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Mindeudesivir hydrobromide

MCE China：Mindeudesivir hydrobromide

Brand：MedChemExpress (MCE)

Cat. No.HY-145119AS

CAS：2779498-79-0

Synonyms：VV116; GS-621763-d1 hydrobromide

Purity：99.46%

Storage：4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Mindeudesivir (JT001; VV116; GS-621763-d1) hydrobromide is a deuterated version of Remdesivir (HY-104077), a highly orally active nucleoside antiviral against SARS-CoV-2 and respiratory syncytial virus (RSV). Mindeudesivir hydrobromide retains the antiviral activity of Remdesivir against COVID-19, and is the first domestically produced deuterium targeting the COVID-19.

In Vitro：Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].Potential advantages of deuterated compounds:(1) Extend the half-life in vivo. Deuterated compounds may be able to prolong the pharmacokinetic characteristics of the compound, that is, prolong the half-life in vivo. This can improve compound safety, efficacy and tolerability, and increase ease of administration. (2) Improve oral bioavailability. Deuterated compounds may reduce the degree of unwanted metabolism (first-pass metabolism) in the gut wall and liver, allowing a greater proportion of the unmetabolized drug to reach its target site of action. High bioavailability determines its activity at low doses and better tolerance. (3) Improve metabolic characteristics. Deuterated compounds may reduce the formation of toxic or reactive metabolites and improve drug metabolism. (4) Improve drug safety. Deuterated compounds may reduce or eliminate adverse side effects of pharmaceutical compounds and are safe. (5) Preserve the therapeutic properties. Deuterated compounds are expected to retain similar biochemical potency and selectivity to hydrogen analogs in previous studies.

In Vivo：VV116 (25, 50 and 100 mg/kg; PO; b.i.d for 4 days) exhibits a stronger activity and decreases the virus titers below the detection limit at 50 mg/kg, also reduces lung injury after RSV infection[1].VV116 (25, 50 and 100 mg/kg; PO; single dosage) exhibits favorable PK properties and good safety profile[1].Pharmacokinetic Parameters of VV116 (JT001) in Balb/c mice[1]. PO (25 mg/kg) PO (50 mg/kg) PO (100 mg/kg) Tmax (h)0.42 ± 0.140.42 ± 0.140.42 ± 0.14 Cmax (ng/mL)5360 ± 56011617 ± 344324017 ± 6521 AUC0-t (ng/mL·h)11461 ± 101324594 ± 105947799 ± 6545 AUC0-∞ (ng/mL·h)11534 ± 99224739 ± 102848014 ± 6696 MRT0-∞ (ng/mL·h)2.25 ± 0.322.15 ± 0.262.28 ± 0.53 Tmax (h)2.30 ± 1.103.27 ± 1.924.25 ± 0.53

IC50 & Target：SARS-CoV-2, RSV[1][2] In Vitro Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].Potential advantages of deuterated compounds:(1) Extend the half-life in vivo. Deuterated compounds may be able to prolong the pharmacokinetic characteristics of the compound, that is, prolong the half-life in vivo. This can improve compound safety, efficacy and tolerability, and increase ease of administration. (2) Improve oral bioavailability. Deuterated compounds may reduce the degree of unwanted metabolism (first-pass metabolism) in the gut wall and liver, allowing a greater proportion of the unmetabolized drug to reach its target site of action. High bioavailability determines its activity at low doses and better tolerance. (3) Improve metabolic characteristics. Deuterated compounds may reduce the formation of toxic or reactive metabolites and improve drug metabolism. (4) Improve drug safety. Deuterated compounds may reduce or eliminate adverse side effects of pharmaceutical compounds and are safe. (5) Preserve the therapeutic properties. Deuterated compounds are expected to retain similar biochemical potency and selectivity to hydrogen analogs in previous studies. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Mindeudesivir hydrobromide Related Antibodies Cell Viability Assay Cell Line: A549 (infected with RSV)[1]

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References：

[1]. Zhang R, et al. Oral remdesivir derivative VV116 is a potent inhibitor of respiratory syncytial virus with efficacy in mouse model. Signal Transduct Target Ther. 2022;7(1):123. Published 2022 Apr 16.  [Content Brief]

[2]. Qian HJ, et al. Safety, tolerability, and pharmacokinetics of VV116, an oral nucleoside analog against SARS-CoV-2, in Chinese healthy subjects [published online ahead of print, 2022 Mar 16]. Acta Pharmacol Sin. 2022;1-9.  [Content Brief]