2. Anti-infection
  3. HBV
  4. NVR 3-778

NVR 3-778 is a first-in-Class and oral bioavailable HBV CAM (capsid assembly modulator) belonging to the SBA (sulfamoylbenzamide) class, with anti-HBV activity.

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NVR 3-778

NVR 3-778 構造式

CAS 番号 : 1445790-55-5

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 165 在庫あり
Solution
10 mM * 1 mL in DMSO USD 165 在庫あり
Solid
5 mg $150 在庫あり
10 mg $230 在庫あり
25 mg $450 在庫あり
50 mg $680 在庫あり
100 mg $980 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

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Based on 3 publication(s) in Google Scholar

Other Forms of NVR 3-778:

NVR 3-778 関連抗体

Top Publications Citing Use of Products

  • 生物活性

  • 純度とドキュメンテーション

  • 参考文献

  • カスタマーレビュー

製品説明

NVR 3-778 is a first-in-Class and oral bioavailable HBV CAM (capsid assembly modulator) belonging to the SBA (sulfamoylbenzamide) class, with anti-HBV activity[1].

IC50 & Target

HBV[1]
Cellular Effect
Cell Line Type Value Description References
HepG2 2.2.15 CC50
15.3 μM
Compound: 1
Cytotoxicity against human HepG2.2.15 cells assessed as reduction in cell viability
Cytotoxicity against human HepG2.2.15 cells assessed as reduction in cell viability
[PMID: 33610748]
HepG2 2.2.15 CC50
15.3 μM
Compound: 1; NVR 3-778
Cytotoxicity against human HepG2.2.15 cells assessed as reduction in cell viability incubated for 3 days followed by replacement of fresh medium containing compound and measured after 3 days by cell titer glo-based luminescence assay
Cytotoxicity against human HepG2.2.15 cells assessed as reduction in cell viability incubated for 3 days followed by replacement of fresh medium containing compound and measured after 3 days by cell titer glo-based luminescence assay
[PMID: 31227344]
HepG2 2.2.15 CC50
4.81 μM
Compound: NVR3-778
Cytotoxicity against human HepG2.2.15 cells
Cytotoxicity against human HepG2.2.15 cells
[PMID: 32173194]
HepG2 2.2.15 CC50
8.6 μM
Compound: NVR 3-778
Cytotoxicity against human HepG2 2.2.15 cells assessed as reduction in cell viability incubated for 5 days by MTT assay
Cytotoxicity against human HepG2 2.2.15 cells assessed as reduction in cell viability incubated for 5 days by MTT assay
[PMID: 33603970]
HepG2 2.2.15 IC50
0.26 μM
Compound: NVR3-778
Antiviral activity against Hepatitis B virus infected in human HepG2.2.15 cells by solid phase radioimmunoassay
Antiviral activity against Hepatitis B virus infected in human HepG2.2.15 cells by solid phase radioimmunoassay
[PMID: 32173194]
体外実験

NVR 3-778 targets HBV core protein and inhibits viral replication[1].
NVR 3-778 inhibits the generation of infectious HBV DNA-containing virus particles with a mean antiviral with an EC50 of 0.40?μM in HepG2.2.15 cells[1].
NVR 3-778 exhibits pan-genotypic antiviral activity and a lack of cross-resistance with nucleos(t)ide inhibitors of HBV replication[1].
NVR 3-778 inhibits pregenomic RNA encapsidation, viral replication, and the production of HBV DNA- and HBV RNA-containing particles[1].
NVR 3-778 also inhibits de novo infection and viral replication in primary human hepatocytes with EC50s of 0.81?μM against HBV DNA and between 3.7μM and 4.8?μM against the production of HBV antigens and intracellular HBV RNA[1].
The EC50 values of NVR 3-778 are increased by 4.5-, 9.3-, and 15.8-fold in the presence of 10%, 20%, and 40% human serum, respectively[1].

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

NVR 3-778 関連抗体
体内実験

NVR 3-778 (1.5?mg/kg; i.g.) displays the mean Cmax and AUC0–inf values of 0.56?μg/ml and 3.50?μg·h/ml, respectively, in dogs following oral administration. And the mean oral bioavailability is determined to be 84.6%[1].

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

Animal Model: Dogs[1]
Dosage: 1.5 mg/kg (Pharmacokinetic Analysis)
Administration: Oral gavage
Result: The mean Cmax and AUC0–inf values are 0.56 µg/ml and 3.50 µg·h/ml and the oral bioavailability is 84.6%.
臨床実験
分子量

432.39

分子式

C18H16F4N2O4S
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=CC(F)=C(F)C(F)=C1)C2=CC=C(F)C(S(=O)(N3CCC(O)CC3)=O)=C2
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 250 mg/mL (578.18 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 2.3127 mL 11.5636 mL 23.1273 mL
5 mM 0.4625 mL 2.3127 mL 4.6255 mL
10 mM 0.2313 mL 1.1564 mL 2.3127 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. 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)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

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 (4.81 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 (4.81 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    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).
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.
純度とドキュメンテーション

純度: 99.88%

COA (247 KB) LCMS (94 KB)

取扱説明書 (2659 KB)
参考文献

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. 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 2.3127 mL 11.5636 mL 23.1273 mL 57.8182 mL
5 mM 0.4625 mL 2.3127 mL 4.6255 mL 11.5636 mL
10 mM 0.2313 mL 1.1564 mL 2.3127 mL 5.7818 mL
15 mM 0.1542 mL 0.7709 mL 1.5418 mL 3.8545 mL
20 mM 0.1156 mL 0.5782 mL 1.1564 mL 2.8909 mL
25 mM 0.0925 mL 0.4625 mL 0.9251 mL 2.3127 mL
30 mM 0.0771 mL 0.3855 mL 0.7709 mL 1.9273 mL
40 mM 0.0578 mL 0.2891 mL 0.5782 mL 1.4455 mL
50 mM 0.0463 mL 0.2313 mL 0.4625 mL 1.1564 mL
60 mM 0.0385 mL 0.1927 mL 0.3855 mL 0.9636 mL
80 mM 0.0289 mL 0.1445 mL 0.2891 mL 0.7227 mL
100 mM 0.0231 mL 0.1156 mL 0.2313 mL 0.5782 mL
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NVR 3-778 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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.

Keywords:

NVR 3-7781445790-55-5HBVHepatitis B virusHepatitisBviruscapsidassemblymodulatorCAMchronichepatitisInhibitorinhibitorinhibit

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製品名:
NVR 3-778
製品番号:
HY-124600
数量:
MCE 日本正規代理店:

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