2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. TRP Channel
  4. AMG9678

AMG9678 is a potent, selective, orally active antagonist of TRPM8 with an IC50 of 31.2 nM.

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AMG9678

AMG9678 화학구조

CAS No. : 1159997-27-9

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AMG9678 Related Antibodies

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

  • Biological Activity

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  • References

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제품 설명

AMG9678 is a potent, selective, orally active antagonist of TRPM8 with an IC50 of 31.2 nM[1].

IC50 & Target

TRPM8

31.2 nM (IC50)

TRPA1

0.6 μM (IC50)

Cellular Effect
Cell Line Type Value Description References
CHO IC50
27 nM
Compound: 29
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

AMG9678 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 7.6 h[1].

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

AMG9678 Related Antibodies
In Vivo

AMG9678 (0-100 mg/kg; p.o.; once) produces a significant and somewhat dose-dependent decrease in body temperature (Tb) in rats[1].
AMG9678 (30 mg/kg; p.o.; once daily for 4 consecutive days) decreases reduced body temperature after repeated dosing 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: 10, 30 and 100 mg/kg
Administration: Oral administration, once or once daily for 4 consecutive days
Result: Produced a significant and somewhat dose-dependent decrease in Tb at 10, 30 and 100 mg/kg. The magnitude of TRPM8 blockade-induced decrease in body temperature is reduced after repeated dosing.
Effect of AMG9678 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
AMG9678 10 (p.o.) 0.72 p < 0.001 60 0.04 ± 0.006
AMG9678 30 (p.o.) 0.70 p < 0.01 60 0.34 ± 0.1
AMG9678 100 (p.o.) 0.83 p < 0.05 60 0.36 ± 0.12
분자량

416.36

화학식

C20H18F6N2O
CAS No.
SMILES

O=C(N1CCC2=C(C=CC=C2)[C@H]1C3=CC=C(C(F)(F)F)C=C3)N[C@@H](C)C(F)(F)F
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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AMG9678 Related Classifications

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  • 농도 희석 계산기

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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:

AMG96781159997-27-9AMG 9678AMG-9678TRP ChannelTransient receptor potential channelsselectiveTRPA1body temperatureInhibitorinhibitorinhibit

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상품명:
AMG9678
Cat. No.:
HY-104062
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