JNJ-17203212 | B2974

JNJ-17203212 is a reversible and potent antagonist of transient receptor potential vanilloid 1 (TRPV1) with pKi values of 6.5, 7.1 and 7.3 at rat, guinea pig and human TRPV1 respectively. It Inhibits capsaicin- and low pH- induced channel activation with pIC₅₀ values of 6.32 and 7.23 respectively. Intraperitoneal administration of JNJ17203212 (20 mg/kg) attenuates capsaicin evoked coughs. Chronic administration of JNJ-17203212 (30 mg/kg, s.c., twice daily) shows analgesic activity in an in vivo model of bone cancer pain.

JNJ-17203212 is a reversible and potent antagonist of transient receptor potential vanilloid 1 (TRPV1) with pKi values of 6.5, 7.1 and 7.3 at rat, guinea pig and human TRPV1 respectively. It Inhibits capsaicin- and low pH- induced channel activation with pIC₅₀ values of 6.32 and 7.23 respectively. Intraperitoneal administration of JNJ17203212 (20 mg/kg) attenuates capsaicin evoked coughs. Chronic administration of JNJ-17203212 (30 mg/kg, s.c., twice daily) shows analgesic activity in an in vivo model of bone cancer pain.

B2974 | JNJ-17203212 DataSheet

Alternate Name/Synonyms: 4-[3-(trifluoromethyl)pyridin-2-yl]-N-[5-(trifluoromethyl)pyridin-2-yl]piperazine-1-carboxamide

Appearance: Solid

Formulation:

CAS Number: 821768-06-3

Structure Available?: True

Peptide sequence:

Salt Form: false

Molecular Formula: C₁₇H₁₅F₆N₅O

Molecular Weight: 419.32

Cell-Permeable?: False

Purity: 98%

Solubilities: ~20 mg/ml in in DMSO

Handling: Do not take internally. Wear gloves and mask when handling the product! Avoid contact by all modes of exposure.

Country of Origin: USA

Tag Line: An antagonist of TRPV1

MDL Number: MFCD12828764

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

InChi: InChI=1S/C17H15F6N5O/c18-16(19,20)11-3-4-13(25-10-11)26-15(29)28-8-6-27(7-9-28)14-12(17(21,22)23)2-1-5-24-14/h1-5,10H,6-9H2,(H,25,26,29)

InChi Key: JFRYYGVYCWYIDQ-UHFFFAOYSA-N