[CAS NO. 821768-06-3]  JNJ-17203212

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PRODUCTS SPECIFICATIONS [821768-06-3]

Catalog
HY-100129
Brand
MCE
CAS
821768-06-3

DESCRIPTION [821768-06-3]

Overview

MDLMFCD12828764
Molecular Weight419.32
Molecular FormulaC17H15F6N5O
SMILESO=C(N1CCN(C2=NC=CC=C2C(F)(F)F)CC1)NC3=NC=C(C(F)(F)F)C=C3

For research use only. We do not sell to patients.

1 Publications Citing Use of MCE


Summary

JNJ-17203212 is a selective, potent and competitive TRPV1 antagonist. JNJ-17203212 is developed for researching pain management, such as migraine [1] [2] .


IC50 & Target

TRPV1


In Vitro

JNJ-17203212 (0.5 μM) potently inhibits imperatorin-induced TRPV1 activation (Ca 2+ increases) in TRPV1-expressing HEK cells [1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.


In Vivo

JNJ-17203212 (0.3 mg/kg ; i.v.) dose-dependently reduces inflammatory soup (IS)-induced the immediate early gene c-fos expression [2] .
JNJ-17203212 completely blocks capsaicin-induced CGRP (the neurotransmitter calcitonin gene-related peptide) release in a dose-dependent manner [2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Sprague-Dawley rats (260-300 g) [2]
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.

Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL ( 238.48 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3848 mL 11.9241 mL 23.8481 mL
5 mM 0.4770 mL 2.3848 mL 4.7696 mL
10 mM 0.2385 mL 1.1924 mL 2.3848 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

    Solubility: ≥ 2.75 mg/mL (6.56 mM); Clear solution

  • 2.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

    Solubility: ≥ 2.75 mg/mL (6.56 mM); Clear solution

* All of the co-solvents are available by MCE.