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.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- CAS No.: 1073616-61-1
- 화학식: C19H18ClF3N4O3
- 분자량:442.82
-
보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
-
Biological Activity
-
Chemical Information
- 순도&문서
- References
-
Help & FAQs
Biological Activity
|
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.
-
Animal Model:Male Sprague-Dawley rats (6 weeks, 180-280 g) bearing acute inflammatory CFA model[1]
-
Dosage:0.3, 1, 3, 10, 30 mg/kg
-
Administration:Oral administration
-
Result:Dose-dependently reversed inflammatory thermal hyperalgesia.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 1073616-61-1
-
분자량 442.82
-
화학식 C19H18ClF3N4O3
-
SMILES
O=C(N1CC=C(C2=NC=C([C@H](O)CO)C=C2Cl)CC1)NC3=NC=C(C(F)(F)F)C=C3
-
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
[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)
Powered by Bioz