2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. TRP Channel
  4. 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.

AMG8788 Chemical Structure

AMG8788 Chemical Structure

CAS No. : 1159996-43-6

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AMG8788 Related Antibodies

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Description

AMG8788 is a potent, selective, orally active antagonist of TRPM8 with an IC50 of 63.2 nM[1].

IC50 & Target

TRPM8

63.2 nM (IC50)

TRPA1

1 μM (IC50)

In Vitro

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.

AMG8788 Related Antibodies
In Vivo

AMG8788 (30 mg/kg; p.o.; once) elicits a transient decrease in body temperature (Tb) in rats[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Sprague Dawley rats weighing 200–350 g (6–12 weeks of age) [1]
Dosage: 30 mg/kg
Administration: Oral administration, once
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
Molecular Weight

414.40

Formula

C23H18F4N2O
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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AMG8788 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AMG87881159996-43-6AMG 8788AMG-8788TRP ChannelTransient receptor potential channelsselectiveTRPA1body temperatureInhibitorinhibitorinhibit

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HY-104061
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