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
Description
IC50 & Target
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TRPM8 63.2 nM (IC50) |
TRPA1 1 μM (IC50) |
Cellular Effect
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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] |
In Vitro
In Vivo
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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