AMG8788

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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

CAS No. : 1159996-43-6

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Other Forms of AMG8788:

TRPM8-IN-1 Get quote

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TRPC TRPM TRPV TRPA TRPML

Biological Activity
Purity & Documentation
References
Customer Review

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)

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	56 nM Compound: 87	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	[PMID: 22329507]
CHO	IC₅₀	57 nM Compound: 1	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	[PMID: 24597733]

In Vitro

AMG8788 potently inhibits the menthol and cold-induced increase in intracellular calcium in cells expressing rat TRPM8, the plasma half-life (T_1/2) in rats is 6.7 h^[1].

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

In Vivo

AMG8788 (30 mg/kg; p.o.; once) elicits a transient decrease in body temperature (T_b) 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 T_b from 40 min to 70 min post dosing.
Effect of AMG8788 on T_b in rats. P value is for comparing compound administered rat T_b with vehicle administered rat T_b. 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 T_b 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.

1159996-43-6

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

Handling Instructions (2659 KB)

References

[1]. Gavva NR, et al. Transient receptor potential melastatin 8 (TRPM8) channels are involved in body temperature regulation. Mol Pain. 2012 May 9;8:36. [Content Brief]

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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