V116517
V116517 is a potent, orally active transient receptor potential vanilloid (TRPV1) antagonist. V116517 shows potent activity in inhibiting both capsaicin (CAP)- and acid (pH 5)-induced currents in rat DRG neurons expressing native TRPV (IC50=423.2 nM for CAP; IC50=180.3 nM for acid). V116517 can be used for the research of pain.
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- CAS No.: 1073616-61-1
- Formule: C19H18ClF3N4O3
- Masse moléculaire:442.82
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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TRPV1 |
V116517 is highly selective for TRPV1 and did not show potency up to 10 μM in both TRPV3 and TRPV4 assays[1].
V116517 has fast-off kinetics for antagonism of both mode activations of TRPV1[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
V116517 exhibits high oral bioavailability (rat 74%, dog 100%, monkey 107%) and Cmax (rat 1380, dog 1120, monkey 459 ng/mL) following oral administration (rat 3, dog 3, monkey 3 mg/kg)[1].
V116517 exhibits terminal elimination half-lives (rat 3.3, dog 3.6 and, monkey 18 h) due to high plasma clearance (0.24, 0.28, and 0.36 L/h/kg respectively) combined with large volumes of distribution (0.68, 1.2, and 6.0 L/kg respectively) following intravenous administration (rat 1, dog 1 and, monkey 1 mg/kg)[1].
V116517 (rat 3 mg/kg; oral administration) is primarily restricted in periphery.The ratio of brain-to-plasma concentration is 0.09 at 3 h[1].
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 (6 weeks, 180-280 g) bearing acute inflammatory CFA model[1]
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Dosage:0.3, 1, 3, 10, 30 mg/kg
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Administration:Oral administration
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Result:Dose-dependently reversed inflammatory thermal hyperalgesia.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1073616-61-1
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Masse moléculaire 442.82
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Formule C19H18ClF3N4O3
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SMILES
O=C(N1CC=C(C2=NC=C([C@H](O)CO)C=C2Cl)CC1)NC3=NC=C(C(F)(F)F)C=C3
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Laykea Tafesse, et al. Structure-activity relationship studies and discovery of a potent transient receptor potential vanilloid (TRPV1) antagonist 4-[3-chloro-5-[(1S)-1,2-dihydroxyethyl]-2-pyridyl]-N-[5-(trifluoromethyl)-2-pyridyl]-3,6-dihydro-2H-pyridine-1-carboxamide (V116517) as a clinical candidate for pain management. J Med Chem. 2014 Aug 14;57(15):6781-94. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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