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Tocris/JNJ 17203212/3361/50/50 mg

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货号: 3361/50

品牌: Tocris

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Description: Reversible, competitive and potent TRPV1 antagonist

Chemical Name: 4-[3-(Trifluoromethyl)-2-pyridinyl]-N-[5-(trifluoromethyl)-2-pyridinyl]-1-piperazinecarboxamide

Purity: ≥99% (HPLC)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

Reversible, competitive and potent TRPV1 antagonist (pK_i values are 6.5, 7.1 and 7.3 at rat, guinea pig and human TRPV1 respectively). Inhibits capsaicin- and H⁺-induced channel activation (pIC₅₀ values are 6.32 and 7.23 respectively) and exhibits antitussive and analgesic activity in vivo.

Compound Libraries

JNJ 17203212 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt	419.32
Formula	C₁₇H₁₅F₆N₅O
Storage	Store at +4°C
Purity	≥99% (HPLC)
CAS Number	821768-06-3
PubChem ID	11339118
InChI Key	JFRYYGVYCWYIDQ-UHFFFAOYSA-N
Smiles	O=C(NC3=NC=C(C(F)(F)F)C=C3)N(CC2)CCN2C1=C(C(F)(F)F)C=CC=N1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	41.93	100
	ethanol	41.93	100

Preparing Stock Solutions

The following data is based on the product molecular weight 419.32. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.38 mL	11.92 mL	23.85 mL
5 mM	0.48 mL	2.38 mL	4.77 mL
10 mM	0.24 mL	1.19 mL	2.38 mL
50 mM	0.05 mL	0.24 mL	0.48 mL

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

References

References are publications that support the products' biological activity.

Swanson et al (2005) Identification and biological evaluation of 4-(3-trifluoromethylpyridin-2-yl)piperazine-1-carboxylic acid (5-trifluoromethylpyridin-2-yl)amide, a high affinity TRPV1 (VR1) vanilloid receptor antagonist. J.Med.Chem. 48 1857 PMID: 15771431

Ghilardi et al (2005) Selective blockade of the capsaicin receptor TRPV1 attenuates bone cancer pain. J.Neurosci. 25 3126 PMID: 15788769

Bhattacharya et al (2007) Pharmacology and antitussive efficacy of 4-(3-trifluoromethyl-pyridin-2-yl)-piperazine-1-carboxylic acid (5-trifluoromethyl-pyridin-2-yl)-amide (JNJ17203212), a transient receptor potential vanilloid 1 antagonist in guinea pigs. J.Pharmacol.Exp.Ther. 323 665 PMID: 17690251

Keywords: JNJ 17203212, supplier, Reversible, competitive, potent, TRPV1, antagonists, Vanillioid, Receptors, VR1, Channels, Transient, Receptor, Potential, JNJ17203212, TRPV, TRPV, Tocris Bioscience

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