MedKoo Biosciences, Inc.
Tel:   +1-919-636-5577    Fax:   +1-919-980-4831    Email:   sales@medkoo.com
Search
Login Register
Search
MedKoo Cat#: 574023 | Name: SR1903 free base
Featured

Description:

WARNING: This product is for research use only, not for human or veterinary use.

SR-1903 is a modulator of retinoic acid receptor-related orphan receptor γ (RORγ) and liver X receptor (LXR). It is an inverse agonist of RORγ and an agonist of LXR. It also binds to peroxisome proliferator-activated receptor γ (PPAR) but does not activate it. SR-1903 inhibits LPS-induced expression of triggering receptor expressed on myeloid cells 1 (TREM-1). It also inhibits LPS-induced expression of the LXR target genes IL-6 and IL-33 and increases expression of ABCG1, FASN, and SCD-1. SR-1903 reduces the severity of collagen-induced arthritis. It reduces blood glucose levels in a glucose tolerance test, serum levels of total cholesterol and LDL, body weight, and fat mass in a mouse model of high-fat diet-induced obesity.

Chemical Structure

SR1903 free base
CAS#1414248-06-8 (free base)

Theoretical Analysis

MedKoo Cat#: 574023

Name: SR1903 free base

CAS#: 1414248-06-8 (free base)

Chemical Formula: C27H27F6N3O

Exact Mass: 523.2058

Molecular Weight: 523.52

Elemental Analysis: C, 61.95; H, 5.20; F, 21.77; N, 8.03; O, 3.06

Price and Availability

Size Price Availability Quantity
1mg USD 250.00 2 weeks
5mg USD 500.00 2 weeks
10mg USD 700.00 2 weeks
Bulk Inquiry
Buy Now
Add to Cart
Related CAS #
2351884-03-0 (TFA) 1414248-06-8 (free base)
Synonym
SR 1903, SR-1903, SR1903
IUPAC/Chemical Name
2'-methyl-4'-[[4-(4-pyridinylmethyl)-1-piperazinyl]methyl]-α,α-bis(trifluoromethyl)-[1,1'-biphenyl]-4-methanol
InChi Key
HSUQYJQLSYQEOB-UHFFFAOYSA-N
InChi Code
InChI=1S/C27H27F6N3O/c1-19-16-21(18-36-14-12-35(13-15-36)17-20-8-10-34-11-9-20)2-7-24(19)22-3-5-23(6-4-22)25(37,26(28,29)30)27(31,32)33/h2-11,16,37H,12-15,17-18H2,1H3
SMILES Code
CC1=C(C2=CC=C(C(O)(C(F)(F)F)C(F)(F)F)C=C2)C=CC(CN(CC3)CCN3CC4=CC=NC=C4)=C1
Appearance
A crystalline solid
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
SR1903 is an inverse agonist of RORγ (IC50 = ~100 nM in a cell-based reporter assay) and an agonist of LXR. It also binds to peroxisome proliferator-activated receptor γ (PPARγ; IC50 = 209 nM) but does not activate it.
In vitro activity:
To be determined
In vivo activity:
SR1903 may represent a viable strategy for treatment of both metabolic and inflammatory disease. In a murine model of obesity, SR1903 aided in the maintenance of the thymic homeostasis, unlike selective RORγ inverse agonists. The ability of SR1903 to block LPS signaling suggests its potential utility for treating innate immune response disorders. Reference: ACS Chem Biol. 2019 May 17;14(5):1051-1062. https://pubmed.ncbi.nlm.nih.gov/30951276/
Solvent mg/mL mM comments
Solubility
DMF 20.0 38.20
DMSO 20.0 38.20
Ethanol 10.0 19.10
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 523.52 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Chang MR, Ciesla A, Strutzenberg TS, Novick SJ, He Y, Garcia-Ordonez RD, Frkic RL, Bruning JB, Kamenecka TM, Griffin PR. Unique Polypharmacology Nuclear Receptor Modulator Blocks Inflammatory Signaling Pathways. ACS Chem Biol. 2019 May 17;14(5):1051-1062. doi: 10.1021/acschembio.9b00236. Epub 2019 Apr 15. PMID: 30951276.
In vitro protocol:
To be determined
In vivo protocol:
1. Chang MR, Ciesla A, Strutzenberg TS, Novick SJ, He Y, Garcia-Ordonez RD, Frkic RL, Bruning JB, Kamenecka TM, Griffin PR. Unique Polypharmacology Nuclear Receptor Modulator Blocks Inflammatory Signaling Pathways. ACS Chem Biol. 2019 May 17;14(5):1051-1062. doi: 10.1021/acschembio.9b00236. Epub 2019 Apr 15. PMID: 30951276.
1. Chang, M.R., Ciesla, A., Strutzenberg, T.S., et al. Unique polypharmacology nuclear receptor modulator blocks inflammatory signaling pathways. ACS Chem. Biol. 14(5), 1051-1062 (2019).