ROR-Antagonists-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/ROR.html RORRAR-related orphan receptorRetinoic acid receptor-related orphan receptors (RORs) are a subfamily of the thyroid hormone receptor, which is a subfamily of thenuclear receptors and belonging to the orphan nuclear receptor family. The ROR subfamily co

2、ntains three members: ROR (NR1F1),ROR (NR1F2), and ROR (NR1F3) and function as ligand-dependent transcription factors.RORs are reported to activate transcription through ligand-dependent interactions with co-regulators and are involved in thedevelopment of secondary lymphoid tissues, autoimmune dise

3、ases, inflammatory diseases, the circadian rhythm, and metabolismhomeostasis.ROR and ROR are important regulators of the immune system. The development and differentiation of Th17cells are dependenton these factors. ROR is expressed in lymphoid tissue inducer cells, innate lymphoid cells, invariant

4、natural killer T cells, and Tcells, which contribute to inflammation and autoimmune disease.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/ROR.html ROR HYPERLINK https:/www.MedChemE/Targets/ROR.html HYPERLINK https:/www.MedChemE/Targets/ROR.html Inhibitors, HYPERLINK https:/www.MedChemE/Target

5、s/ROR.html HYPERLINK https:/www.MedChemE/Targets/ROR.html Agonists, HYPERLINK https:/www.MedChemE/Targets/ROR.html HYPERLINK https:/www.MedChemE/Targets/ROR.html Antagonists HYPERLINK https:/www.MedChemE/Targets/ROR.html HYPERLINK https:/www.MedChemE/Targets/ROR.html & HYPERLINK https:/www.MedChemE/

6、Targets/ROR.html HYPERLINK https:/www.MedChemE/Targets/ROR.html Modulators HYPERLINK https:/www.MedChemE/racemic-ml-209.html ()-ML HYPERLINK https:/www.MedChemE/racemic-ml-209.html HYPERLINK https:/www.MedChemE/racemic-ml-209.html 209Cat. No.: HY-126037 HYPERLINK https:/www.MedChemE/3-oxo-5-cholanoi

7、c-acid.html 3-Oxo-5-cholanoic HYPERLINK https:/www.MedChemE/3-oxo-5-cholanoic-acid.html HYPERLINK https:/www.MedChemE/3-oxo-5-cholanoic-acid.html acid(Dehydrolithocholic acid; 3-oxoLCA) Cat. No.: HY-125801()-ML 209 (compound 4n), a diphenylpropanamide,is a retinoic acid-related orphan receptor RORan

8、tagonist with an IC of 1.1 M. ()-ML 20950inhibits RORt transcriptional activity with anIC of 300 nM in HEK293t cells.503-Oxo-5-cholanoic acid (Dehydrolithocholic acid),a bile acid metabolite, inhibits thediferentiation of TH17 cells by directly bindingto the key transcription factor RORt (K =1.13dM)

9、.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/a-9758.html A-9758 HYPERLINK https:/www.MedChemE/a-9758.html HYPERLINK https:/www.MedChemE/arn-6039.html ARN-6039C

10、at. No.: HY-126252 Cat. No.: HY-115777A-9758 is a ROR ligand and a potent, selectiveRORt inverse agonist (IC =5 nM), and exhibits50robust potency against IL-17A release. A-9758 iseffective in suppressing both Th17 differentiationand Th17 effector function.ARN-6039 is an orally available inverse agon

11、ist ofROR for autoimmune demyelinating disease.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/AZD-0284.html AZD-0284 HYPERLINK https:/www.MedChemE/AZD-0284.html HYPERLINK

12、 https:/www.MedChemE/bevurogant.html BevurogantCat. No.: HY-120384 Cat. No.: HY-132810AZD-0284 is a selective inverse agonist of thenuclear receptor ROR. AZD-0284 has the potentialfor plaque psoriasis vulgaris and respiratorytract disorders treatment.Bevurogant is a retinoid-related orphanreceptor-g

13、amma t (RORt) antagonist. Bevurogantcan be used for the research of chronicinflammatory diseases.Purity: 99.90%Clinical Data: Phase 1Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98.57%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/b

14、ms-986251.html BMS-986251 HYPERLINK https:/www.MedChemE/bms-986251.html HYPERLINK https:/www.MedChemE/cedirogant.html CedirogantCat. No.: HY-136527(ABBV-157) Cat. No.: HY-137434BMS-986251 is an orally active and selectiveRORt inverse agonist with an EC of 12 nM for50RORt GAL4. BMS-986251 inhibits IL

15、-17 with anEC of 24 nM in human whole blood assay.50Cedirogant (ABBV-157) is an orally active RORtinverse agonist. Cedirogant can be used forpsoriasis research.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.41%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 m

16、g, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/LYC-55716.html Cintirorgon HYPERLINK https:/www.MedChemE/LYC-55716.html HYPERLINK https:/www.MedChemE/fm26.html FM26(LYC-55716) Cat. No.: HY-104037Cat. No.: HY-133128Cintirorgon (LYC-55716) is a first-in-class,selective and orally bioavailable ROR agoni

17、st.FM26 (compound 25) is a potent and allostericretinoic acid receptor-related orphan receptor t(RORt) inverse agonists with an IC of 264 nM.50FM26 has a distinct isoxazole chemotype andeffectively reduces IL-17a mRNA production in EL4cells.Purity: 99.95%Clinical Data: Phase 2Size: 10 mM 1 mL, 1 mg,

18、 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/GNE-0946.html GNE-0946 HYPERLINK https:/www.MedChemE/GNE-0946.html HYPERLINK https:/www.MedChemE/GNE-6468.html GNE-6468

19、Cat. No.: HY-19774 Cat. No.: HY-19775GNE-0946 is a potent and selective ROR( RORc)agonist with an EC value of 4 nM for HEK-29350cell.GNE-6468 is a highly potent and selective ROR(RORc) inverse agonist with an EC value of 1350nM for HEK-293 cell. GNE-6468 exhibits an EC50of 30 nM for IL-17 PBMC.Purit

20、y: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.50%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg, 250 mg HYPERLINK https:/www.MedChemE/ROR-gama-modulator-1.html GSK2981278 HYPERLINK https:/www.MedChemE/ROR-gama-modulator-1.html HYPERLINK ht

21、tps:/www.MedChemE/ROR-gamma-t-IN-1.html GSK805Cat. No.: HY-19770 Cat. No.: HY-12776GSK2981278 is a potent and selective ROR inverseagonist. GSK2981278 inhibits activation of the il17promoter and interferes ROR-DNA binding.GSK805 is a potent, orally bioavailable, and CNSpenetrant RORt inhibitor with

22、pIC of 8.4 and508.2 for ROR FRET assay and Th17 assay.Purity: 99.69%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98.26%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/L_601920-0

23、.html Methyl-3-hydroxycholenate HYPERLINK https:/www.MedChemE/L_601920-0.html HYPERLINK https:/www.MedChemE/neoruscogenin.html NeoruscogeninCat. No.: HY-100084 Cat. No.: HY-N2253Methyl-3-hydroxycholenate is a ROR gammamodulator extracted from patent US20110263046 A1,in figure 2.Neoruscogenin, a memb

24、er of the steroidal sapogeninfamily, is a bioavailable, potent, andhigh-affinity agonist of the nuclear receptorROR (NR1F1).Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.15%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 20 mg HYPERLINK https:/www.MedChemE/Nobi

25、letin.html Nobiletin HYPERLINK https:/www.MedChemE/Nobiletin.html HYPERLINK https:/www.MedChemE/PF-06747711.html PF-06747711Cat. No.: HY-N0155 Cat. No.: HY-112706Nobiletin is a poly-methoxylated flavone from thecitrus peel that improves memory loss. Nobiletinis a retinoid acid receptor-related orpha

26、nreceptors (RORs) agonist.PF-06747711 is a potent, selective, and orallyactive retinoic acid receptor-related orphan C2(RORC2, also known as RORt) inverse agonist,with an IC of 4.1 nM. Anti-skin inflammatory50activity.Purity: 99.52%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg,

27、 50 mg, 100 mgPurity: 99.86%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg HYPERLINK https:/www.MedChemE/retezorogant.html Retezorogant HYPERLINK https:/www.MedChemE/retezorogant.html HYPERLINK https:/www.MedChemE/ror-agonist-1.html ROR HYPERLINK https:/www.MedChemE/ror-agonist-1.html

28、HYPERLINK https:/www.MedChemE/ror-agonist-1.html agonist-1Cat. No.: HY-145590 Cat. No.: HY-128353Retezorogant is a retinoid-related orphan receptor (ROR) antagonist, extracted from patentWO2016093342 A1.ROR agonist-1 is a potent and orally bioavailableinverse agonist of the retinoic acidreceptor-rel

29、ated orphan receptor C2 (RORC2),inhibition of IL-17A production from human primaryT 17 cells with a p of 7.5.H IC50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/ror-agonis

30、t-1.html ROR HYPERLINK https:/www.MedChemE/ror-agonist-1.html HYPERLINK https:/www.MedChemE/ror-agonist-1.html agonist HYPERLINK https:/www.MedChemE/ror-agonist-1.html HYPERLINK https:/www.MedChemE/ror-agonist-1.html 1 HYPERLINK https:/www.MedChemE/ror-agonist-1.html HYPERLINK https:/www.MedChemE/ro

31、r-gamma-t-agonist-1.html RORt HYPERLINK https:/www.MedChemE/ror-gamma-t-agonist-1.html HYPERLINK https:/www.MedChemE/ror-gamma-t-agonist-1.html agonist HYPERLINK https:/www.MedChemE/ror-gamma-t-agonist-1.html HYPERLINK https:/www.MedChemE/ror-gamma-t-agonist-1.html 1Cat. No.: HY-132900 Cat. No.: HY-

32、126321ROR agonist 1 is a potent and orally bioavailableROR agonist (EC = 21 nM) with antitumor50activity.RORt agonist 1 (compound 14) is a potent, orallybioavailable RORt agonist with an EC of5020.8nM. RORt agonist 1 showes high metabolicstability, improved aqueous solubility andexcellent mouse PK p

33、rofile.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/rort-agonist-2.html RORt HYPERLINK https:/www.MedChemE/rort-agonist-2.html HYPERLINK https:/www.MedChemE/rort-agonist-2.html agonist

34、 HYPERLINK https:/www.MedChemE/rort-agonist-2.html HYPERLINK https:/www.MedChemE/rort-agonist-2.html 2 HYPERLINK https:/www.MedChemE/rort-agonist-2.html HYPERLINK https:/www.MedChemE/rort-agonist-3.html RORt HYPERLINK https:/www.MedChemE/rort-agonist-3.html HYPERLINK https:/www.MedChemE/rort-agonist

35、-3.html agonist HYPERLINK https:/www.MedChemE/rort-agonist-3.html HYPERLINK https:/www.MedChemE/rort-agonist-3.html 3Cat. No.: HY-142937 Cat. No.: HY-142938RORt agonist 2 is a potent agonist of RORt.RORt agonist 2 promotes the differentiation ofTh17 cells and enhances the levels ofpro-inflammatory c

36、ytokines, thereby increasing thecytotoxicity of lymphocytes.RORt agonist 3 is a potent agonist of RORt.RORt agonist 3 promotes the differentiation ofTh17 cells and enhances the levels ofpro-inflammatory cytokines, thereby increasing thecytotoxicity of lymphocytes.Purity: 98%Clinical Data: No Develop

37、ment ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/rort-inhibitor-1.html RORt HYPERLINK https:/www.MedChemE/rort-inhibitor-1.html HYPERLINK https:/www.MedChemE/rort-inhibitor-1.html inhibitor HYPERLINK https:/www.MedChemE/rort

38、-inhibitor-1.html HYPERLINK https:/www.MedChemE/rort-inhibitor-1.html 1 HYPERLINK https:/www.MedChemE/rort-inhibitor-1.html HYPERLINK https:/www.MedChemE/rort-inverse-agonist-10.html RORt HYPERLINK https:/www.MedChemE/rort-inverse-agonist-10.html HYPERLINK https:/www.MedChemE/rort-inverse-agonist-10

39、.html Inverse HYPERLINK https:/www.MedChemE/rort-inverse-agonist-10.html HYPERLINK https:/www.MedChemE/rort-inverse-agonist-10.html agonist HYPERLINK https:/www.MedChemE/rort-inverse-agonist-10.html HYPERLINK https:/www.MedChemE/rort-inverse-agonist-10.html 10Cat. No.: HY-142296 Cat. No.: HY-133552R

40、ORt inhibitor 1 is a RORt allosteric inhibitorwith an IC value of 1 nM.50RORt Inverse agonist 10 is a potent and orallybioavailable RORt (retinoic acidreceptor-related orphan nuclear receptor gamma t)inverse agonist, with an IC of 51 nM.50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg,

41、5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/rort-inverse-agonist-13.html RORt HYPERLINK https:/www.MedChemE/rort-inverse-agonist-13.html HYPERLINK https:/www.MedChemE/rort-inverse-agonist-13.html inverse HYPERLINK https:/www.MedChemE/rort-inver

42、se-agonist-13.html HYPERLINK https:/www.MedChemE/rort-inverse-agonist-13.html agonist HYPERLINK https:/www.MedChemE/rort-inverse-agonist-13.html HYPERLINK https:/www.MedChemE/rort-inverse-agonist-13.html 13 HYPERLINK https:/www.MedChemE/rort-inverse-agonist-13.html HYPERLINK https:/www.MedChemE/rort

43、-inverse-agonist-14.html RORt HYPERLINK https:/www.MedChemE/rort-inverse-agonist-14.html HYPERLINK https:/www.MedChemE/rort-inverse-agonist-14.html inverse HYPERLINK https:/www.MedChemE/rort-inverse-agonist-14.html HYPERLINK https:/www.MedChemE/rort-inverse-agonist-14.html agonist HYPERLINK https:/w

44、ww.MedChemE/rort-inverse-agonist-14.html HYPERLINK https:/www.MedChemE/rort-inverse-agonist-14.html 14Cat. No.: HY-131338 Cat. No.: HY-132195RORt inverse agonist 13 (Compound 3i) is apotent, orally active and selective RORt inverseagonist, with improved drug-like properties, withan IC of 63.8 nM.50R

45、ORt inverse agonist 14 (8e) is a potent, orallyactive and selective RORt inverse agonist (EC50of 2.5 nM) with anti-inflammatory activity. RORtinverse agonist 14 is used in the study forrheumatoid arthritis and psoriasis.Purity: 99.22%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 m

46、g, 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/ROR_gamma_t_Inverse_agonist_2.html RORt HYPERLINK https:/www.MedChemE/ROR_gamma_t_Inverse_agonist_2.html HYPERLINK https:/www.MedChemE/ROR_gamma_t_Inverse_agonist_2.html Inverse HYP

47、ERLINK https:/www.MedChemE/ROR_gamma_t_Inverse_agonist_2.html HYPERLINK https:/www.MedChemE/ROR_gamma_t_Inverse_agonist_2.html agonist HYPERLINK https:/www.MedChemE/ROR_gamma_t_Inverse_agonist_2.html HYPERLINK https:/www.MedChemE/ROR_gamma_t_Inverse_agonist_2.html 2 HYPERLINK https:/www.MedChemE/ROR

48、_gamma_t_Inverse_agonist_2.html HYPERLINK https:/www.MedChemE/rort-inverse-agonist-23.html RORt HYPERLINK https:/www.MedChemE/rort-inverse-agonist-23.html HYPERLINK https:/www.MedChemE/rort-inverse-agonist-23.html inverse HYPERLINK https:/www.MedChemE/rort-inverse-agonist-23.html HYPERLINK https:/ww

49、w.MedChemE/rort-inverse-agonist-23.html agonist HYPERLINK https:/www.MedChemE/rort-inverse-agonist-23.html HYPERLINK https:/www.MedChemE/rort-inverse-agonist-23.html 23Cat. No.: HY-111748 Cat. No.: HY-139847RORt Inverse agonist 2 is a selective, orallyactive RORt inverse agonist with an EC of50119 n

50、M.RORt inverse agonist 23 is a potent, selective,and orally available novel retinoic acidreceptor-related orphan receptor t inverseagonist.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg4 Tel: 609-228-6898 Fax: 609-22

51、8-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/rort-inverse-agonist-26.html RORt HYPERLINK https:/www.MedChemE/rort-inverse-agonist-26.html HYPERLINK https:/www.MedChemE/rort-inverse-agonist-26.html inverse HYPERLINK https:/www.MedChemE/rort-inverse-agonist-26.html HYPERLINK https:/www.Me

52、dChemE/rort-inverse-agonist-26.html agonist HYPERLINK https:/www.MedChemE/rort-inverse-agonist-26.html HYPERLINK https:/www.MedChemE/rort-inverse-agonist-26.html 26 HYPERLINK https:/www.MedChemE/rort-inverse-agonist-26.html HYPERLINK https:/www.MedChemE/rort-inverse-agonist-28.html RORt HYPERLINK ht

53、tps:/www.MedChemE/rort-inverse-agonist-28.html HYPERLINK https:/www.MedChemE/rort-inverse-agonist-28.html inverse HYPERLINK https:/www.MedChemE/rort-inverse-agonist-28.html HYPERLINK https:/www.MedChemE/rort-inverse-agonist-28.html agonist HYPERLINK https:/www.MedChemE/rort-inverse-agonist-28.html H

54、YPERLINK https:/www.MedChemE/rort-inverse-agonist-28.html 28Cat. No.: HY-142806 Cat. No.: HY-142703RORt inverse agonist 26 is a potent reverseagonist of RORt. RORt inverse agonist 26regulates the differentiation of Th17 cells andinhibits the production of IL-17.RORt inverse agonist 28 is a potent re

55、verseagonist of RORt. RORt inverse agonist 28regulates the differentiation of Th17 cells andinhibits the production of IL-17.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/ror-gamma-t-in

56、verse-agonist-3.html RORt HYPERLINK https:/www.MedChemE/ror-gamma-t-inverse-agonist-3.html HYPERLINK https:/www.MedChemE/ror-gamma-t-inverse-agonist-3.html Inverse HYPERLINK https:/www.MedChemE/ror-gamma-t-inverse-agonist-3.html HYPERLINK https:/www.MedChemE/ror-gamma-t-inverse-agonist-3.html agonis

57、t HYPERLINK https:/www.MedChemE/ror-gamma-t-inverse-agonist-3.html HYPERLINK https:/www.MedChemE/ror-gamma-t-inverse-agonist-3.html 3 HYPERLINK https:/www.MedChemE/ror-gamma-t-inverse-agonist-3.html HYPERLINK https:/www.MedChemE/ror-gamma-t-inverse-agonist-6.html RORt HYPERLINK https:/www.MedChemE/r

58、or-gamma-t-inverse-agonist-6.html HYPERLINK https:/www.MedChemE/ror-gamma-t-inverse-agonist-6.html Inverse HYPERLINK https:/www.MedChemE/ror-gamma-t-inverse-agonist-6.html HYPERLINK https:/www.MedChemE/ror-gamma-t-inverse-agonist-6.html agonist HYPERLINK https:/www.MedChemE/ror-gamma-t-inverse-agoni

59、st-6.html HYPERLINK https:/www.MedChemE/ror-gamma-t-inverse-agonist-6.html 6Cat. No.: HY-128573 Cat. No.: HY-130243RORt Inverse agonist 3 is a potent, selective andorally active ROR inverse agonist, with EC s50of 0.22 M and 0.15 M for hROR and RORt (humanIL-17 cells), respectively.RORt Inverse agoni

60、st 6 (compound 43) is a RORtinverse agonist for the study of Th17-drivenautoimmune diseases. RORt Inverse agonist 6(compound 43) suppresses IL-17A gene expression byIL-23 stimulation in vivo.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.97%Clinical Data: No Development