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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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T614319-5mg | 5mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $996.90 | |
T614319-25mg | 25mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $2,986.90 |
Synonyms | compound 10;TAK-828;TAK828F |
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Specifications & Purity | Moligand™ |
Grade | Moligand™ |
Action Type | AGONIST |
Mechanism of action | Agonist of RAR-related orphan receptor-γ |
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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IUPAC Name | 2-[3-[(5R)-5-[(7-fluoro-1,1-dimethyl-2,3-dihydroinden-5-yl)carbamoyl]-2-methoxy-7,8-dihydro-5H-1,6-naphthyridine-6-carbonyl]cyclobutyl]acetic acid |
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INCHI | InChI=1S/C28H32FN3O5/c1-28(2)8-6-16-13-18(14-20(29)24(16)28)30-26(35)25-19-4-5-22(37-3)31-21(19)7-9-32(25)27(36)17-10-15(11-17)12-23(33)34/h4-5,13-15,17,25H,6-12H2,1-3H3,(H,30,35)(H,33,34)/t15-,17+,25-/m1/s1 |
InChi Key | ICMFYVOUDGRBLG-VFHHBZAHSA-N |
Canonical SMILES | COc1ccc2c(n1)CCN([C@H]2C(=O)Nc1cc(F)c2c(c1)CCC2(C)C)C(=O)[C@@H]1C[C@@H](C1)CC(=O)O |
Isomeric SMILES | CC1(CCC2=C1C(=CC(=C2)NC(=O)[C@H]3C4=C(CCN3C(=O)C5CC(C5)CC(=O)O)N=C(C=C4)OC)F)C |
PubChem CID | 118622692 |
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1. Kotake S, Udagawa N, Takahashi N, Matsuzaki K, Itoh K, Ishiyama S, Saito S, Inoue K, Kamatani N, Gillespie MT et al.. (1999) IL-17 in synovial fluids from patients with rheumatoid arthritis is a potent stimulator of osteoclastogenesis.. J Clin Invest, 103 (9): (1345-52). [PMID:10225978] [10.1021/op500134e] |
2. Ivanov II, McKenzie BS, Zhou L, Tadokoro CE, Lepelley A, Lafaille JJ, Cua DJ, Littman DR. (2006) The orphan nuclear receptor RORgammat directs the differentiation program of proinflammatory IL-17+ T helper cells.. Cell, 126 (6): (1121-33). [PMID:16990136] [10.1021/op500134e] |
3. Rovedatti L, Kudo T, Biancheri P, Sarra M, Knowles CH, Rampton DS, Corazza GR, Monteleone G, Di Sabatino A, Macdonald TT. (2009) Differential regulation of interleukin 17 and interferon gamma production in inflammatory bowel disease.. Gut, 58 (12): (1629-36). [PMID:19740775] [10.1021/op500134e] |
4. Nair RP, Duffin KC, Helms C, Ding J, Stuart PE, Goldgar D, Gudjonsson JE, Li Y, Tejasvi T, Feng BJ et al.. (2009) Genome-wide scan reveals association of psoriasis with IL-23 and NF-kappaB pathways.. Nat Genet, 41 (2): (199-204). [PMID:19169254] [10.1021/op500134e] |
5. Kebir H, Ifergan I, Alvarez JI, Bernard M, Poirier J, Arbour N, Duquette P, Prat A. (2009) Preferential recruitment of interferon-gamma-expressing TH17 cells in multiple sclerosis.. Ann Neurol, 66 (3): (390-402). [PMID:19810097] [10.1021/op500134e] |
6. Annunziato F, Cosmi L, Santarlasci V, Maggi L, Liotta F, Mazzinghi B, Parente E, Filì L, Ferri S, Frosali F et al.. (2007) Phenotypic and functional features of human Th17 cells.. J Exp Med, 204 (8): (1849-61). [PMID:17635957] [10.1021/op500134e] |
7. Wilke CM, Bishop K, Fox D, Zou W. (2011) Deciphering the role of Th17 cells in human disease.. Trends Immunol, 32 (12): (603-11). [PMID:21958759] [10.1021/op500134e] |
8. Miossec P, Kolls JK. (2012) Targeting IL-17 and TH17 cells in chronic inflammation.. Nat Rev Drug Discov, 11 (10): (763-76). [PMID:23023676] [10.1021/op500134e] |
9. Campa M, Mansouri B, Warren R, Menter A. (2016) A Review of Biologic Therapies Targeting IL-23 and IL-17 for Use in Moderate-to-Severe Plaque Psoriasis.. Dermatol Ther (Heidelb), 6 (1): (1-12). [PMID:26714681] [10.1021/op500134e] |
10. Beringer A, Noack M, Miossec P. (2016) IL-17 in Chronic Inflammation: From Discovery to Targeting.. Trends Mol Med, 22 (3): (230-241). [PMID:26837266] [10.1021/op500134e] |
11. Shibata A, Uga K, Sato T, Sagara M, Igaki K, Nakamura Y, Ochida A, Kono M, Shirai J, Yamamoto S et al.. (2018) Pharmacological inhibitory profile of TAK-828F, a potent and selective orally available RORγt inverse agonist.. Biochem Pharmacol, 150 (13): (35-45). [PMID:29369782] [10.1021/op500134e] |
12. Kono M, Ochida A, Oda T, Imada T, Banno Y, Taya N, Masada S, Kawamoto T, Yonemori K, Nara Y et al.. (2018) Discovery of [ cis-3-({(5 R)-5-[(7-Fluoro-1,1-dimethyl-2,3-dihydro-1 H-inden-5-yl)carbamoyl]-2-methoxy-7,8-dihydro-1,6-naphthyridin-6(5 H)-yl}carbonyl)cyclobutyl]acetic Acid (TAK-828F) as a Potent, Selective, and Orally Available Novel Retinoic Acid Receptor-Related Orphan Receptor γt Inverse Agonist.. J Med Chem, 61 (7): (2973-2988). [PMID:29510038] [10.1021/op500134e] |