| Identification | Back Directory | [Name]
Pimodivir | [CAS]
1629869-44-8 | [Synonyms]
VX-787
CS-2483
Pimodivir
VRT0928787
VRT-0928787
VRT 0928787
Pimodivir (VX-787)
VX-787 (Pimodivir)
VX-787; VX 787; VX787; JNJ-872; JNJ 872; JNJ872; VRT-0928787; VRT 0928787; VRT0928787;PIMODIVIR
(2S,3S)-3-[[5-Fluoro-2-(5-fluoro-1H-pyrrolo[2,3-b]pyridin-3-yl)-4-pyrimidinyl]amino]bicyclo[2.2.2]octane-2-carboxylic acid
Bicyclo[2.2.2]octane-2-carboxylic acid, 3-[[5-fluoro-2-(5-fluoro-1H-pyrrolo[2,3-b]pyridin-3-yl)-4-pyrimidinyl]amino]-, (2S,3S)- | [Molecular Formula]
C20H19F2N5O2 | [MDL Number]
MFCD31382121 | [MOL File]
1629869-44-8.mol | [Molecular Weight]
399.39 |
| Chemical Properties | Back Directory | [density ]
1.501±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO, not in water:100.0(Max Conc. mg/mL);250.38(Max Conc. mM) | [form ]
A solid | [pka]
4.32±0.40(Predicted) | [color ]
White to light yellow | [InChIKey]
JGPXDNKSIXAZEQ-SBBZOCNPSA-N | [SMILES]
C12CCC(CC1)[C@H](NC1C(F)=CN=C(C3C4=CC(F)=CN=C4NC=3)N=1)[C@H]2C(O)=O |
| Hazard Information | Back Directory | [Description]
Pimodivir is an inhibitor of influenza virus polymerase basic protein 2 (PB2; KD = <0.003 μM). It also binds to glycogen synthase kinase 3β (GSK3β; Ki = ~1.6 μM) and inhibits the activity of Axl and calcium/calmodulin-dependent protein kinase IIβ (CaMKIIβ) by greater than 50% in a panel of 65 human and rat kinases. Pimodivir decreases the replication of seven adamantine- and neuraminidase inhibitor-resistant strains of influenza virus A (EC50s = <0.15-2.8 nM in a cell-based assay). It increases the antiviral activity of oseltamivir , zanamivir , and favipiravir (T-705; ) with 50% combination index (CI50) values of 0.58, 0.64, and 0.89, respectively, in a cell-based assay. Pimodivir increases survival in a mouse model of intranasal influenza A infection when administered at doses of 1, 3, and 10 mg/kg twice per day. | [Uses]
Pimodivir is an orally bioavailable azaindole inhibitor of influenza PB2. | [in vivo]
Pimodivir (2, 6, and 20 mg/kg/day, p.o.) and GS 4071 (20 mg/kg/day) completely prevent death in the H1N1pdm virus infection in mice. Pimodivir (20 mg/kg/day) is more effective than GS 4071 (20 mg/kg/day) in improving body weight and reducing the severity of lung infection[1].
Moreover, Pimodivir (VX-787) shows 100% survival in a +48 h delay to treatment mouse influenza model at 10, 3 and 1 mpk (BID × 10 days) whereas the SOC, GS 4071, provide no survival benefit in this model at 10 mpk[3].
Pimodivir (VX-787; 1, 3, or 10 mg/kg, bid) provided complete survival, with a dose-dependent reduction in BW loss of the mice[4].
| [storage]
Store at -20°C | [References]
[1] MICHAEL P. CLARK*. Discovery of a Novel, First-in-Class, Orally Bioavailable Azaindole Inhibitor (VX-787) of Influenza PB2[J]. Journal of Medicinal Chemistry, 2014, 57 15: 6668-6678. DOI: 10.1021/jm5007275
[2] RANDAL A BYRN. Preclinical activity of VX-787, a first-in-class, orally bioavailable inhibitor of the influenza virus polymerase PB2 subunit.[J]. Antimicrobial Agents and Chemotherapy, 2015: 1569-1582. DOI: 10.1128/aac.04623-14 |
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xinguokeji Gold
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13120711461 |
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