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| Targets |
Fibroblast activation protein (FAP) and prolyl oligopeptidase (PREP); BR-102910 is a selective FAP inhibitor (antagonist) with an IC₅₀ of 2 nM. FAP is a serine protease that is overexpressed in the stroma of many cancers and in fibrotic tissues. It also inhibits PREP with an IC₅₀ of 49.00 μM. PREP is a prolyl endopeptidase involved in the regulation of neuropeptide levels and has been implicated in various diseases, including type 2 diabetes.
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| ln Vitro |
In vitro, BR-102910 shows potent inhibition of FAP with an IC₅₀ of 2 nM. It also inhibits PREP, though with lower potency (IC₅₀ of 49.00 μM). The compound's selectivity for FAP over PREP is significant, suggesting it may be a useful tool for studying FAP biology. The compound is typically dissolved in DMSO for in vitro assays. Its effects on FAP activity can be measured using standard enzyme activity assays.
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| ln Vivo |
In a dose-dependent manner, BR102910 (C57BL/6J mice, 0-30 mg/kg, po, once) exhibits a substantial suppression of FAP [1].
In vivo, BR-102910 (0-30 mg/kg; p.o.; once) exhibits a substantial suppression of FAP in a dose-dependent manner in C57BL/6J mice. The compound is administered orally. This in vivo efficacy supports its potential for studying FAP-related diseases, such as cancer and fibrosis. The compound is also being investigated for its potential in type 2 diabetes research. The animal model used is C57BL/6J mice with 5 mice per group. |
| Enzyme Assay |
To assess FAP inhibitory activity, enzyme assays are performed using recombinant FAP and a fluorogenic substrate. BR-102910 is incubated with the enzyme at various concentrations, and the IC₅₀ is determined by measuring the inhibition of substrate cleavage. The compound is typically dissolved in DMSO and diluted in assay buffer. The assays are conducted under conditions optimized for FAP activity. Similar protocols can be used to assess PREP inhibition. These protocols are for research purposes only and have not been independently validated by all suppliers.
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| Animal Protocol |
Animal/Disease Models: C57BL/6J mice (n = 5 per group) [1]
Doses: 0, 10 and 30 mg/kg Route of Administration: Orally, once Experimental Results: Demonstrated significant FAP inhibition in a dose-dependent manner effect. In vivo efficacy is evaluated in C57BL/6J mice. BR-102910 is administered orally at doses of 0, 10, and 30 mg/kg. The animals are treated once, and FAP inhibition is measured in relevant tissues or plasma. The compound demonstrates significant FAP inhibition in a dose-dependent manner. This protocol is used to assess the in vivo activity of the FAP inhibitor. All procedures are conducted in accordance with institutional animal care guidelines and are for research use only. |
| ADME/Pharmacokinetics |
BR-102910 has a molecular weight of 459.3 and the chemical formula C₁₈H₁₄Cl₂F₂N₄O₂S. It is soluble in DMSO at approximately 100 mg/mL (217.72 mM). The compound has a logP of 3.9, indicating moderate lipophilicity. It should be stored as a powder at -20°C for up to 3 years and at 4°C for up to 2 years. In solvent, it is stable at -80°C for 6 months and at -20°C for 1 month. The compound should be protected from moisture and light.
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| Toxicity/Toxicokinetics |
Specific toxicity data for BR-102910 are not extensively documented. As a FAP inhibitor, it may affect tissues where FAP is expressed, such as the stroma of cancers and fibrotic tissues. The compound is for research use only and not for human therapeutic use. It should be handled with appropriate safety precautions, including the use of personal protective equipment. The compound should be stored in a sealed container in a cool, dry place away from incompatible materials.
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| References | |
| Additional Infomation |
BR-102910 is also known as BR102910. It is a selective fibroblast activation protein (FAP) inhibitor with an IC₅₀ of 2 nM. It also inhibits prolyl oligopeptidase (PREP) with an IC₅₀ of 49.00 μM. The compound may be utilized in type 2 diabetes research. It is supplied as a white to off-white solid powder and should be stored at -20°C. It is for research use only.
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| Molecular Formula |
C18H14CL2F2N4O2S
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| Molecular Weight |
459.297167301178
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| Exact Mass |
458.018
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| CAS # |
2505339-54-6
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| PubChem CID |
155754825
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| Appearance |
White to off-white solid powder
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| LogP |
3.9
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
29
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| Complexity |
692
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| Defined Atom Stereocenter Count |
1
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| SMILES |
ClC1=C(C=CC(=C1)CC1=NC(=CS1)C(NCC(N1CC(CC1C#N)(F)F)=O)=O)Cl
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| InChi Key |
JTSUDVSZJDOOJG-NSHDSACASA-N
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| InChi Code |
InChI=1S/C18H14Cl2F2N4O2S/c19-12-2-1-10(3-13(12)20)4-15-25-14(8-29-15)17(28)24-7-16(27)26-9-18(21,22)5-11(26)6-23/h1-3,8,11H,4-5,7,9H2,(H,24,28)/t11-/m0/s1
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| Chemical Name |
N-[2-[(2S)-2-cyano-4,4-difluoropyrrolidin-1-yl]-2-oxoethyl]-2-[(3,4-dichlorophenyl)methyl]-1,3-thiazole-4-carboxamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~217.72 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.44 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.44 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.2177 mL | 1.0886 mL | 2.1772 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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