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| Other Sizes |
SAFit2 (SA-Fit-2) is a novel and potent inhibitor of the FK506-binding protein 51 (FKBP51) with Ki of 6 nM. The FK506-binding protein 51 (FKBP51) is a key regulator of stress hormone receptors and an established risk factor for stress-related disorders.
| ln Vitro |
In 51KO cells, SAFit2 administration had no anti-FKBP51 panoramic effect, but it did raise the expression of pAKT2 (soleus and EDL ablated) and pAS160 (EDL ablated) in WT cells. Moreover, following SAFit2 administration, GLUT4 rose in the membrane fraction of primary EDL-expressing myotubes in WT cells but not in 51KO animals [2].
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| ln Vivo |
Under both control and high-fat diet (HFD) circumstances, it was discovered that SAFit2 led to weight loss for 30 days. When SAFit2 was applied an hour before testing, no changes in anxiety-related behaviors were seen. SAFit2 significantly increases phosphorylated AKT2 and AS160 in the EDL as well as increases GLUT4 expression on the soleus muscle membrane [2]. The elevated plus maze (EPM) significantly increased the open-arm time (z=-2.183, p<0.05) in response to the induction of treatment injection 16 hours prior to testing, indicating that SAFit2 induced an anxiolytic phenotype. The study found that the SAFit2 treatment led to a significant increase in both the delay time (z=-2-265, p<0.05) and travel distance (t(20)=-2.371, p<0.05) in the illuminated compartment.
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| References |
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| Molecular Formula |
C46H62N2O10
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| Molecular Weight |
802.991894245148
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| Exact Mass |
802.44
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| CAS # |
1643125-33-0
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| PubChem CID |
86277887
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| Appearance |
Off-white to pink solid powder
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| LogP |
8.2
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
19
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| Heavy Atom Count |
58
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| Complexity |
1200
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| Defined Atom Stereocenter Count |
3
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| SMILES |
O=C([C@H](C1C=C(C(=C(C=1)OC)OC)OC)C1CCCCC1)N1CCCC[C@H]1C(=O)O[C@@H](C1C=CC=C(C=1)OCCN1CCOCC1)CCC1C=CC(=C(C=1)OC)OC
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| InChi Key |
ZDBWLRLGUBSLPG-FDHYQTMZSA-N
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| InChi Code |
InChI=1S/C46H62N2O10/c1-51-39-20-18-32(28-40(39)52-2)17-19-38(34-14-11-15-36(29-34)57-27-24-47-22-25-56-26-23-47)58-46(50)37-16-9-10-21-48(37)45(49)43(33-12-7-6-8-13-33)35-30-41(53-3)44(55-5)42(31-35)54-4/h11,14-15,18,20,28-31,33,37-38,43H,6-10,12-13,16-17,19,21-27H2,1-5H3/t37-,38+,43-/m0/s1
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| Chemical Name |
[(1R)-3-(3,4-dimethoxyphenyl)-1-[3-(2-morpholin-4-ylethoxy)phenyl]propyl] (2S)-1-[(2S)-2-cyclohexyl-2-(3,4,5-trimethoxyphenyl)acetyl]piperidine-2-carboxylate
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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 |
| 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 (~124.53 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.11 mM) (saturation unknown) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
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 (2.59 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (2.59 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.2453 mL | 6.2267 mL | 12.4535 mL | |
| 5 mM | 0.2491 mL | 1.2453 mL | 2.4907 mL | |
| 10 mM | 0.1245 mL | 0.6227 mL | 1.2453 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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