[CAS NO. 1335106-03-0] SR1001

Name: SR1001
Brand: Arctom Scientific
SKU: SLK-S6724

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PRODUCTS SPECIFICATIONS [1335106-03-0]

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Catalog

SLK-S6724

Brand

Selleck

CAS

1335106-03-0

DESCRIPTION [1335106-03-0]

Overview

MDL	MFCD23160036
Molecular Weight	477.40
Molecular Formula	C15H13F6N3O4S2
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

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.0947 mL	10.4734 mL	20.9468 mL
5 mM	0.4189 mL	2.0947 mL	4.1894 mL
10 mM	0.2095 mL	1.0473 mL	2.0947 mL
50 mM	0.0419 mL	0.2095 mL	0.4189 mL

Description

SR1001 is a inverse agonist with Ki values of 172 nM and 111 nM for RORα and RORγ respectively.

Targets

RORγ ^[2]	RORα ^[2]
111 nM(Ki)	172 nM(Ki)

In vitro

SR1001 binds specifically to the ligand binding domains (LBDs) of RORα and RORγt inducing a conformational change within the LBD that encompasses repositioning of helix 12 leading to diminished affinity for coactivators and increased affinity for corepressors resulting in suppression of the receptors transcriptional activity.

References

[1] Laura A. Solt, et al. Endocrinology. 2015, 156(3): 869-881.
[2] Laura A. Solt, et al. Nature. 2011, 472(7344): 491-494.
[3] Sun Y, et al. Proc Natl Acad Sci U S A. 2015, 112(33):10401-6.