2. Anti-infection
  3. RSV
  4. TMC353121

TMC353121 is a potent respiratory syncytial virus (RSV) fusion inhibitor with pEC50 of 9.9.

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

TMC353121 Chemical Structure

TMC353121 Chemical Structure

CAS No. : 857066-90-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 154 In-stock
Solution
10 mM * 1 mL in DMSO USD 154 In-stock
Solid
5 mg USD 125 In-stock
10 mg USD 200 In-stock
25 mg USD 390 In-stock
50 mg USD 620 In-stock
100 mg   Get quote  
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Customer Review

Based on 6 publication(s) in Google Scholar

TMC353121 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

TMC353121 is a potent respiratory syncytial virus (RSV) fusion inhibitor with pEC50 of 9.9.

IC50 & Target

pEC50: 9.9 (RSV)[1]
Cellular Effect
Cell Line Type Value Description References
M-HeLa CC50
4436 ng/mL
Compound: 56d
Cytotoxicity against human HeLaM cells by MTT assay
Cytotoxicity against human HeLaM cells by MTT assay
[PMID: 18254606]
In Vitro

TMC353121 shows activity against groups A and B RSV and against a panel of clinical isolates with equal potency[1]. TMC353121 is a potent RSV fusion inhibitor in vitro. TMC353121 is active against wild-type RSV (strain LO), with a 50% effective concentration (EC50) of 0.07 ng/mL in HeLaM cells[2].

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

TMC353121 Related Antibodies
In Vivo

After i.v. bolus administration of a single dose of 10 mg/kg to Sprague-Dawley rats, the plasma drug concentration-time profile of TMC353121 exhibits multicompartmental pharmacokinetics. Mean plasma drug concentrations decrease rapidly during the first hours after dosing and then more slowly, with a half-life of about 12 h, as determined for the last part of the curve between 8 and 24 h postdose. TMC353121 is rapidly eliminated from plasma (CL=8.6 liters/h/kg) and extensively distributed (Vss=55 liters/kg)[2]. TMC353121 is administered once, i.v. at 2.5 mg/kg or at 0.25 mg/kg. Drug levels are determined in lung tissue, serum, and BAL fluid at different time points. TMC353121 followed multicompartment pharmacokinetics, with a fast decay in serum within the first hour after i.v. injection, followed by a slower decay. The drug is eliminated quickly from the blood resulting in very low blood levels after 24 h. Lung concentrations are much higher than serum concentrations and in BAL fluid the drug is just above the limit of detection at 8 h after injection. Very low drug levels can still be detected in the lung 5 days after treatment[3].

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

558.71

Formula

C32H42N6O3
CAS No.
Appearance

Solid

Color

Pink to red

SMILES

OC1=CC=C(C)N=C1CN2C3=CC(CNC4=CC(C)=CC=C4CCCO)=CC=C3N=C2NCCCN5CCOCC5
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (89.49 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 1.7898 mL 8.9492 mL 17.8984 mL
5 mM 0.3580 mL 1.7898 mL 3.5797 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • 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: ≥ 2.5 mg/mL (4.47 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: 2.5 mg/mL (4.47 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 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 (25.0 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.
Purity & Documentation

Purity: ≥98.0%

SDS (251 KB)

COA (249 KB) HNMR (279 KB)

Handling Instructions (2659 KB)
References
Animal Administration
[2][3]

Rats[2]
Sprague-Dawley and cotton rats are given a single-bolus dose of 10 mg/kg TMC353121 intravenously (i.v.). Blood samples are taken from the orbital venous plexus of three Sprague-Dawley rats at 15 min and 1, 8, and 24 h postdose and from six Sprague-Dawley rats and six cotton rats at 3 h postdose. Blood samples are centrifuged at 1,500× g for 10 min, and plasma is separated and frozen until bioanalysis. After blood sampling, the rats are exsanguinated from the vena femoralis under isoflurane-oxygen anesthesia. Then they are euthanized by CO2 asphyxiation, and the lungs are subjected to lavage once via a tracheal cannula with phosphate-buffered saline (PBS) containing 2% bovine serum albumin (BSA) at room temperature at a volume of 5 mL per Sprague-Dawley rat or 2.5 mL per cotton rat. After gentle injection of the lavage fluid into the lungs, the fluid is withdrawn for collection of the bronchoalveolar lavage fluid (BALF) and the lungs are dissected. BALF is collected in order to assess TMC353121 concentrations in the lung epithelial lining fluid (ELF) after correction for the dilution with lavage fluid. A single lavage with a short dwelling time is applied as previously recommended for better accuracy of the determination of ELF dilution. BSA is added to the lavage fluid in order to prevent the adsorption of TMC353121 to syringes or other containers. The BALF is centrifuged at 300× g for 10 min, and the supernatant is separated. BALF supernatant and lung tissue samples are then frozen until bioanalysis. BALF supernatant is referred as BALF throughout this paper.
Mice[3]
Inbred 8- to 12-week-old female BALB/c mice are used. TMC353121 is administered intravenously in saline at doses of 0.25-10 mg/kg, and at various times in relation to the RSV infection. Mice are infected with 2×106 plaque-forming unit (PFU) of plaque-purified human strain RSV A2 (100 μL intranasally). Individual body weight is used to monitor animal health and response to infection, and is recorded daily.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7898 mL 8.9492 mL 17.8984 mL 44.7459 mL
5 mM 0.3580 mL 1.7898 mL 3.5797 mL 8.9492 mL
10 mM 0.1790 mL 0.8949 mL 1.7898 mL 4.4746 mL
15 mM 0.1193 mL 0.5966 mL 1.1932 mL 2.9831 mL
20 mM 0.0895 mL 0.4475 mL 0.8949 mL 2.2373 mL
25 mM 0.0716 mL 0.3580 mL 0.7159 mL 1.7898 mL
30 mM 0.0597 mL 0.2983 mL 0.5966 mL 1.4915 mL
40 mM 0.0447 mL 0.2237 mL 0.4475 mL 1.1186 mL
50 mM 0.0358 mL 0.1790 mL 0.3580 mL 0.8949 mL
60 mM 0.0298 mL 0.1492 mL 0.2983 mL 0.7458 mL
80 mM 0.0224 mL 0.1119 mL 0.2237 mL 0.5593 mL
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TMC353121 Related Classifications

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:

TMC353121857066-90-1TMC 353121TMC-353121RSVRespiratory syncytial virusInhibitorinhibitorinhibit

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