AMG9678
AMG9678 is a potent, selective, orally active antagonist of TRPM8 with an IC50 of 31.2 nM.
For research use only. We do not sell to patients.
- CAS No.: 1159997-27-9
- Formula: C20H18F6N2O
- Molecular Weight:416.36
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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
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
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TRPM8 31.2 nM (IC50) |
TRPA1 0.6 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
27 nM
Compound: 29
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Antagonist activity at rat TRPM8 expressed in CHO cells assessed as inhibition of icilin-induced Ca2+ influx incubated 2.5 mins prior to icilin challenge by luminometry
Antagonist activity at rat TRPM8 expressed in CHO cells assessed as inhibition of icilin-induced Ca2+ influx incubated 2.5 mins prior to icilin challenge by luminometry
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[PMID: 24597733] |
In Vitro
AMG9678 potently inhibits the menthol and cold-induced increase in intracellular calcium in cells expressing rat TRPM8, the plasma half-life (T1/2) in rats is 7.6 h[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
AMG9678 (30 mg/kg; p.o.; once daily for 4 consecutive days) decreases reduced body temperature after repeated dosing in rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague Dawley rats weighing 200–350 g (6–12 weeks of age) [1]
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Dosage:10, 30 and 100 mg/kg
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Administration:Oral administration, once or once daily for 4 consecutive days
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Result:Produced a significant and somewhat dose-dependent decrease in Tb at 10, 30 and 100 mg/kg. The magnitude of TRPM8 blockade-induced decrease in body temperature is reduced after repeated dosing.
Effect of AMG9678 on Tb in rats. P value is for comparing compound administered rat Tb with vehicle administered rat Tb. End of the study plasma concentration is reported in μM. Asterisk indicates one-way ANOVA followed by Dunnett's MCT
Compound Dose mg/kg (route) Max Tb decrease (°C) P value * Time post dosing (min) Plasma concentration AMG9678 10 (p.o.) 0.72 p < 0.001 60 0.04 ± 0.006 AMG9678 30 (p.o.) 0.70 p < 0.01 60 0.34 ± 0.1 AMG9678 100 (p.o.) 0.83 p < 0.05 60 0.36 ± 0.12
Chemical Information
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CAS No. 1159997-27-9
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Molecular Weight 416.36
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Formula C20H18F6N2O
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SMILES
O=C(N1CCC2=C(C=CC=C2)[C@H]1C3=CC=C(C(F)(F)F)C=C3)N[C@@H](C)C(F)(F)F
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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.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
AMG9678 Related Classifications
HY-104062 Related Classifications
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