INT-767 , CAS No.I611121, Agonist of Farnesoid X receptor;Agonist of GPBA receptor

Item Number
I611121
Grouped product items
SKUSizeAvailabilityPrice Qty
I611121-5mg
5mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$572.90
I611121-25mg
25mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$2,000.90

Basic Description

SynonymsINT767
Specifications & PurityMoligand™
GradeMoligand™
Action TypeAGONIST
Mechanism of actionAgonist of Farnesoid X receptor;Agonist of GPBA receptor

Associated Targets(Human)

NR1H4 Tclin Bile acid receptor (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
GPBAR1 Tchem G-protein coupled bile acid receptor 1 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Associated Targets(non-human)

Hdac6 Histone deacetylase 6 (222 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

INCHI InChI=1S/C25H44O6S/c1-5-17-21-14-16(26)8-11-25(21,4)20-9-12-24(3)18(6-7-19(24)22(20)23(17)27)15(2)10-13-31-32(28,29)30/h15-23,26-27H,5-14H2,1-4H3,(H,28,29,30)/p-1/t15-,16-,17-,18-,19+,20+,21+,22+,23-,24-,25-/m1/s1
InChi Key XGIYOABXZNJOHV-APIYUPOTSA-M
Canonical SMILES CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)CC[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)[C@@H](CCOS(=O)(=O)[O-])C
Isomeric SMILES CC[C@@H]1[C@@H]2C[C@@H](CC[C@@]2([C@H]3CC[C@]4([C@H]([C@@H]3[C@@H]1O)CC[C@@H]4[C@H](C)CCOS(=O)(=O)O)C)C)O
PubChem CID 23642339

Certificates

Certificate of Analysis(COA)

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Related Documents

References

1. Rizzo G, Passeri D, De Franco F, Ciaccioli G, Donadio L, Rizzo G, Orlandi S, Sadeghpour B, Wang XX, Jiang T et al..  (2010)  Functional characterization of the semisynthetic bile acid derivative INT-767, a dual farnesoid X receptor and TGR5 agonist..  Mol Pharmacol,  78  (4): (617-30).  [PMID:20631053] [10.1021/op500134e]
2. Wang XX, Luo Y, Wang D, Adorini L, Pruzanski M, Dobrinskikh E, Levi M.  (2017)  A dual agonist of farnesoid X receptor (FXR) and the G protein-coupled receptor TGR5, INT-767, reverses age-related kidney disease in mice..  J Biol Chem,  292  (29): (12018-12024).  [PMID:28596381] [10.1021/op500134e]
3. Wang XX, Wang D, Luo Y, Myakala K, Dobrinskikh E, Rosenberg AZ, Levi J, Kopp JB, Field A, Hill A et al..  (2018)  FXR/TGR5 Dual Agonist Prevents Progression of Nephropathy in Diabetes and Obesity..  J Am Soc Nephrol,  29  (1): (118-137).  [PMID:29089371] [10.1021/op500134e]
4. Comeglio P, Cellai I, Mello T, Filippi S, Maneschi E, Corcetto F, Corno C, Sarchielli E, Morelli A, Rapizzi E et al..  (2018)  INT-767 prevents NASH and promotes visceral fat brown adipogenesis and mitochondrial function..  J Endocrinol,  238  (2): (107-127).  [PMID:29945982] [10.1021/op500134e]
5. Hu YB, Liu XY, Zhan W.  (2018)  Farnesoid X receptor agonist INT-767 attenuates liver steatosis and inflammation in rat model of nonalcoholic steatohepatitis..  Drug Des Devel Ther,  12  (13): (2213-2221).  [PMID:30038487] [10.1021/op500134e]
6. Iracheta-Vellve A, Calenda CD, Petrasek J, Ambade A, Kodys K, Adorini L, Szabo G.  (2018)  FXR and TGR5 Agonists Ameliorate Liver Injury, Steatosis, and Inflammation After Binge or Prolonged Alcohol Feeding in Mice..  Hepatol Commun,  (11): (1379-1391).  [PMID:30411084] [10.1021/op500134e]

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