JTS-653
JTS-653 is a highly potent and selective transient receptor potential vanilloid 1 (TRPV1) antagonist in vitro and in vivo. JTS-653 attenuates chronic pain refractory to non-steroidal anti-inflammatory agents.
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- CAS. Nr.: 942614-99-5
- Formel: C23H21F3N4O4
- Molecular Weight:474.43
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
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TRPV1 |
JTS-653 inhibits proton-induced activation of human and rat TRPV1 with IC50s of 0.320 and 0.347 nM, respectively[1].
JTS-653 blocks heat-induced inward currents in rat TRPV1 with an IC50 of 1.4 nM[1].
In the competition experiments, JTS-653 displaces [3H]RTX binding to human and rat TRPV1 in a concentration-related manner with Ki values of 11.44 and 4.40 nM, respectively[1].
JTS653 inhibits the 30 nM Capsaicin-induced activation of human and rat TRPV1 with IC50s of 0.236 and 0.247 nM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
JTS-653 attenuates chronic pain refractory to non-steroidal anti-inflammatory agents in rats and mice including post-herpetic pain. JTS-653 (0.3, 1, 3 mg/kg) shows its effect in a dose-related manner, with statistical significance at 0.3 mg/kg or above[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats aged 5 to 6 weeks[2]
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Dosage:0.3, 1, 3 mg/kg
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Administration:0.5 h, 2 h, 8 h, 25 h
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Result:Partially attenuated mechanical hyperalgesia in the L5 spinal nerve ligation model in rats at 0.3 mg/kg.
Increased the paw withdrawal threshold (PWT) of the ipsilateral paw at 0.5, 2, and 8 h after the administration and its effect disappeared by 25 h after administration.
Showed its maximum effect with 1 mg/kg at 2 h after administration.
Chemical Information
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CAS. Nr. 942614-99-5
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Molecular Weight 474.43
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Formel C23H21F3N4O4
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SMILES
OC[C@@H]1N(C(N=C2)=CC=C2C)C3=CC=CC(C(NC(C=C4)=CN=C4OCC(F)(F)F)=O)=C3OC1
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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
[1]. Yoshihiro Kitagawa, et al. Pharmacological characterization of (3S)-3-(hydroxymethyl)-4-(5-methylpyridin-2-yl)-N-[6-(2,2,2-trifluoroethoxy)pyridin-3-yl]-3,4-dihydro-2H-benzo[b][1,4]oxazine-8-carboxamide (JTS-653), a novel transient receptor potential vanilloid 1 antagonist. J Pharmacol Exp Ther. 2012 Aug;342(2):520-8. [Content Brief]
[2]. Yoshihiro Kitagawa, et al. Orally administered selective TRPV1 antagonist, JTS-653, attenuates chronic pain refractory to non-steroidal anti-inflammatory drugs in rats and mice including post-herpetic pain. J Pharmacol Sci. 2013;122(2):128-37. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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