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SR 1555 (hydrochloride) (CAS 0) LS-H84

ROR gamma agonist
LS-H84-1 / 1 mg / $175
LS-H84-5 / 5 mg / $225
LS-H84-10 / 10 mg / $265
LS-H84-25 / 25 mg / $395
USA Shipment Only
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Description: Retinoic acid receptor-related nuclear receptor gamma (ROR gamma) plays a central role in T cell differentiation, particularly in the development of TH17 cells, which are implicated in autoimmune diseases like multiple sclerosis and rheumatoid arthritis. SR 1555 is a selective ligand of ROR gamma (IC50 = 1 µM). It does not bind ROR alpha, LXR, or FXR. SR 1555 acts as an inverse agonist of ROR gamma, inhibiting endogenous IL-17A gene expression in mouse splenocytes and suppressing differentiation of TH17 cells when cultured under TH17 polarizing conditions. Moreover, SR 1555 stimulates T regulatory development when cultured under T regulatory polarizing conditions, unlike digoxin and ursolic acid. H84_ChemicalStructureImage.png
1-(4-((4'-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-[1,1'-biphenyl]-4-yl)methyl)piperazin-1-yl)ethanone, monohydrochloride
 
biochemical, chemical, agonist
LS-H84
0
C22H22F6N2O2 • HCl
≥98%
A crystalline solid
 
O=C(C)N(CC1)CCN1CC2=CC=C(C3=CC=C(C(O)(C(F)(F)F)C(F)(F)F)C=C3)C=C2.Cl
InChI=1S/C22H22F6N2O2.ClH/c1-15(31)30-12-10-29(11-13-30)14-16-2-4-17(5-3-16)18-6-8-19(9-7-18)20(32,21(23,24)25)22(26,27)28;/h2-9,32H,10-14H2,1H3;1H
OHUOFZJUUXXRGG-UHFFFAOYSA-N
Shipped Ambient, store at -20°C, ≥ 2 years shelf life.
This product is for research use only. Not for administration to humans, or for human or veterinary diagnostic or therapeutic use.
Data Sheet DataSheet    SDS SDS
Related Products: RORC / ROR Gamma related products

Usage Information

SR 1555 (hydrochloride) is supplied as a crystalline solid. A stock solution may be made by dissolving the SR 1555 (hydrochloride) in the solvent of choice. SR 1555 (hydrochloride) is soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide (DMF), which should be purged with an inert gas. The solubility of SR 1555 (hydrochloride) in these solvents is approximately 1.6, 3, and 5 mg/ml, respectively. SR 1555 (hydrochloride) is sparingly soluble in aqueous buffers. For maximum solubility in aqueous buffers, SR 1555 (hydrochloride) should first be dissolved in DMF and then diluted with the aqueous buffer of choice. SR 1555 (hydrochloride) has a solubility of approximately 0.16 mg/ml in a 1:6 solution of DMF:PBS (pH 7.2) using this method. We do not recommend storing the aqueous solution for more than one day.

References:
  1. Ivanov, I.I., McKenzie, B.S., Zhou, L., et al. The orphan nuclear receptor RORgt directs the differentiation program of proinflammatory IL-17+ T helper cells. Cell 126, 1121-1133 (2006).
  2. Solt, L.A., Kumar, N., Nuhant, P., et al. Suppression of TH17 differentiation and autoimmunity by a synthetic ROR ligand. Nat. Lett. 472(7344), 491-4 (2011).
  3. Solt, L.A., Kumar, N., He, Y., et al. Identification of a selective RORg ligand that suppresses TH17 cells and stimulates T regulatory cells. ACS Chem. Biol. 7, 1515-1519 (2012).

 


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