1. Anti-infection
  2. SARS-CoV RSV Influenza Virus
  3. Mindeudesivir hydrobromide

Mindeudesivir hydrobromide  (Synonyms: VV116; GS-621763-d1 hydrobromide)

Cat. No.: HY-145119AS Purity: 99.46%
SDS COA Handling Instructions

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.

For research use only. We do not sell to patients.

Mindeudesivir hydrobromide Chemical Structure

Mindeudesivir hydrobromide Chemical Structure

CAS No. : 2779498-79-0

Size Price Stock Quantity
5 mg USD 340 In-stock
10 mg USD 440 In-stock
25 mg USD 850 In-stock
50 mg USD 1400 In-stock
100 mg USD 2200 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Mindeudesivir hydrobromide:

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  • Biological Activity

  • Purity & Documentation

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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[1][2].

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.

Cell Viability Assay

Cell Line: A549 (infected with RSV)[1]
Concentration: 0-1000 μM
Incubation Time: 48 hours
Result: Inhibited RSV replication in A549 cells with EC50 of 1.20 ± 0.32 μM, CC50 of 95.92 ± 9.27 μM and selectivity index (SI) of 80.
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 ± 0.14 0.42 ± 0.14 0.42 ± 0.14
Cmax (ng/mL) 5360 ± 560 11617 ± 3443 24017 ± 6521
AUC0-t (ng/mL·h) 11461 ± 1013 24594 ± 1059 47799 ± 6545
AUC0-∞ (ng/mL·h) 11534 ± 992 24739 ± 1028 48014 ± 6696
MRT0-∞ (ng/mL·h) 2.25 ± 0.32 2.15 ± 0.26 2.28 ± 0.53
Tmax (h) 2.30 ± 1.10 3.27 ± 1.92 4.25 ± 0.53

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Balb/c mice[1]
Dosage: 25, 50 and 100 mg/kg
Administration: PO; single dosage (Pharmacokinetics Analysis)
Result: Exhibited favorable PK properties and good safety profile.
Animal Model: Balb/c mice (6-8 weeks; intranasally infected with 4 × 10^6 FFU of RSV)[1]
Dosage: 25, 50 and 100 mg/kg
Administration: PO; b.i.d for 4 days
Result: Exhibited a stronger activity and decreased the virus titers below the detection limit at 50 mg/kg, also reduced lung injury after RSV infection.
Clinical Trial
Molecular Weight

583.45

Formula

C24H31DBrN5O7

CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

[H]Br.N#C[C@](O[C@@H]1COC(C(C)C)=O)(C2=CC([2H])=C3N2N=CN=C3N)[C@@H]([C@@H]1OC(C(C)C)=O)OC(C(C)C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (428.49 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7139 mL 8.5697 mL 17.1394 mL
5 mM 0.3428 mL 1.7139 mL 3.4279 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (3.57 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (3.57 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7139 mL 8.5697 mL 17.1394 mL 42.8486 mL
5 mM 0.3428 mL 1.7139 mL 3.4279 mL 8.5697 mL
10 mM 0.1714 mL 0.8570 mL 1.7139 mL 4.2849 mL
15 mM 0.1143 mL 0.5713 mL 1.1426 mL 2.8566 mL
20 mM 0.0857 mL 0.4285 mL 0.8570 mL 2.1424 mL
25 mM 0.0686 mL 0.3428 mL 0.6856 mL 1.7139 mL
30 mM 0.0571 mL 0.2857 mL 0.5713 mL 1.4283 mL
40 mM 0.0428 mL 0.2142 mL 0.4285 mL 1.0712 mL
50 mM 0.0343 mL 0.1714 mL 0.3428 mL 0.8570 mL
60 mM 0.0286 mL 0.1428 mL 0.2857 mL 0.7141 mL
80 mM 0.0214 mL 0.1071 mL 0.2142 mL 0.5356 mL
100 mM 0.0171 mL 0.0857 mL 0.1714 mL 0.4285 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Mindeudesivir hydrobromide
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