[CAS NO. 1355050-21-3] GS-443902trisodium
PRODUCTS SPECIFICATIONS [1355050-21-3]
DESCRIPTION [1355050-21-3]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 597.15 |
| Molecular Formula | C12H13N5Na3O13P3 |
| SMILES | O=P(OP(O)(O[Na])=O)(O[Na])OP(OC[C@@H](O1)[C@@H](O)[C@@H](O)[C@]1(C#N)C2=CC=C3N2N=CN=C3N)(O[Na])=O |
7 Publications Citing Use of MCE
Summary
In Vitro
In a continuous 72 h incubation of 1 µM Remdesivir (GS-5734), the GS-443902 trisodium (GS-441524 triphosphate trisodium; Remdesivir metabolite trisodium) level is measured at 2, 24, 48 and 72 h, and reaches a C
max
of 300, 110, and 90 pmol/million cells in macrophages, HMVEC, and HeLa cells lines respectively
[1]
.
GS-443902 trisodium (compound 8a) is a triphosphates (TP) derivative
[2]
.
GS-443902 trisodium (NTP; 0.01, 0.1, 1, 10, 100 μM) inhibits RSV RdRp-catalysed RNA synthesis by incorporating into the nascent viral RNA transcript and causing its premature termination. GS-5734 selectively inhibits EBOV replication by targeting its RdRp and inhibiting viral RNA synthesis following efficient intracellular conversion to GS-443902 sodium
[3]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Remdesivir (GS-5734; 10 mg kg; i.v.) rapidly distributes into peripheral blood mononuclear cells (PBMCs), and efficient conversion to GS-443902 trisodium (Remdesivir metabolite trisodium; NTP) is apparent within 2 h of dose administration in rhesus monkeys. In PBMCs, GS-443902 trisodium represents the predominant metabolite and is persistent with a t
1/2
of 14 h and levels required for >50% virus inhibition for 24 hours
[3]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Shipping with dry ice.
Storage
-80°C, protect from light, stored under nitrogen
* The compound is unstable in solutions, freshly prepared is recommended.
Solvent & Solubility
H 2 O : 33.33 mg/mL ( 55.82 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.6746 mL | 8.3731 mL | 16.7462 mL |
| 5 mM | 0.3349 mL | 1.6746 mL | 3.3492 mL |
| 10 mM | 0.1675 mL | 0.8373 mL | 1.6746 mL |
-
1.
Add each solvent one by one: PBS
Solubility: 50 mg/mL (83.73 mM); Clear solution; Need ultrasonic
References
- [1] Siegel D, et al. Discovery and Synthesis of a Phosphoramidate Prodrug of a Pyrrolo[2,1-f][triazin-4-amino] Adenine C-Nucleoside (GS-5734) for the Treatment of Ebola and Emerging Viruses. Med Chem. 2017 Mar 9;60(5):1648-1661.
- [2] Warren TK, et al. Therapeutic efficacy of the small molecule GS-5734 against Ebola virus in rhesus monkeys. Nature. 2016 Mar 17;531(7594):381-5.
- [3] Cho A, et al. Synthesis and antiviral activity of a series of 1'-substituted 4-aza-7,9-dideazaadenosine C-nucleosides. Bioorg Med Chem Lett. 2012 Apr 15;22(8):2705-7.