| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| Other Sizes |
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| ln Vitro |
Although FAP has been linked to cancer, its precise function is still unknown due to the lack of inhibitors that would separate it from other prolyl peptidases, such dipeptidyl peptidase 4 (DPP-4). FAP is specifically inhibited by Ac-Gly-BoroPro in contrast to other prolyl peptidases. Submicromolar concentrations of Ac-Gly-BoroPro react with FAP easily, and the inhibition levels reach steady-state quickly (Ki=23±3 nM). On the other hand, DPP-4 took longer to attain steady-state inhibition levels (Ki=377±18 nM) and required greater doses of Ac-Gly-BoroPro for inhibition. Other prolyl peptidases (DPP-7, DPP-8, DPP-9, prolyl oligopeptidase, and acyl peptide hydrolase) are inhibited by Ac-Gly-BoroPro with Ki values 9–5400 times greater than that of FAP inhibition. Ac-Gly-BoroPro's N-acyl linkage inhibits the inhibitor's N-terminus, reducing its nucleophilicity and decreasing the likelihood that it will cyclize [1].
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|---|---|
| References |
| Molecular Formula |
C8H15BN2O4
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|---|---|
| Molecular Weight |
214.026702165604
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| Exact Mass |
214.112
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| CAS # |
886992-99-0
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| PubChem CID |
102176419
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Index of Refraction |
1.520
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| LogP |
-1.21
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
15
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| Complexity |
259
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| Defined Atom Stereocenter Count |
1
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| SMILES |
B([C@H]1CCCN1C(=O)CNC(=O)C)(O)O
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| InChi Key |
UUOZISWTWURDGU-SSDOTTSWSA-N
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| InChi Code |
InChI=1S/C8H15BN2O4/c1-6(12)10-5-8(13)11-4-2-3-7(11)9(14)15/h7,14-15H,2-5H2,1H3,(H,10,12)/t7-/m1/s1
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| Chemical Name |
[(2S)-1-(2-acetamidoacetyl)pyrrolidin-2-yl]boronic acid
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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: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. (3). This product is not stable in solution, please use freshly prepared working solution for optimal results. |
| 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 : ≥ 50 mg/mL (~233.61 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (11.68 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% 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 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (11.68 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.6722 mL | 23.3612 mL | 46.7224 mL | |
| 5 mM | 0.9344 mL | 4.6722 mL | 9.3445 mL | |
| 10 mM | 0.4672 mL | 2.3361 mL | 4.6722 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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