1. Metabolic Enzyme/Protease
  2. Prolyl Endopeptidase (PREP)
  3. BR102910

BR102910 is a selective fibroblast activation protein (FAP) inhibitor with the IC50 of 2 nM. BR102910 also inhibits prolyl oligopeptidase (PREP) with the IC50 of 49.00 μM. BR102910 can be used for the researchof type 2

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

BR102910 Chemical Structure

BR102910 Chemical Structure

CAS No. : 2505339-54-6

Size Price Stock Quantity
5 mg USD 667 In-stock
10 mg USD 1127 In-stock
25 mg USD 2185 In-stock
50 mg USD 3680 In-stock
100 mg USD 5520 In-stock
200 mg   Get quote  
500 mg   Get quote  

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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

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Description

BR102910 is a selective fibroblast activation protein (FAP) inhibitor with the IC50 of 2 nM. BR102910 also inhibits prolyl oligopeptidase (PREP) with the IC50 of 49.00 μM. BR102910 can be used for the researchof type 2

IC50 & Target

IC50: 2 nM (FAP), 49.0 μM (PREP), >100 μM (DPP-4)[1]

In Vivo

BR102910 (C57BL/6J mice, 0-30 mg/kg, Orally, once) shows significant FAP inhibition in a dose dependent manner[1].

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

Animal Model: C57BL/6J mice (n = 5 per group)[1]
Dosage: 0, 10 and 30 mg/kg
Administration: Orally, once
Result: Showed significant FAP inhibition in a dose dependent manner.
Molecular Weight

459.30

Formula

C18H14Cl2F2N4O2S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CSC(CC2=CC=C(Cl)C(Cl)=C2)=N1)NCC(N3[C@H](C#N)CC(F)(F)C3)=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 : 100 mg/mL (217.72 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 2.1772 mL 10.8861 mL 21.7723 mL
5 mM 0.4354 mL 2.1772 mL 4.3545 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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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    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.44 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 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.44 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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
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 2.1772 mL 10.8861 mL 21.7723 mL 54.4307 mL
5 mM 0.4354 mL 2.1772 mL 4.3545 mL 10.8861 mL
10 mM 0.2177 mL 1.0886 mL 2.1772 mL 5.4431 mL
15 mM 0.1451 mL 0.7257 mL 1.4515 mL 3.6287 mL
20 mM 0.1089 mL 0.5443 mL 1.0886 mL 2.7215 mL
25 mM 0.0871 mL 0.4354 mL 0.8709 mL 2.1772 mL
30 mM 0.0726 mL 0.3629 mL 0.7257 mL 1.8144 mL
40 mM 0.0544 mL 0.2722 mL 0.5443 mL 1.3608 mL
50 mM 0.0435 mL 0.2177 mL 0.4354 mL 1.0886 mL
60 mM 0.0363 mL 0.1814 mL 0.3629 mL 0.9072 mL
80 mM 0.0272 mL 0.1361 mL 0.2722 mL 0.6804 mL
100 mM 0.0218 mL 0.1089 mL 0.2177 mL 0.5443 mL
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BR102910 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.

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BR102910
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