| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg | |||
| Other Sizes |
| Targets |
SLF targets FK506-binding proteins (FKBPs), particularly FKBP12 and FKBP51. FKBPs are peptidyl-prolyl cis-trans isomerases (PPIases) that play roles in protein folding, trafficking, and signaling. FKBP12 is the primary target of the immunosuppressant drugs FK506 and rapamycin, while FKBP51 is involved in stress response and cancer. SLF binds to the FKBP12 active site with an IC₅0 of 2.6 microM and to FKBP51 with an affinity of 3.1 microM. By binding to FKBPs, SLF can modulate their PPIase activity and protein-protein interactions.
|
|---|---|
| ln Vitro |
The three fused scout fragments, KB02, KB03, and KB05, exhibit broad cysteine reactivity in the human proteome and cover two distinct electrophile groups (chloroacetamide and acrylamide). These fragments bind tightly and selectively to the SLF ligand, which is bound to the cytosolic prolyl isomerase FKBP12, which has been widely employed in research on ligand-induced protein degradation[3].
In vitro studies demonstrate that SLF is a synthetic ligand for FKBP12 and FKBP51 with potent binding affinities. The compound's binding to FKBP12 is characterized by an IC₅0 of 2.6 microM, while its affinity for FKBP51 is 3.1 microM. SLF increases Ca2+ influx and protein synthesis in cells, which may contribute to its effects on skeletal muscle function. The compound's in vitro activity is assessed using FKBP binding assays (e.g., fluorescence polarization, SPR, or competition binding with FK506), cellular calcium flux assays, and protein synthesis assays. Its utility in PROTAC synthesis has been demonstrated. |
| ln Vivo |
In vivo activity of SLF has been evaluated in models of central nervous system diseases and cancer. The compound's ability to increase Ca2+ influx and protein synthesis suggests potential applications in improving skeletal muscle function. However, detailed in vivo efficacy data are limited, and SLF is primarily used as a research tool for studying FKBP biology and for developing PROTAC molecules. As a synthetic ligand, SLF may be used to modulate FKBP activity in vivo, though its utility is primarily in research rather than therapeutic applications.
|
| Enzyme Assay |
In vitro enzyme/receptor binding assays for SLF involve measuring its binding affinity to FKBP12 and FKBP51. The assay typically uses purified recombinant FKBP proteins and a fluorescently labeled FK506 or rapamycin probe in a competition binding format. The compound is incubated with the FKBP protein and the probe, and the displacement of the probe is measured by fluorescence polarization or TR-FRET. IC₅0 values are calculated from dose-response curves. Binding affinity (Kd) may also be determined using surface plasmon resonance or isothermal titration calorimetry. The compound's PPIase activity inhibition is assessed using a standard chymotrypsin-coupled assay.
|
| Cell Assay |
Cellular assays for SLF are conducted to evaluate its effects on FKBP function and downstream signaling. Cells are treated with varying concentrations of the compound (typically 0.1-100 microM) for various time points. FKBP binding is confirmed using pull-down assays with FKBP-specific antibodies or by assessing the displacement of FK506 from FKBP. Calcium flux is measured using fluorescent calcium indicators such as Fluo-4. Protein synthesis is assessed by measuring incorporation of labeled amino acids or by Western blotting for specific proteins. The compound's effects on cell viability and proliferation are assessed using MTT or similar assays. Its utility in PROTAC-mediated protein degradation is evaluated by Western blotting for the target protein.
|
| Animal Protocol |
In vivo animal studies with SLF are limited, as the compound is primarily used as a research tool. For in vivo studies, SLF may be administered to animal models of central nervous system diseases or cancer to assess its effects on FKBP function and disease progression. However, detailed in vivo study protocols are not extensively reported in the literature. SLF may also be used in vivo as part of PROTAC molecules to induce targeted protein degradation. The compound's pharmacokinetic properties and toxicity profiles in animal models are not extensively characterized.
|
| ADME/Pharmacokinetics |
Pharmacokinetic properties of SLF have been partially characterized. The compound has a molecular weight of 524.65 g/mol and a molecular formula of C30H40N2O₆. It is soluble in ethanol (50 mg/mL) and is available in high purity (≥98%). The compound is typically stored at -20degC. Detailed PK parameters such as half-life, bioavailability, and volume of distribution are not extensively reported in the available literature. The compound's physicochemical properties suggest it may have reasonable bioavailability for research applications.
|
| Toxicity/Toxicokinetics |
Toxicological data for SLF are limited, as the compound is primarily used as a research tool rather than a therapeutic agent. The compound is not intended for human therapeutic use and is supplied for research purposes only. In cell-based assays, the compound is generally well-tolerated at concentrations used for FKBP binding studies (typically 0.1-100 microM). Higher concentrations may cause non-specific effects. Standard safety precautions should be followed when handling this compound. Specific toxicity profiles in animal models are not reported in the available literature.
|
| References | |
| Additional Infomation |
SLF is a synthetic ligand for FK506-binding proteins (FKBP12 and FKBP51) with an IC₅0 of 2.6 microM for FKBP12 and an affinity of 3.1 microM for FKBP51. It increases Ca2+ influx and protein synthesis to improve skeletal muscle function. SLF is used in the study of central nervous system diseases and cancer, and can be used in the synthesis of PROTAC molecules. The compound is not an FDA-approved drug and has no clinical indications. It is available in high purity (≥98%) and is typically stored at -20degC.
|
| Molecular Formula |
C30H40N2O6
|
|---|---|
| Molecular Weight |
524.65
|
| Exact Mass |
524.288
|
| CAS # |
195513-96-3
|
| Related CAS # |
SLF TFA;2378802-47-0
|
| PubChem CID |
35027274
|
| Appearance |
Light yellow to yellow ointment
|
| Density |
1.2±0.1 g/cm3
|
| Boiling Point |
656.9±65.0 °C at 760 mmHg
|
| Flash Point |
351.1±34.3 °C
|
| Vapour Pressure |
0.0±2.0 mmHg at 25°C
|
| Index of Refraction |
1.559
|
| LogP |
3.63
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
12
|
| Heavy Atom Count |
38
|
| Complexity |
802
|
| Defined Atom Stereocenter Count |
2
|
| SMILES |
O([C@@]([H])(C1C([H])=C([H])C([H])=C(C=1[H])N([H])[H])C([H])([H])C([H])([H])C1C([H])=C([H])C(=C(C=1[H])OC([H])([H])[H])OC([H])([H])[H])C([C@]1([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])N1C(C(C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])C([H])([H])[H])=O)=O)=O
|
| InChi Key |
IIDSDBBDZNDWCN-BJKOFHAPSA-N
|
| InChi Code |
InChI=1S/C30H40N2O6/c1-6-30(2,3)27(33)28(34)32-17-8-7-12-23(32)29(35)38-24(21-10-9-11-22(31)19-21)15-13-20-14-16-25(36-4)26(18-20)37-5/h9-11,14,16,18-19,23-24H,6-8,12-13,15,17,31H2,1-5H3/t23-,24+/m0/s1
|
| Chemical Name |
[(1R)-1-(3-aminophenyl)-3-(3,4-dimethoxyphenyl)propyl] (2S)-1-(3,3-dimethyl-2-oxopentanoyl)piperidine-2-carboxylate
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : 100 mg/mL (190.60 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.96 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 20.8 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: ≥ 2.08 mg/mL (3.96 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 20.8 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 | 1.9060 mL | 9.5302 mL | 19.0603 mL | |
| 5 mM | 0.3812 mL | 1.9060 mL | 3.8121 mL | |
| 10 mM | 0.1906 mL | 0.9530 mL | 1.9060 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
