2. Metabolic Enzyme/Protease
  3. Ser/Thr Protease
  4. Berotralstat dihydrochloride

Berotralstat dihydrochloride  (Synonyms: BCX7353 dihydrochloride)

Cat. No.: HY-109127A Purity: 98.49%
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Berotralstat dihydrochloride is a low toxicity, effective, highly specific, second-generation, synthetic and orally active plasma kallikrein inhibitor used for the research of hereditary angioedema (HAE) attacks. Berotralstat dihydrochloride works by blocking the enzymatic activity of plasma kallikrein in releasing bradykinin, the major biologic peptide that promotes swelling and pain associated with attacks of HAE.

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

Berotralstat dihydrochloride Chemical Structure

Berotralstat dihydrochloride Chemical Structure

CAS No. : 1809010-52-3

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 1748 In-stock
Solution
10 mM * 1 mL in DMSO USD 1748 In-stock
Solid
1 mg USD 420 In-stock
5 mg USD 1250 In-stock
10 mg USD 2000 In-stock
25 mg USD 3900 In-stock
50 mg USD 6000 In-stock
100 mg USD 9000 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

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

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Based on 1 publication(s) in Google Scholar

Other Forms of Berotralstat dihydrochloride:

Berotralstat dihydrochloride Related Antibodies

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Description

Berotralstat dihydrochloride is a low toxicity, effective, highly specific, second-generation, synthetic and orally active plasma kallikrein inhibitor used for the research of hereditary angioedema (HAE) attacks. Berotralstat dihydrochloride works by blocking the enzymatic activity of plasma kallikrein in releasing bradykinin, the major biologic peptide that promotes swelling and pain associated with attacks of HAE[1][2].

Clinical Trial
Molecular Weight

635.48

Formula

C30H28Cl2F4N6O
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(C1=CC(C(F)(F)F)=NN1C2=CC(CN)=CC=C2)NC3=CC([C@@H](C4=CC(C#N)=CC=C4)NCC5CC5)=CC=C3F.[H]Cl.[H]Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, stored under nitrogen, away from moisture

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

Solvent & Solubility
In Vitro: 

DMSO : 120 mg/mL (188.83 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 1.5736 mL 7.8681 mL 15.7361 mL
5 mM 0.3147 mL 1.5736 mL 3.1472 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 (stored under nitrogen, 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.

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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: ≥ 1.2 mg/mL (1.89 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.2 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.0 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: ≥ 1.2 mg/mL (1.89 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.2 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.0 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).

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, 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 (stored under nitrogen, 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 1.5736 mL 7.8681 mL 15.7361 mL 39.3403 mL
5 mM 0.3147 mL 1.5736 mL 3.1472 mL 7.8681 mL
10 mM 0.1574 mL 0.7868 mL 1.5736 mL 3.9340 mL
15 mM 0.1049 mL 0.5245 mL 1.0491 mL 2.6227 mL
20 mM 0.0787 mL 0.3934 mL 0.7868 mL 1.9670 mL
25 mM 0.0629 mL 0.3147 mL 0.6294 mL 1.5736 mL
30 mM 0.0525 mL 0.2623 mL 0.5245 mL 1.3113 mL
40 mM 0.0393 mL 0.1967 mL 0.3934 mL 0.9835 mL
50 mM 0.0315 mL 0.1574 mL 0.3147 mL 0.7868 mL
60 mM 0.0262 mL 0.1311 mL 0.2623 mL 0.6557 mL
80 mM 0.0197 mL 0.0984 mL 0.1967 mL 0.4918 mL
100 mM 0.0157 mL 0.0787 mL 0.1574 mL 0.3934 mL
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Berotralstat dihydrochloride 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:

Berotralstat1809010-52-3BCX7353BCX 7353BCX-7353Ser/Thr ProteaseSerine proteasesSerine endopeptidasesThreonine proteasesSafeEffectiveSpecificSecond-generationSyntheticOralSwellInhibitorinhibitorinhibit

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