An FKBP51 inhibitor
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SAfit2

Item No. 24366

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(2S)-1-[(2S)-2-cyclohexyl-2-(3,4,5-trimethoxyphenyl)acetyl]-2-piperidinecarboxylic acid, (1R)-3-(3,4-dimethoxyphenyl)-1-[3-[2-(4-morpholinyl)ethoxy]phenyl]propyl ester
CAS Number
1643125-33-0
Molecular Formula
C46H62N2O10
Formula Weight
803.0
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 50 mg/mlDMSO: 50 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/mlEthanol: 10 mg/ml
λmax
207, 281 nm
SMILES
O=C([C@H]1N(C([C@H](C2=CC(OC)=C(OC)C(OC)=C2)C3CCCCC3)=O)CCCC1)O[C@H](CCC4=CC(OC)=C(OC)C=C4)C5=CC(OCCN6CCOCC6)=CC=C5
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
InChi Key
ZDBWLRLGUBSLPG-FDHYQTMZSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $143

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    1 mg

    $268

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    5 mg

    $913

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    Product Description

    SAfit2 is a potent inhibitor of FK506-binding protein 51 (FKBP51; Ki = 6 nM).1 It is highly selective for FKBP51 over FKBP52 (Ki = >50,000 nM) and has increased brain permeability in comparison to SAfit1. SAfit2 (20 mg/kg) enhances HPA axis suppression in mice by decreasing plasma corticosterone levels to a greater extent than in control mice following dexamethasone administration. It also does not increase plasma corticosterone levels as high as in control mice following subsequent administration of corticotropin-releasing factor (CRF). It decreases the time spent immobile in the forced swim test and increases the time spent in the open arms of the elevated plus maze, indicating antidepressant-like and anxiolytic-like activity, respectfully.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Gaali, S., Kirschner, A., Cuboni, S., et al. Selective inhibitors of the FK506-binding protein 51 by induced fit. Nat. Chem. Biol. 11(1), 33-37 (2015).

    2. Hartmann, J., Wagner, K.V., Gaali, S., et al. Pharmacological inhibition of the psychiatric risk factor FKBP51 has anxiolytic properties. J. Neurosci. 35(24), 9007-9016 (2015).