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JNJ-17203212
CAS No. 821768-06-3
JNJ-17203212( JNJ17203212 | JNJ 17203212 )
Catalog No. M16055 CAS No. 821768-06-3
A potent, selective and orally bioavailable TRPV1 receptor antagonist with IC50 of 65 nM and 102 nM for hTRPV1 and rTRPV1, respectively.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 2MG | 35 | In Stock |
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| 5MG | 58 | In Stock |
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| 10MG | 102 | In Stock |
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| 25MG | 237 | In Stock |
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| 50MG | 385 | In Stock |
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| 100MG | 621 | In Stock |
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| 200MG | Get Quote | In Stock |
|
| 500MG | Get Quote | In Stock |
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| 1G | Get Quote | In Stock |
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Biological Information
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Product NameJNJ-17203212
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NoteResearch use only, not for human use.
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Brief DescriptionA potent, selective and orally bioavailable TRPV1 receptor antagonist with IC50 of 65 nM and 102 nM for hTRPV1 and rTRPV1, respectively.
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DescriptionA potent, selective and orally bioavailable TRPV1 receptor antagonist with IC50 of 65 nM and 102 nM for hTRPV1 and rTRPV1, respectively; exhibits high selectivity against a panel of receptors and transporters, and does not inhibits related TRP channels TRPV2, TRPV4, or TRPA1; inhibits both pH (pIC50=7.23) and capsaicin (pIC50=6.32)-induced channel activation; attenuates capsaicin evoked coughs, prevents core hypothermia evoked by capsaicin in vivo.Pain Preclinical.
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In VitroJNJ-17203212 (0.5 μM) potently inhibits imperatorin-induced TRPV1 activation (Ca2+ increases) in TRPV1-expressing HEK cells.
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In VivoJNJ-17203212 (0.3 mg/kg; i.v.) dose-dependently reduces inflammatory soup (IS)-induced the immediate early gene c-fos expression.JNJ-17203212 completely blocks capsaicin-induced CGRP (the neurotransmitter calcitonin gene-related peptide) release in a dose-dependent manner. Animal Model:Male Sprague-Dawley rats (260-300 g)Dosage:0.3 mg/kg Administration:Intravenous injection Result:Had a dose-dependent effect on the elevated c-fos expression that occurred after intracisternal injection of IS.
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SynonymsJNJ17203212 | JNJ 17203212
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PathwayMembrane Transporter/Ion Channel
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TargetTRP/TRPV Channel
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RecptorTRP/TRPV Channel
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Research AreaNeurological Disease
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IndicationPain
Chemical Information
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CAS Number821768-06-3
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Formula Weight419.3243
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Molecular FormulaC17H15F6N5O
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Purity>98% (HPLC)
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Solubility10 mM in DMSO
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SMILESO=C(N1CCN(C2=NC=CC=C2C(F)(F)F)CC1)NC3=NC=C(C(F)(F)F)C=C3
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Chemical Name1-Piperazinecarboxamide, 4-[3-(trifluoromethyl)-2-pyridinyl]-N-[5-(trifluoromethyl)-2-pyridinyl]-
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Swanson DM, et al. J Med Chem. 2005 Mar 24;48(6):1857-72.
2. Bhattacharya A, et al. J Pharmacol Exp Ther. 2007 Nov;323(2):665-74.
3. Cefalu JS, et al. J Urol. 2009 Aug;182(2):776-85.
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