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MedKoo Cat#: 574411 | Name: SR1001
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Description:

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

SR1001 is a novel ROR Ligand that suppresses TH17 differentiation and autoimmunity. SR1001 enhances the inhibitory ability of melatonin on Th17 and DN T cells production, and agonist SR1078 weakens the effects of melatonin.

Chemical Structure

SR1001
SR1001
CAS#1335106-03-0

Theoretical Analysis

MedKoo Cat#: 574411

Name: SR1001

CAS#: 1335106-03-0

Chemical Formula: C15H13F6N3O4S2

Exact Mass: 477.0252

Molecular Weight: 477.39

Elemental Analysis: C, 37.74; H, 2.74; F, 23.88; N, 8.80; O, 13.41; S, 13.43

Price and Availability

Size Price Availability Quantity
25mg USD 250.00 2 Weeks
50mg USD 450.00 2 Weeks
100mg USD 750.00 2 Weeks
200mg USD 1,250.00 2 Weeks
500mg USD 2,150.00 2 Weeks
1g USD 2,950.00 2 Weeks
2g USD 5,250.00 2 Weeks
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Related CAS #
No Data
Synonym
SR1001, SR 1001, SR-1001
IUPAC/Chemical Name
N-[4-Methyl-5-[[[4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]amino]sulfonyl]-2-thiazolyl]-acetamide
InChi Key
OZBSSKGBKHOLGA-UHFFFAOYSA-N
InChi Code
InChI=1S/C15H13F6N3O4S2/c1-7-11(29-12(22-7)23-8(2)25)30(27,28)24-10-5-3-9(4-6-10)13(26,14(16,17)18)15(19,20)21/h3-6,24,26H,1-2H3,(H,22,23,25)
SMILES Code
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
Appearance
Solid powder
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, DMF, and ethanol
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:
SR1001 is a selective RORα and RORγt inverse agonist with Kis 172 and 111 nM, respectively.
In vitro activity:
This study suggests that simvastatin-mediated macrophage apoptosis might be modulated by SR1001 administration. Compared with non-treated controls, simvastatin significantly decreased THP-1 macrophage cell viability (p=0.04) and cell count (p=0.03). However, this negative effect of simvastatin seemed to be partly prevented by SR1001. Reference: Anatol J Cardiol. 2017 May;17(5):362-366. https://pubmed.ncbi.nlm.nih.gov/28613211/
In vivo activity:
SR1001 inhibited TH17 cell differentiation and function by binding to RORα and RORγt, altering their transcriptional activity. SR1001 effectively suppressed TH17 cell development and cytokine expression in mice and human cells, suggesting potential for treating autoimmune diseases. Reference: Nature. 2011 Apr 28;472(7344):491-4. https://pubmed.ncbi.nlm.nih.gov/21499262/
Solvent mg/mL mM comments
Solubility
DMF 20.0 41.89
DMSO 20.0 41.89
Ethanol 30.0 62.84
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 477.39 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. Çoban N, Güleç Ç, Özsait Selçuk B, Erginel-Ünaltuna N. Role of simvastatin and RORα activity in the macrophage apoptotic pathway. Anatol J Cardiol. 2017 May;17(5):362-366. doi: 10.14744/AnatolJCardiol.2016.7411. Epub 2017 Feb 1. PMID: 28613211; PMCID: PMC5469082. 2. Xiao L, Zhang Z, Luo X, Yang H, Li F, Wang N. Retinoid acid receptor-related orphan receptor alpha (RORα) regulates macrophage M2 polarization via activation of AMPKα. Mol Immunol. 2016 Dec;80:17-23. doi: 10.1016/j.molimm.2016.10.006. Epub 2016 Oct 24. PMID: 27788394. 3. Liu P, Xiao Z, Lu X, Zhang X, Huang J, Li C. Fasudil and SR1001 synergistically protect against sepsis-associated pancreatic injury by inhibiting RhoA/ROCK pathway and Th17/IL-17 response. Heliyon. 2023 Sep 18;9(9):e20118. doi: 10.1016/j.heliyon.2023.e20118. PMID: 37809525; PMCID: PMC10559842. 4. Solt LA, Kumar N, Nuhant P, Wang Y, Lauer JL, Liu J, Istrate MA, Kamenecka TM, Roush WR, Vidović D, Schürer SC, Xu J, Wagoner G, Drew PD, Griffin PR, Burris TP. Suppression of TH17 differentiation and autoimmunity by a synthetic ROR ligand. Nature. 2011 Apr 28;472(7344):491-4. doi: 10.1038/nature10075. Epub 2011 Apr 17. PMID: 21499262; PMCID: PMC3148894.
In vitro protocol:
1. Çoban N, Güleç Ç, Özsait Selçuk B, Erginel-Ünaltuna N. Role of simvastatin and RORα activity in the macrophage apoptotic pathway. Anatol J Cardiol. 2017 May;17(5):362-366. doi: 10.14744/AnatolJCardiol.2016.7411. Epub 2017 Feb 1. PMID: 28613211; PMCID: PMC5469082. 2. Xiao L, Zhang Z, Luo X, Yang H, Li F, Wang N. Retinoid acid receptor-related orphan receptor alpha (RORα) regulates macrophage M2 polarization via activation of AMPKα. Mol Immunol. 2016 Dec;80:17-23. doi: 10.1016/j.molimm.2016.10.006. Epub 2016 Oct 24. PMID: 27788394.
In vivo protocol:
1. Liu P, Xiao Z, Lu X, Zhang X, Huang J, Li C. Fasudil and SR1001 synergistically protect against sepsis-associated pancreatic injury by inhibiting RhoA/ROCK pathway and Th17/IL-17 response. Heliyon. 2023 Sep 18;9(9):e20118. doi: 10.1016/j.heliyon.2023.e20118. PMID: 37809525; PMCID: PMC10559842. 2. Solt LA, Kumar N, Nuhant P, Wang Y, Lauer JL, Liu J, Istrate MA, Kamenecka TM, Roush WR, Vidović D, Schürer SC, Xu J, Wagoner G, Drew PD, Griffin PR, Burris TP. Suppression of TH17 differentiation and autoimmunity by a synthetic ROR ligand. Nature. 2011 Apr 28;472(7344):491-4. doi: 10.1038/nature10075. Epub 2011 Apr 17. PMID: 21499262; PMCID: PMC3148894.
1: Wang H, Wang F, Li Y, Zhou P, Cai S, Wu Q, Ding T, Wu C, Zhu Q. Exosomal miR-205-5p contributes to the immune liver injury induced by trichloroethylene: Pivotal role of RORα mediating M1 Kupffer cell polarization. Ecotoxicol Environ Saf. 2024 Oct 15;285:117050. doi: 10.1016/j.ecoenv.2024.117050. Epub 2024 Sep 14. PMID: 39278002. 2: Teppan J, Schwanzer J, Rittchen S, Bärnthaler T, Lindemann J, Nayak B, Reiter B, Luschnig P, Farzi A, Heinemann A, Sturm E. The disrupted molecular circadian clock of monocytes and macrophages in allergic inflammation. Front Immunol. 2024 May 28;15:1408772. doi: 10.3389/fimmu.2024.1408772. PMID: 38863703; PMCID: PMC11165079. 3: Yuan B, Fang XL, Yang SW, Tian T, Zhu LG, Li Y, DU XZ, Peng XY, Yao XQ, Wang JH. Electroacupuncture of scalp acupoint alleviates cerebral ischemic inflammatory injury by down-regulating RORγt and promoting balance of IL-17A+Th17/FOXP3+Treg in MCAO rats. Zhen Ci Yan Jiu. 2024 Feb 25;49(2):135-144. English, Chinese. doi: 10.13702/j.1000-0607.20221062. PMID: 38413034. 4: Liu P, Xiao Z, Lu X, Zhang X, Huang J, Li C. Fasudil and SR1001 synergistically protect against sepsis-associated pancreatic injury by inhibiting RhoA/ROCK pathway and Th17/IL-17 response. Heliyon. 2023 Sep 18;9(9):e20118. doi: 10.1016/j.heliyon.2023.e20118. PMID: 37809525; PMCID: PMC10559842. 5: Wang S, Deng W, Li F, Xiang L, Lv P, Chen Y. Treatment with butyrate alleviates dextran sulfate sodium and Clostridium difficile-induced colitis by preventing activity of Th17 cells via regulation of SIRT1/mTOR in mice. J Nutr Biochem. 2023 Jan;111:109155. doi: 10.1016/j.jnutbio.2022.109155. Epub 2022 Sep 24. PMID: 36162566. 6: Peng Z, Peng S, Lin K, Zhao B, Wei L, Tuo Q, Liao D, Yuan T, Shi Z. Chronic stress-induced depression requires the recruitment of peripheral Th17 cells into the brain. J Neuroinflammation. 2022 Jul 14;19(1):186. doi: 10.1186/s12974-022-02543-6. PMID: 35836182; PMCID: PMC9281140. 7: Liu Y, Chen XQ, Wang F, Cheng B, Zhou G. Melatonin relieves Th17/CD4-CD8- T cells inflammatory responses via nuclear- receptor dependent manner in peripheral blood of primary Sjögren's syndrome. Int Immunopharmacol. 2022 Aug;109:108778. doi: 10.1016/j.intimp.2022.108778. Epub 2022 May 7. PMID: 35537347. 8: Song L, Qi S, Hu W, Fang Z, Yu D, Liu T, Wu J, Wu Y, Wu A, Feng L, Xie J, Zhang B, He W, Ning Z, Liu L, Qin JJ, Li S. Integrative analysis reveals clinically relevant molecular fingerprints in pancreatic cancer. Mol Ther Nucleic Acids. 2021 Jul 2;26:11-21. doi: 10.1016/j.omtn.2021.06.015. PMID: 34513290; PMCID: PMC8408433. 9: Wang J, Xu Y, Jing H, Chang Q, Wu X, Zhang Z. RORγt inhibitor SR1001 alleviates acute pancreatitis by suppressing pancreatic IL-17-producing Th17 and γδ-T cells in mice with ceruletide-induced pancreatitis. Basic Clin Pharmacol Toxicol. 2021 Nov;129(5):357-368. doi: 10.1111/bcpt.13642. Epub 2021 Sep 2. PMID: 34384137; PMCID: PMC9291878. 10: Wang S, Deng W, Li F, Chen YE, Wang PU. Blockade of T helper 17 cell function ameliorates recurrent Clostridioides difficile infection in mice. Acta Biochim Biophys Sin (Shanghai). 2021 Oct 12;53(10):1290-1299. doi: 10.1093/abbs/gmab107. PMID: 34379099. 11: Auclair M, Roblot N, Capel E, Fève B, Antoine B. Pharmacological modulation of RORα controls fat browning, adaptive thermogenesis, and body weight in mice. Am J Physiol Endocrinol Metab. 2021 Feb 1;320(2):E219-E233. doi: 10.1152/ajpendo.00131.2020. Epub 2020 Nov 30. PMID: 33252251; PMCID: PMC8260366. 12: Toporova L, Grimaldi M, Boulahtouf A, Balaguer P. Assessing the Selectivity of FXR, LXRs, CAR, and RORγ Pharmaceutical Ligands With Reporter Cell Lines. Front Pharmacol. 2020 Jul 24;11:1122. doi: 10.3389/fphar.2020.01122. PMID: 32792956; PMCID: PMC7394005. 13: Zapadka TE, Lindstrom SI, Taylor BE, Lee CA, Tang J, Taylor ZRR, Howell SJ, Taylor PR. RORγt Inhibitor-SR1001 Halts Retinal Inflammation, Capillary Degeneration, and the Progression of Diabetic Retinopathy. Int J Mol Sci. 2020 May 17;21(10):3547. doi: 10.3390/ijms21103547. PMID: 32429598; PMCID: PMC7279039. 14: Li Z, Zhao J, Liu H, Wang J, Lu W. Melatonin inhibits apoptosis in mouse Leydig cells via the retinoic acid-related orphan nuclear receptor α/p53 pathway. Life Sci. 2020 Apr 1;246:117431. doi: 10.1016/j.lfs.2020.117431. Epub 2020 Feb 13. PMID: 32061868. 15: Li C, Peng G, Long J, Xiao P, Zeng X, Yang H. Protective effects of resveratrol and SR1001 on hypoxia-induced pulmonary hypertension in rats. Clin Exp Hypertens. 2020 Aug 17;42(6):519-526. doi: 10.1080/10641963.2020.1714643. Epub 2020 Jan 23. PMID: 31973589. 16: Zhu XY, Guo SY, Xia B, Li CQ, Wang L, Wang YH. Development of zebrafish demyelination model for evaluation of remyelination compounds and RORγt inhibitors. J Pharmacol Toxicol Methods. 2019 Jul-Aug;98:106585. doi: 10.1016/j.vascn.2019.106585. Epub 2019 May 18. PMID: 31112751. 17: Yang Y, Jia Y, Sun Q, Dong H, Zhao R. White light emitting diode induces autophagy in hippocampal neuron cells through GSK-3-mediated GR and RORα pathways. Aging (Albany NY). 2019 Mar 28;11(6):1832-1849. doi: 10.18632/aging.101878. PMID: 30923260; PMCID: PMC6461168. 18: Wei PC, Tong L, Li R. [Effect of RORC inhibitor on HIF-1α and VEGF in nasal mucosa of allergic rhinitis of mice]. Zhonghua Er Bi Yan Hou Tou Jing Wai Ke Za Zhi. 2018 Oct 7;53(10):751-756. Chinese. doi: 10.3760/cma.j.issn.1673-0860.2018.10.007. PMID: 30347534. 19: Weng X, Liu Y, Cui S, Cheng B. The role of RORα in salivary gland lesions in patients with primary Sjögren's syndrome. Arthritis Res Ther. 2018 Sep 6;20(1):205. doi: 10.1186/s13075-018-1698-5. PMID: 30189901; PMCID: PMC6127992. 20: Ghoshal S, Stevens JR, Billon C, Girardet C, Sitaula S, Leon AS, Rao DC, Skinner JS, Rankinen T, Bouchard C, Nuñez MV, Stanhope KL, Howatt DA, Daugherty A, Zhang J, Schuelke M, Weiss EP, Coffey AR, Bennett BJ, Sethupathy P, Burris TP, Havel PJ, Butler AA. Adropin: An endocrine link between the biological clock and cholesterol homeostasis. Mol Metab. 2018 Feb;8:51-64. doi: 10.1016/j.molmet.2017.12.002. Epub 2017 Dec 30. PMID: 29331507; PMCID: PMC5985041.