AMG-8562
Based on 1 Customer Validation
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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 98.82%
- CAS. Nr.: 1041478-78-7
- Formel: C24H25F3N2O2
- Molecular Weight:430.47
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
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) |
In Vitro
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. .
In Vivo
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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Appearance Solid
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Molecular Weight 430.47
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Formel C24H25F3N2O2
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Color Light yellow to yellow
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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
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 100 mg/mL (232.30 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (11.62 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation
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Data Sheet (287 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.3230 mL | 11.6152 mL | 23.2304 mL | 58.0761 mL |
| 5 mM | 0.4646 mL | 2.3230 mL | 4.6461 mL | 11.6152 mL | |
| 10 mM | 0.2323 mL | 1.1615 mL | 2.3230 mL | 5.8076 mL | |
| 15 mM | 0.1549 mL | 0.7743 mL | 1.5487 mL | 3.8717 mL | |
| 20 mM | 0.1162 mL | 0.5808 mL | 1.1615 mL | 2.9038 mL | |
| 25 mM | 0.0929 mL | 0.4646 mL | 0.9292 mL | 2.3230 mL | |
| 30 mM | 0.0774 mL | 0.3872 mL | 0.7743 mL | 1.9359 mL | |
| 40 mM | 0.0581 mL | 0.2904 mL | 0.5808 mL | 1.4519 mL | |
| 50 mM | 0.0465 mL | 0.2323 mL | 0.4646 mL | 1.1615 mL | |
| 60 mM | 0.0387 mL | 0.1936 mL | 0.3872 mL | 0.9679 mL | |
| 80 mM | 0.0290 mL | 0.1452 mL | 0.2904 mL | 0.7260 mL | |
| 100 mM | 0.0232 mL | 0.1162 mL | 0.2323 mL | 0.5808 mL |
AMG-8562 Related Classifications
HY-114583 Related Classifications
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