, inhibits nematode motility and L3-stage molting, and exerts L4-stage larvicidal activity. GPCR antagonist-1 can be used for the research of filarial infections.
For research use only. We do not sell to patients.
- Formula: C28H43NO2
- Molecular Weight:425.65
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
In Vitro
GPCR antagonist-1 (s-17) (day 3) inhibits adult female Brugia pahangi motility with an IC50 of 6.5 μM and adult male motility with an IC50 of 2.6 μM, with selectivity indices of 3.2 and 8, respectively[1].
GPCR antagonist-1 (day 7 (female); day 5 (male)) inhibits adult female Onchocerca ochengi motility with an IC50 of 0.29 μM and adult male motility with an IC50 of 3.6 μM[1].
GPCR antagonist-1 causes >50% molting inhibition of Onchocerca volvulus L3 larvae in vitro[1].
GPCR antagonist-1 shows larvicidal activity against Brugia pahangi L4 larvae in vitro[1].
GPCR antagonist-1 (30 μM; 3 days) destroys gut microvilli in adult female Brugia pahangi, while causing minimal damage to gonad contents in vitro[1].
GPCR antagonist-1 shows improved metabolic stability in mouse liver microsomes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Meriones unguiculatus (male, 5-7 months old, 50-60 g, infected via intraperitoneal injection of 200 third-stage larvae)[1]
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Dosage:50 mg/kg
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Administration:p.o.; twice daily 6 h apart; 10 days
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Result:Induced a 49.5% reduction in microfilariae secretion.
Increased the proportion of deformed embryos 2.2-fold (from 11.2% to 24.1%).
Chemical Information
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Molecular Weight 425.65
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Formula C28H43NO2
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SMILES
CC(OC1=CC=C(C=C1)[C@H]([C@@H](NCCCCCCCC)CC2=CC=CC=C2)OCC)C
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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-1 Related Classifications
HY-187424 Related Classifications
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