GNE-6468|GNE6468

Cas No.:	1677668-27-7
Chemical Name:	4-(6-(2-chloro-6-cyclopropylbenzoyl)imidazo[1,5-a]pyrimidin-8-yl)-2-hydroxybenzoic acid
Synonyms:	GNE6468
SMILES:	C(O)(=O)C1=CC=C(C2=C3N(C(C(=O)C4=C(C5CC5)C=CC=C4Cl)=N2)C=CC=N3)C=C1O
Formula:	C₂₃H₁₆ClN₃O₄
M.Wt:	433.85
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

GNE-6468 (GNE6468) is a potent and selective RORc inverse agonist (EC50=2 nM) with >1,000-fold selectivity for RORc over PPARγ; displays excellent selectivity profiles against a panel of other nuclear receptors in Gal4 human transcription assays; displays potent inhibition of IL-17 production with EC50 of 30 nM in human PBMC cytokine production assays, without effect on IFNγ production; GNE-6468 is a chemical biology tool to further explore the role of RORc in human biology.

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101

Cat. No.	Product name	Field of application
DC47346	RORγ agonist 1	RORγ agonist 1 is a potent and orally bioavailable RORγ agonist (EC50 = 21 nM) with antitumor activity.
DC47345	RORγt inverse agonist 23	RORγt inverse agonist 23 is a potent, selective, and orally available novel retinoic acid receptor-related orphan receptor γt inverse agonist.
DC40046	Vimirogant hydrochloride	Vimirogant (VTP-43742) hydrochloride is a potent, selective, and orally active RORγt inhibitor (Ki=3.5 nM; IC50=17 nM). Vimirogant hydrochloride exhibits >1000-fold selectivity versus the RORα and RORβ isotypes. Vimirogant hydrochloride inhibits Th17 differentiation and IL-17A secretion from mouse splenocytes (IC50=57 nM) without affecting Th1, Th2, or Treg cell differentiation. Vimirogant hydrochloride has the potential for autoimmune disorders research.
DC28379	TMP920	TMP920 is a highly potent and selective RORγt antagonist. TMP920 inhibits RORγt binding to the SRC1 peptide with an IC50 of 0.03 μM.
DC28137	TMP780	TMP780 is an inverse agonist of RORγt with an IC50 of 13 nM. RORγt is a tractable drug target for the treatment of cutaneous inflammatory disorders.
DC11046	SR2211	SR2211 (SR-2211) is a potent, selective RORγ inverse agonist (Ki=105 nM, IC50=320 nM) that potently inhibits production of IL-17 in cells.
DC8096	SR1001	SR1001 is a high-affinity synthetic ligand of RORα and RORγ; suppresses TH17 cell differentiation and inhibits autoimmunity.
DC11202	RORγt inverse agonist 32	RORγt inverse agonist 32 is a potent, orally bioavailable inverse agonist of RORγt with IC50 of 9 nM in SPA binding assays.
DC11054	RORγt inverse agonist 22	RORγt inverse agonist 22 is a potent, subtype selective RORγt inverse agonist with binding IC50 of 18 nM, displays >192-fold selectivity over RORα and RORβ.
DC11224	PF-06747711	PF-06747711 (PF06747711) is a potent, selective, orally bioavailable RORC2 (RORγt) inverse agonist with IC50 of 4.1 nM.