JNJ 17203212 A high affinity TRPV1 receptor antagonist

JNJ 17203212  (CAS 821768-06-3)

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Synonym: 4-[3-(TRIFLUOROMETHYL)-PYRIDIN-2-YL]-N-[5-(TRIFLUOROMETH YL)-PYRIDIN-2-YL]-1-PIPERAZINECARBOXAMIDE
Application: A high affinity TRPV1 receptor antagonist
CAS Number: 821768-06-3
Purity: ≥98%
Molecular Weight: 419.33
Molecular Formula: C17H15F6N5O
Supplemental Information: This is classified as a Dangerous Good for transport and may be subject to additional shipping charges.
* Refer to Certificate of Analysis for lot specific data (including water content).
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Ordering Information

PRODUCT NAME CATALOG # UNIT PRICE QTY FAVORITES
JNJ 17203212 sc-204024 10 mg $159.00
JNJ 17203212 sc-204024A 50 mg $670.00

JNJ 17203212 is a high affinity transient receptor potential vanilloid 1 (TRPV1) receptor antagonist. TRPV1 is a Capsaicin (sc-3577) receptor that behaves as a non-selective cation channel that is mainly found in the sensory neurons, and specifically detects painful stimuli, low pH and heat. The compound has been used to investigate TRPV1 in rodent and guinea pig sensory reflexes. Research indicates that JNJ 17203212 elevates the micturition reflex threshold for activation in rodent bladder studies, and in rats weakens colonic hypersensitivity.


References

1. Swanson, D.M., et al. 2005. J. Med. Chem. 48: 1857-1872. PMID: 15771431
2. Ghilardi, J.R., et al. 2005. J. Neurosci. 25: 3126-3131. PMID: 15788769
3. Bhattacharya, A., et al. 2007. J. Pharmacol. Exp. Ther. 323: 665-674. PMID: 17690251
4. Cefalu, J.S., et al. 2009. J. Urol. 182: 776-785. PMID: 19539322
5. Schumacher, M.A. and Eilers, H. 2010. Front. Biosci. 15: 872-882. PMID: 20515731
6. Wiskur, B.J., et al. 2010. Methods Find Exp Clin Pharmacol. 32: 557-564. PMID: 21132125

Physical State :
Solid
Solubility :
Soluble in DMSO (100 mM), and ethanol (100 mM).
Storage :
Store at -20° C
Melting Point :
89.4-89.8° C
Boiling Point :
551.32° C at 760 mmHg (Predicted)
Density :
1.47 g/cm3 (Predicted)
Refractive Index :
n20D 1.54 (Predicted)
IC50 :
Vanilloid receptor: IC50 = 16 nM (rat); VR1: IC50 = 16 nM (human); BJP: IC50 = 65 nM
pK Values :
pKa: 12.62 (Predicted), pKb: 5.99 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
11339118
SMILES :
C1CN(CCN1C2=C(C=CC=N2)C(F)(F)F)C(=O)NC3=NC=C(C=C3)C(F)(F)F

Download SDS (MSDS)

Certificate of Analysis

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