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.

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AMG8788

AMG8788 화학구조

CAS No. : 1159996-43-6

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Other Forms of AMG8788:

AMG8788 Related Antibodies

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View All TRP Channel Isoform Specific Products:

View All Isoforms
TRPA1 TRPC3 TRPC4 TRPC5 TRPC6 TRPC7 TRPM8 TRPM2 TRPM3 TRPM4 TRPM7 TRPML1 TRPML2 TRPML3 TRPV1 TRPV2 TRPV3 TRPV4 TRPV6

  • Biological Activity

  • 순도&문서

  • References

  • 고객리뷰

제품 설명

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 (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
분자량

414.40

화학식

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
선적

Room temperature in continental US; may vary elsewhere.
보관

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

  • 몰농도 계산기

  • 농도 희석 계산기

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
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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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상품명:
AMG8788
Cat. No.:
HY-104061
수량:
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