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SAfit2

Product Name
SAfit2
CAS No.
1643125-33-0
Chemical Name
SAfit2
Synonyms
SAfit2;SAFit2, 10 mM in DMSO;(R)-3-(3,4-Dimethoxyphenyl)-1-(3-(2-morpholinoethoxy)phenyl)propyl (S)-1-((S)-2-cyclohexyl-2-(3,4,5-trimethoxyphenyl)acetyl)piperidine-2-carboxylate;(1R)-3-(3,4-dimethoxyphenyl)-1-{3-[2-(morpholin-4-yl)ethoxy]phenyl}propyl (2S)-1-[(2S)-2-cyclohexyl-2-(3,4,5-trimethoxyphenyl)acetyl]piperidine-2-carboxylate;2-Piperidinecarboxylic acid, 1-[(2S)-2-cyclohexyl-2-(3,4,5-trimethoxyphenyl)acetyl]-, (1R)-3-(3,4-dimethoxyphenyl)-1-[3-[2-(4-morpholinyl)ethoxy]phenyl]propyl ester, (2S)-
CBNumber
CB64666288
Molecular Formula
C46H62N2O10
Formula Weight
802.99
MOL File
1643125-33-0.mol
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SAfit2 Property

Boiling point:
877.0±65.0 °C(Predicted)
Density 
1.168±0.06 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMF: 50 mg/ml; DMSO: 50 mg/ml; DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml; Ethanol: 10 mg/ml
form 
A crystalline solid
pka
6.43±0.10(Predicted)
color 
Off-white to pink
InChIKey
ZDBWLRLGUBSLPG-FDHYQTMZSA-N
SMILES
N1(C([C@@H](C2CCCCC2)C2=CC(OC)=C(OC)C(OC)=C2)=O)CCCC[C@H]1C(O[C@@H](C1=CC=CC(OCCN2CCOCC2)=C1)CCC1=CC=C(OC)C(OC)=C1)=O
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Cayman Chemical
Product number
24366
Product name
SAfit2
Purity
≥95%
Packaging
500μg
Price
$130
Updated
2024/03/01
Cayman Chemical
Product number
24366
Product name
SAfit2
Purity
≥95%
Packaging
1mg
Price
$243
Updated
2024/03/01
Cayman Chemical
Product number
24366
Product name
SAfit2
Purity
≥95%
Packaging
5mg
Price
$830
Updated
2024/03/01
TRC
Product number
S139585
Product name
SAFit2
Packaging
5mg
Price
$2085
Updated
2021/12/16
ChemScene
Product number
CS-0022959
Product name
SAFit2
Purity
98.59%
Packaging
5mg
Price
$290
Updated
2021/12/16
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SAfit2 Chemical Properties,Usage,Production

Description

SAfit2 is a potent inhibitor of FK506-binding protein 51 (FKBP51; Ki = 6 nM). 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.

Uses

SAFit2 is a highly selective inhibitor of FKBP51. The selective inhibition of FKBP51, using SAFit1(S139583) & SAFit2 , has shown to enhances neurite elongation in neuronal cultures and improves neuroendocrine feedback and stress-coping behavior in mice.

in vivo

It is found that 30 days of SAFit2 administration leads to a reduction in body weight under both control and high-fat diet (HFD) conditions. SAFit2 significantly increases phosphorylated AKT2 and AS160 in EDL muscle and likewise increases expression of GLUT4 at the membrane in soleus muscle[2]. When SAFit2 is applied 1 h before testing, no alterations in anxiety-related behavior are observed. However, SAFit2 treatment induces an anxiolytic phenotype in mice injected 16 h prior testing, which is reflected in a significantly increased open arm time in the elevated plus maze (EPM) (z=-2.183, p<0.05).? SAFit2 treatment leads to a significantly reduced latency to enter the lit compartment (z=-2 to 265, p<0.05), as well as a significantly increased distance traveled (t(20)=-2.371, p<0.05) in the lit compartment[3].

References

[1] STEFFEN GAALI. Selective inhibitors of the FK506-binding protein 51 by induced fit[J]. Nature chemical biology, 2014, 11 1: 33-37. DOI: 10.1038/nchembio.1699
[2] JAKOB HARTMANN. Pharmacological Inhibition of the Psychiatric Risk Factor FKBP51 Has Anxiolytic Properties.[J]. Journal of Neuroscience, 2015, 35 24: 9007-9016. DOI: 10.1523/jneurosci.4024-14.2015

SAfit2 Preparation Products And Raw materials

Raw materials

Preparation Products

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SAfit2 Suppliers

China 29 United States 2 Global 31
ShangHai Caerulum Pharma Discovery Co., Ltd.
Tel
18149758185
Email
sales-cpd@caerulumpharma.com
Country
China
ProdList
3506
Advantage
58
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696，15000506266 15000506266
Fax
+86-21-52996696
Country
China
ProdList
4757
Advantage
55
Shanghai EFE Biological Technology Co., Ltd.
Tel
021-65675885 18964387627
Fax
021-65675885
Email
info@efebio.com
Country
China
ProdList
9803
Advantage
58
Shanghai Han-Xiang Chemical Co., Ltd.
Tel
15971444841
Fax
18327183813
Email
amber@biochempartner.com
Country
China
ProdList
3061
Advantage
58
Fan De(Beijing) Biotechnology Co., Ltd.
Tel
15911056312
Email
liming@bio-fount.com
Country
China
ProdList
9729
Advantage
58
Henan Alpha Chemical Co., Ltd.
Tel
0371-55055611 18137792234
Fax
QQ：3002694073
Email
3002694073@qq.com
Country
China
ProdList
9987
Advantage
58
Jilin Province Woda Biotechnology Co., Ltd.
Tel
13504435624
Email
1927928688@qq.com
Country
China
ProdList
1615
Advantage
58
TargetMol Chemicals Inc.
Tel
+1-781-999-5354; +17819995354
Email
marketing@targetmol.com
Country
United States
ProdList
32435
Advantage
58
ChemeGen(Shanghai) Biotechnology Co.,Ltd.
Tel
18818260767
Fax
QQ 3610331285
Email
sales@chemegen.com
Country
China
ProdList
11218
Advantage
58
Guangzhou Younan Technology Co., Ltd
Tel
020-82000279 18988941452
Fax
QQ：3283937693
Email
YN_research@163.com
Country
China
ProdList
3011
Advantage
58

1643125-33-0, SAfit2Related Search:


  • SAfit2
  • 2-Piperidinecarboxylic acid, 1-[(2S)-2-cyclohexyl-2-(3,4,5-trimethoxyphenyl)acetyl]-, (1R)-3-(3,4-dimethoxyphenyl)-1-[3-[2-(4-morpholinyl)ethoxy]phenyl]propyl ester, (2S)-
  • (R)-3-(3,4-Dimethoxyphenyl)-1-(3-(2-morpholinoethoxy)phenyl)propyl (S)-1-((S)-2-cyclohexyl-2-(3,4,5-trimethoxyphenyl)acetyl)piperidine-2-carboxylate
  • (1R)-3-(3,4-dimethoxyphenyl)-1-{3-[2-(morpholin-4-yl)ethoxy]phenyl}propyl (2S)-1-[(2S)-2-cyclohexyl-2-(3,4,5-trimethoxyphenyl)acetyl]piperidine-2-carboxylate
  • SAFit2, 10 mM in DMSO
  • 1643125-33-0
  • C46H62N2O10