2. Cytoskeleton
  3. Integrin
  4. Bexotegrast

Bexotegrast  (Synonyms: PLN-74809)

Cat. No.: HY-137561 Purity: 98.94%
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Bexotegrast (PLN-74809) is an orally active, potent dual αvβ6/αvβ1 integrin inhibitor with Kd of 5.7 nM and 3.4 nM, respectively. Bexotegrast inhibits αvβ6- and αvβ1-induced TGF-β activation with IC50 values of 29.8 nM and 19.2 nM, respectively. Bexotegrast has antifibrogenic effects and block multiple avenues of TGF-β activation in the fibrotic lung.

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

Bexotegrast Chemical Structure

Bexotegrast Chemical Structure

CAS No. : 2376257-44-0

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Based on 1 publication(s) in Google Scholar

Other Forms of Bexotegrast:

Bexotegrast Related Antibodies

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αvβ1 αvβ3 αvβ5 αvβ6 αvβ8 α5β1 α1β1 α2β1 α4β1 α9β1 αIIbβ3 α4β7 αLβ2

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Description

Bexotegrast (PLN-74809) is an orally active, potent dual αvβ6/αvβ1 integrin inhibitor with Kd of 5.7 nM and 3.4 nM, respectively. Bexotegrast inhibits αvβ6- and αvβ1-induced TGF-β activation with IC50 values of 29.8 nM and 19.2 nM, respectively. Bexotegrast has antifibrogenic effects and block multiple avenues of TGF-β activation in the fibrotic lung[1][2].

IC50 & Target

αvβ6

5.7 nM (Kd)

αvβ1

3.4 nM (Kd)

In Vitro

Bexotegrast (PLN-74809; 1.82 µM; 7-day incubation) significantly reduces collagen type I alpha I (COL1A1) mRNA expression by 54% in precision-cut lung slices (PCLSs). PLN-74809 shows an approximately 50% reduction in Smad2 phosphorylation[2].
Bexotegrast (1.82 µM; 3-day incubation) dose-dependently reduces Col1a1 mRNA expression in PCLSs prepared from fibrotic mouse lungs by up to 71%[2].
Bexotegrast fully inhibits αvβ6 integrin-mediated adhesion to LAP by normal human bronchial epithelial cells with an IC50 of 39.3 nM[2].

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

Bexotegrast Related Antibodies
In Vivo

Bexotegrast (PLN-74809; orally; 100, 250, and 500 mg/kg twice daily; from Day 7 to Day 21) shows a dose-dependent, significant reduction in interstitial fibrillar collagen deposition in Bleomycin-challenged mice. Bexotegrast dose-dependently blocks Smad3 phosphorylation[2].

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

Animal Model: C57BL/6 mice[2]
Dosage: 100, 250, and 500 mg/kg
Administration: Orally; twice daily; from Day 7 to Day 21
Result: Showed a dose-dependent, significant reduction in interstitial fibrillar collagen deposition in Bleomycin (3 units/kg)-challenged mice.
Dose-dependently blocked Smad3 phosphorylation.
Molecular Weight

492.61

Formula

C27H36N6O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC([C@H](CCN(CCOC)CCCCC(N1)=CC=C2C1=NCCC2)NC3=NC=NC4=C3C=CC=C4)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

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

Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (507.50 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 2.0300 mL 10.1500 mL 20.3000 mL
5 mM 0.4060 mL 2.0300 mL 4.0600 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 and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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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 (4.22 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 (4.22 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.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  PBS

    Solubility: 12.5 mg/mL (25.38 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

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 and light)

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: 98.94%

SDS (252 KB)

COA (247 KB) HNMR (266 KB) RP-HPLC (274 KB) LCMS (96 KB)

Handling Instructions (2659 KB)
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 and light). 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 2.0300 mL 10.1500 mL 20.3000 mL 50.7501 mL
5 mM 0.4060 mL 2.0300 mL 4.0600 mL 10.1500 mL
10 mM 0.2030 mL 1.0150 mL 2.0300 mL 5.0750 mL
15 mM 0.1353 mL 0.6767 mL 1.3533 mL 3.3833 mL
20 mM 0.1015 mL 0.5075 mL 1.0150 mL 2.5375 mL
25 mM 0.0812 mL 0.4060 mL 0.8120 mL 2.0300 mL
30 mM 0.0677 mL 0.3383 mL 0.6767 mL 1.6917 mL
40 mM 0.0508 mL 0.2538 mL 0.5075 mL 1.2688 mL
50 mM 0.0406 mL 0.2030 mL 0.4060 mL 1.0150 mL
60 mM 0.0338 mL 0.1692 mL 0.3383 mL 0.8458 mL
80 mM 0.0254 mL 0.1269 mL 0.2538 mL 0.6344 mL
100 mM 0.0203 mL 0.1015 mL 0.2030 mL 0.5075 mL
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Bexotegrast 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:

Bexotegrast2376257-44-0PLN-74809PLN74809PLN 74809Integrinαvβ6αvβ1integrinTGF-βantifibrogenicfibrotic lungInhibitorinhibitorinhibit

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