AMG-8562
AMG-8562 is a selective, orally active transient receptor potential vanilloid 1 (TRPV1) modulator that inhibits the activation of rat TRPV1 by Capsaicin (HY-10448), Anandamide (HY-10863) and N-arachidonyldopamine (HY-110018), with IC50 values of 1.75, 9.29 and 3.87 nM, respectively. AMG-8562 blocks capsaicin-induced activation, potentiates pH5-induced activation and has no effect on heat-induced activation of rat TRPV1, whereas it completely blocks capsaicin- and heat-induced activation and partially blocks pH5-induced activation of human TRPV1. AMG-8562 can be used in studies of TRPV1 activation patterns, hyperalgesia and pain-related research.
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- CAS. Nr.: 1041478-78-7
- Formel: C24H25F3N2O2
- Molecular Weight:430.47
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Speicherung:
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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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
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TRPV1 1.75 nM (IC50, Rat TRPV1; capsaicin-induced activation) |
TRPV1 9.29 nM (IC50, Rat TRPV1; anandamide-induced activation at pH 6) |
TRPV1 3.87 nM (IC50, Rat TRPV1; NADA-induced activation at pH 6) |
AMG-8562 completely blocks capsaicin (HY-10448)- and heat-induced activation of human TRPV1, and partially blocks pH 5-induced activation of human TRPV1[1].
AMG-8562 is selective for TRPV1, with an IC50 of approximately 3 μM against human TRPV4, and IC50 values all >20 μM against rat TRPA1, rat TRPM8, rat TRPV2 and human TRPV3. It also exhibits no partial agonist activity on these channels[1].
AMG-8562 blocks the activation of rat TRPV1 by capsaicin, anandamide, and NADA, with corresponding IC50 values of 1.75 nM, 9.29 nM, and 3.87 nM, respectively. This reagent does not block heat-induced activation, enhances activation under pH 5 conditions, and exhibits no partial agonist activity under physiological pH conditions[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
AMG-8562 (30-100 mg/kg; p.o.; single administration) reduces the hyperalgesic window by 27% at oral doses of 30 and 100 mg/kg in a rat model of CFA-induced thermal hyperalgesia[1].
AMG-8562 (30-100 mg/kg; p.o.; single administration) reduces the area of hyperalgesia by 29% at oral doses of 30 and 100 mg/kg in a rat model of heat hyperalgesia induced by plantar skin incision[1].
AMG-8562 (30 mg/kg; p.o.; single administration) significantly reduces acetic acid (HY-Y0319)-induced writhing responses in mice by 59% at an oral dose of 30 mg/kg[1].
AMG-8562 (1-30 mg/kg; p.o.; single dose; 3 mg/kg; i.v.; single dose) does not induce hyperthermia in rats, but causes a mild, dose-dependent decrease in core body temperature, with a maximum reduction of 1.0°C at the 3 mg/kg i.v. dose and 0.6°C at the highest p.o. dose of 30 mg/kg[1].
AMG-8562 (100 mg/kg; p.o.; single administration) does not impair spontaneous locomotor activity in mice or rats at an oral dose of 100 mg/kg, indicating that its analgesic efficacy is not interfered with by sedation or motor impairment[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (adult male, 150-250 g)[1]
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Dosage:0.1 mg/kg; 0.3 mg/kg; 1 mg/kg; 3 mg/kg
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Administration:p.o.; single dose
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Result:Significantly and dose-dependently decreased capsaicin-induced flinching.
Produced 100% blockade of flinching at 3 mg/kg dose.
Achieved significant reduction in flinches at minimally effective dose of 1 mg/kg.
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Animal Model:Sprague-Dawley (adult male, 150-250 g)[1]
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Dosage:30 mg/kg; 100 mg/kg
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Administration:p.o.; single dose
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Result:Significantly reduced thermal hyperalgesia at both 30 mg/kg and 100 mg/kg doses.
Increased paw withdrawal latency to 5.8 s at 30 mg/kg dose, producing 27% reduction of the hyperalgesia window.
Increased paw withdrawal latency to 5.8 s at 100 mg/kg dose, producing 27% reduction of the hyperalgesia window.\nSignificantly reduced thermal hyperalgesia at both 30 mg/kg and 100 mg/kg doses.
Increased paw withdrawal latency to 5.5 s at 30 mg/kg dose, producing 29% reduction of the hyperalgesia window.
Increased paw withdrawal latency to 5.9 s at 100 mg/kg dose, producing 29% reduction of the hyperalgesia window.
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Animal Model:CD-1 (adult male, 20-25 g)[1]
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Dosage:10 mg/kg; 30 mg/kg; 100 mg/kg
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Administration:p.o.; single dose
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Result:Reduced writhes to 19.22 at 10 mg/kg dose.
Reduced writhes to 14.8 at 30 mg/kg dose, producing 59% statistically significant reduction compared to vehicle.
Reduced writhes to 15.0 at 100 mg/kg dose.
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Animal Model:Sprague-Dawley (adult male, 150-250 g)[1]
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Dosage:3 mg/kg (i.v.); 1 mg/kg (p.o.); 3 mg/kg (p.o.); 10 mg/kg (p.o.); 30 mg/kg (p.o.)
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Administration:i.v.; single dose; p.o.; single dose
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Result:Caused a significant maximal decrease in core body temperature of 1.0°C at 20 minutes post-dosing with 3 mg/kg i.v. dose.
Caused a modest maximal decrease in core body temperature of 0.6°C at 160 minutes post-dosing with oral doses of 1, 3, 10, and 30 mg/kg.
Produced no hyperthermia at any dose.
Chemical Information
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CAS. Nr. 1041478-78-7
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Molecular Weight 430.47
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Formel C24H25F3N2O2
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SMILES
C(=C/C(NC1=C2C(C[C@@H](O)C2)=CC=C1)=O)\C3=C(C=C(C(F)(F)F)C=C3)N4CCCCC4
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
AMG-8562 Related Classifications
HY-114583 Related Classifications
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