AMG8788
AMG8788 is a potent, selective, orally active antagonist of TRPM8 with an IC50 of 63.2 nM.
For research use only. We do not sell to patients.
- CAS No.: 1159996-43-6
- Formula: C23H18F4N2O
- Molecular Weight:414.40
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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
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TRPM8 63.2 nM (IC50) |
TRPA1 1 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
56 nM
Compound: 87
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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 icilin induction by flash luminometry
Antagonist activity at rat TRPM8 expressed in CHO cells assessed as inhibition of icilin-induced Ca2+ influx incubated 2.5 mins prior icilin induction by flash luminometry
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[PMID: 22329507] |
| CHO | IC50 |
57 nM
Compound: 1
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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] |
AMG8788 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 6.7 h[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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:30 mg/kg
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Administration:Oral administration, once
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Result:Produced a significant decrease of Tb from 40 min to 70 min post dosing.
Effect of AMG8788 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 AMG8788 30 (p.o.) 0.53 p < 0.05 40 1.5 ± 0.6
Chemical Information
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CAS No. 1159996-43-6
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Molecular Weight 414.40
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Formula C23H18F4N2O
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SMILES
O=C(N1CCC2=C(C=CC=C2)[C@H]1C3=CC=C(C(F)(F)F)C=C3)NC4=CC=C(F)C=C4
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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)
AMG8788 Related Classifications
HY-104061 Related Classifications
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