Pimodivir
Pimodivir Basic information
- Product Name:
- Pimodivir
- Synonyms:
-
- Pimodivir
- Pimodivir (VX-787)
- VX-787
- (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
- CS-2483
- VRT 0928787
- VRT0928787
- VRT-0928787
- CAS:
- 1629869-44-8
- MF:
- C20H19F2N5O2
- MW:
- 399.39
- Mol File:
- 1629869-44-8.mol
Pimodivir Chemical Properties
- 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
Pimodivir Usage And Synthesis
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].
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
PimodivirSupplier
- Tel
- 13120711461
- 363372932@qq.com
- Tel
- 025-58849295 18951903616;
- info@adooq.cn
- Tel
- 021-52996696，15000506266 15000506266
- Tel
- 021-61350663 13052117465
- sales@zehanbiopharma.com
- Tel
- 15850786624
- sales@cqpharm.com