SAFit2

SAFit2
Legal status
Legal status	US: Investigational drug;
Identifiers
	IUPAC 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;
CAS Number	1643125-33-0;
PubChem CID	86277887;
ChemSpider	32779480;
ChEMBL	ChEMBL3623630;
Chemical and physical data
Formula	C46H62N2O10
Molar mass	803.006 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES COC1=C(C=C(C=C1)CC[C@H](C2=CC(=CC=C2)OCCN3CCOCC3)OC(=O)[C@@H]4CCCCN4C(=O)[C@@H](C5CCCCC5)C6=CC(=C(C(=C6)OC)OC)OC)OC;
	InChI 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; Key:ZDBWLRLGUBSLPG-FDHYQTMZSA-N;

SAFit2 is a drug which acts as a potent and selective inhibitor of the signalling factor FK506 binding protein 51 (FKBP51), which is involved in the downstream response to glucocorticoid release in the body.^[1] Since elevated glucocorticoid levels are a characteristic marker of chronic stress, blocking glucocorticoid signalling pathways using SAFit2 has been shown to counteract many of the associated symptoms such as obesity,^[2]^[3] chronic pain,^[4]^[5] depression and anxiety,^[6]^[7] and addiction.^[8]^[9] While SAFit2 itself is a relatively large molecule and is unlikely to have suitable properties to be developed for medical use, it has demonstrated that inhibition of FKBP51 may be a useful therapeutic approach for alleviating consequences of long-term chronic stress and pain.