SR1001|SR-1001,SR 1001|DC Chemicals

Cas No.:	1335106-03-0
Chemical Name:	SR1001,N-{4-Methyl-5-[4-(2,2,2-trifluoro-1-hydroxy-1-trifluoroMethyl-ethyl)-phenylsulfaMoyl]-thiazol-2-yl}-acetaMide
Synonyms:	SR-1001,SR 1001
SMILES:	CC(NC1=NC(C)=C(S(=O)(NC2=CC=C(C(C(F)(F)F)(O)C(F)(F)F)C=C2)=O)S1)=O
Formula:	C₁₅H₁₃F₆N₃O₄S₂
M.Wt:	477.4
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

SR1001 is a high-affinity synthetic ligand of RORα and RORγ; suppresses TH17 cell differentiation and inhibits autoimmunity. in vitro: SR1001 binds specifically to the ligand-binding domains of RORα and RORγt, inducing a conformational change within the ligand-binding domain that encompasses the repositioning of helix 12 and leads to diminished affinity for co-activators and increased affinity for co-repressors, resulting in suppression of the receptors' transcriptional activity. SR1001 inhibited the development of murine T(H)17 cells, as demonstrated by inhibition of interleukin-17A gene expression and protein production. Furthermore, SR1001 inhibited the expression of cytokines when added to differentiated murine or human T(H)17 cells. SR1001 reduced the interaction of a coactivator TRAP220 NR box 2 peptide with RORγ in a dose dependent manner(IC50=117 nM). in vivo: SR1001 was a RORα inverse agonist eliminated the circadian pattern of expression of CS mRNA in mice. For the detailed information of SR1001, the solubility of SR1001 in water, the solubility of SR1001 in DMSO, the solubility of SR1001 in PBS buffer, the animal experiment (test) of SR1001, the cell expriment (test) of SR1001, the in vivo, in vitro and clinical trial test of SR1001, the EC50, IC50,and affinity,of SR1001, For the detailed information of SR1001, the solubility of SR1001 in water, the solubility of SR1001 in DMSO, the solubility of SR1001 in PBS buffer, the animal experiment (test) of SR1001, the cell expriment (test) of SR1001, the in vivo, in vitro and clinical trial test of SR1001, the EC50, IC50,and affinity,of SR1001, Please contact DC Chemicals.

MSDS

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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.
DC44172	RORγt inverse agonist 13	RORγt inverse agonist 13 (Compound 3i) is a potent, orally active and selective RORγt inverse agonist, with improved drug-like properties, with an IC50 of 63.8 nM.
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.