JNJ-2408068 - CAS 317846-22-3
Catalog number: 317846-22-3
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C22H30N6O
Molecular Weight:
394.52
COA:
Inquire
Targets:
Others
Description:
JNJ-2408068 is a potent inhibitor of respiratory syncytial virus (RSV), exhibits potent antiviral activity with 50% effective concentrations (EC50s) of 1.4 and 2.1 nM, respectively.
Purity:
≥98%
Appearance:
Solid powder
Synonyms:
R170591; R-170591; R 170591; HE066500; HE-066500; HE 066500; JNJ-2408068; JNJ 2408068; JNJ2408068. 2-[[2-[[1-(2-aminoethyl)piperidin-4-yl]amino]-4-methylbenzimidazol-1-yl]methyl]-6-methylpyridin-3-ol;
Solubility:
Soluble in DMSO
Storage:
Store at -20 °C
MSDS:
Inquire
Application:
Respiratory syncytial virus inhibitor
Quality Standard:
Enterprise standard
Shelf Life:
As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly.
Quantity:
Milligrams-Grams
InChIKey:
RDQSNNMSDOHAPG-UHFFFAOYSA-N
InChI:
1S/C22H30N6O/c1-15-4-3-5-19-21(15)26-22(25-17-8-11-27(12-9-17)13-10-23)28(19)14-18-20(29)7-6-16(2)24-18/h3-7,17,29H,8-14,23H2,1-2H3,(H,25,26)
Canonical SMILES:
CC1=C2C(=CC=C1)N(C(=N2)NC3CCN(CC3)CCN)CC4=C(C=CC(=N4)C)O
Current Developer:
Johnson & Johnson
1.Cold virus fusion or stopping fusion cold--inhibitors of the human respiratory syncytial virus F protein.
Del Vecchio AM;Sarisky RT Recent Pat Antiinfect Drug Discov. 2006 Jun;1(2):247-54.
Human respiratory syncytial virus (HRSV) is a major respiratory viral pathogen causing moderate to severe upper and lower respiratory tract infections in all ages and across a wide range of patient populations. There are no currently approved vaccines and although a number of candidates are in various stages of development, the challenges are quite substantial. Presently, only a single agent is approved for HRSV prophylaxis, and therapeutic treatment options are severely limited and ineffective, particularly in the infant population. Antibody prophylaxis is restricted to use in populations at high-risk for hospitalization (infants under 35 weeks gestational age, infants with chronic lung disease, and infants with congenital heart disease). Aerosol administration of the guanosine analog ribavirin has been approved for the treatment of severe HRSV LRTI in both children and mechanically ventilated patients; however, there is still debate over its overall benefit and the risks associated with its use. Current therapy for those hospitalized due to HRSV is supportive. As such, there is great medical need for the development of agents to prevent and treat HRSV infections in all populations.
2.Small molecules VP-14637 and JNJ-2408068 inhibit respiratory syncytial virus fusion by similar mechanisms.
Douglas JL;Panis ML;Ho E;Lin KY;Krawczyk SH;Grant DM;Cai R;Swaminathan S;Chen X;Cihlar T Antimicrob Agents Chemother. 2005 Jun;49(6):2460-6.
Here we present data on the mechanism of action of VP-14637 and JNJ-2408068 (formerly R-170591), two small-molecule inhibitors of respiratory syncytial virus (RSV). Both inhibitors exhibited potent antiviral activity with 50% effective concentrations (EC50s) of 1.4 and 2.1 nM, respectively. A similar inhibitory effect was observed in a RSV-mediated cell fusion assay (EC50=5.4 and 0.9 nM, respectively). Several drug-resistant RSV variants were selected in vitro in the presence of each compound. All selected viruses exhibited significant cross-resistance to both inhibitors and contained various single amino acid substitutions in two distinct regions of the viral F protein, the heptad repeat 2 (HR2; mutations D486N, E487D, and F488Y), and the intervening domain between HR1 and HR2 (mutation K399I and T400A). Studies using [3H]VP-14637 revealed a specific binding of the compound to RSV-infected cells that was efficiently inhibited by JNJ-2408068 (50% inhibitory concentration=2.9 nM) but not by the HR2-derived peptide T-118. Further analysis using a transient T7 vaccinia expression system indicated that RSV F protein is sufficient for this interaction. F proteins containing either the VP-14637 or JNJ-2408068 resistance mutations exhibited greatly reduced binding of [3H]VP-14637.
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