MedKoo Cat#: 125877 | Name: SR10171

Description:

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

SR10171 is a PPARα agonist. SR10171 is an optimized analog of SR1664 which demonstrates high-affinity binding to PPARγ and unlike SR1664, exhibits partial inverse agonism of PPRE-mediated transcriptional activity and demonstrates modest PPARα agonist activity (EC50=1.5μM). The structure-activity relation-ship (SAR) of SR10171 is consistent with other examples from this chemical series. Importantly, SR10171 effectively blocks phosphorylation of S273 (pS273), which has been shown to correlate with PPARγ insulin sensitizing activity; however, in contrast to full agonist rosiglitazone, SR10171 inverse agonism actively suppresses PPARγ basal transcriptional activity.

Chemical Structure

SR10171
SR10171
CAS#1415321-54-8

Theoretical Analysis

MedKoo Cat#: 125877

Name: SR10171

CAS#: 1415321-54-8

Chemical Formula: C34H40N2O4

Exact Mass: 540.2988

Molecular Weight: 540.70

Elemental Analysis: C, 75.53; H, 7.46; N, 5.18; O, 11.84

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
No Data
Synonym
SR10171; SR 10171; SR-10171
IUPAC/Chemical Name
(S)-2-(3-((5-((1-(4-(tert-butyl)phenyl)ethyl)carbamoyl)-2,3-dimethyl-1H-indol-1-yl)methyl)phenoxy)-2-methylpropanoic acid
InChi Key
DLXSTRGKTJFVEB-QFIPXVFZSA-N
InChi Code
InChI=1S/C34H40N2O4/c1-21-23(3)36(20-24-10-9-11-28(18-24)40-34(7,8)32(38)39)30-17-14-26(19-29(21)30)31(37)35-22(2)25-12-15-27(16-13-25)33(4,5)6/h9-19,22H,20H2,1-8H3,(H,35,37)(H,38,39)/t22-/m0/s1
SMILES Code
CC(C)(OC1=CC=CC(CN2C(C)=C(C)C3=C2C=CC(C(N[C@H](C4=CC=C(C(C)(C)C)C=C4)C)=O)=C3)=C1)C(O)=O
Appearance
To be determined
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
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
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

Preparing Stock Solutions

The following data is based on the product molecular weight 540.70 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
1: Stechschulte LA, Czernik PJ, Rotter ZC, Tausif FN, Corzo CA, Marciano DP, Asteian A, Zheng J, Bruning JB, Kamenecka TM, Rosen CJ, Griffin PR, Lecka- Czernik B. PPARG Post-translational Modifications Regulate Bone Formation and Bone Resorption. EBioMedicine. 2016 Aug;10:174-84. doi: 10.1016/j.ebiom.2016.06.040. Epub 2016 Jun 29. PMID: 27422345; PMCID: PMC5006645. 2: Lam VQ, Zheng J, Griffin PR. Unique Interactome Network Signatures for Peroxisome Proliferator-activated Receptor Gamma (PPARγ) Modulation by Functional Selective Ligands. Mol Cell Proteomics. 2017 Dec;16(12):2098-2110. doi: 10.1074/mcp.RA117.000308. Epub 2017 Sep 29. PMID: 28972081; PMCID: PMC5724174. 3: Frkic RL, Marshall AC, Blayo AL, Pukala TL, Kamenecka TM, Griffin PR, Bruning JB. PPARγ in Complex with an Antagonist and Inverse Agonist: a Tumble and Trap Mechanism of the Activation Helix. iScience. 2018 Feb 27;5:69-79. doi: 10.1016/j.isci.2018.06.012. Epub 2018 Jul 2. PMID: 30123887; PMCID: PMC6095676.