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Purity: ≥98%
SR1001 (SR-1001) is a novel, potent and selective antagonist/inhibitor/inverse agonist of the nuclear retinoic acid receptor-related orphan receptors RORα and RORγ with immunomodulatory effects. It inhibits RORα and RORγ with Kis 172 and 111 nM, respectively, and exhibits no activity at LXR or RORβ. RORα and RORγt are essential for the development of TH17 cells, T-helper cells that produce interleukin-17 and have recently been shown to have pathological roles in various autoimmune diseases. SR1001 binds to the ligand-binding domain of RORα and RORγt to decrease affinity of the receptor for coactivators and increse affinity for co-repressors. It inhibited the differentiation and function of TH17 cells and suppressed the clinical severity of a mouse model of multiple sclerosis.
| ln Vitro |
By reducing the expression of the IL-17A gene and the synthesis of IL-17A protein, SR1001 prevents the proliferation of TH17 cells. In a dose-dependent manner, SR1001 diminishes the coactivator TRAP220 NR box 2 peptide's responsiveness to RORγ (IC50 value ≈ 117 nM). Moreover, SR1001 suppresses the expression of cytokines when added to secretions or human TH17 cells [1].
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| ln Vivo |
In rat models, SR1001 successfully genetically predisposes the clinical severity of autoimmunity. Cyp7b1, Rev-erbα, and Serine 1 are hepatic ROR targets whose expression is inhibited when SR1001 is applied to C57BL/6 mice[1]. The internal citrate synthase mRNA expression pattern is eliminated by the SR1001a RORα counterregulator [2].
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| References |
[1]. Solt LA, et al. Suppression of TH17 differentiation and autoimmunity by a synthetic ROR ligand. Nature. 2011 Apr 28;472(7344):491-4.
[2]. Crumbley C, et al. Regulation of expression of citrate synthase by the retinoic acid receptor-related orphan receptor α (RORα). PLoS One. 2012;7(4):e33804 |
| Molecular Formula |
C15H13F6N3O4S2
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|---|---|
| Molecular Weight |
477.4018
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| CAS # |
1335106-03-0
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| SMILES |
S(C1=C(C([H])([H])[H])N=C(N([H])C(C([H])([H])[H])=O)S1)(N([H])C1C([H])=C([H])C(=C([H])C=1[H])C(C(F)(F)F)(C(F)(F)F)O[H])(=O)=O
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 39 mg/mL (~81.69 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.36 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.08 mg/mL (4.36 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.36 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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