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Purity: ≥98%
| Targets |
SR-0987 is a T cell-specific agonist of RORγ (RORγt), a nuclear receptor involved in the differentiation and function of Th17 cells. By activating RORγt, SR-0987 induces the expression of IL-17, a pro-inflammatory cytokine. It also decreases the expression of PD-1, an immune checkpoint molecule. Its mechanism involves agonism at RORγt, leading to modulation of T-cell function and immune responses.
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| ln Vitro |
SR0987, which has an EC50 of about 800 nM, demonstrates a concentration-dependent increase of reporter gene expression. While PD-1 surface expression was not affected by treatment with demofenol, it was statistically significant when treated with SR0987. An increase in IL17 production is observed after treatment with SR0987 and/or demosterol [1].
In vitro, SR-0987 is a RORγt agonist with an EC50 of 800 nM in a gene reporter assay. It induces IL-17 expression and decreases PD-1 expression in T cells. SR-0987 treatment significantly reduces the surface expression of PD-1. It increases IL17 production in T cells. Its in vitro activity is characterized by potent RORγt agonism and modulation of T-cell function. |
| ln Vivo |
In vivo, SR-0987 has potential for the treatment of cancer. As a RORγt agonist, it may enhance anti-tumor immune responses by inducing IL-17 and decreasing PD-1 expression. However, detailed in vivo efficacy data for specific disease models are limited. SR-0987 is primarily used as a research tool for studying RORγt biology and T-cell function.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for SR-0987 typically involve measuring its binding to RORγt or its activity in gene reporter assays. The compound is a T cell-specific RORγ (RORγt) agonist with an EC50 of 800 nM. These assays confirm its mechanism of action as a RORγt agonist.
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| Cell Assay |
In vitro cellular assays for SR-0987 typically involve treating T cells with the compound and measuring IL-17 and PD-1 expression. SR-0987 induces IL-17 expression and decreases PD-1 expression in T cells in vitro. These cell-based studies demonstrate its functional activity as a RORγt agonist and its effects on T-cell function.
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| Animal Protocol |
In vivo animal models for SR-0987 may include models of cancer or autoimmune diseases where RORγt plays a role. The compound is administered by appropriate routes, and immune responses or tumor growth are assessed. However, detailed animal protocol information is limited. SR-0987 is primarily used as a research tool for studying RORγt biology and T-cell function.
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| ADME/Pharmacokinetics |
SR-0987 has a molecular formula of C18H14F3N3O2S and a molecular weight of 393.38. Its CAS number is 303126-97-8. The compound is also known as SR0987. It is a RORγt agonist with an EC50 of 800 nM. SR-0987 induces IL-17 expression and decreases PD-1 expression in T cells. It is a SR1078 analog.
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| Toxicity/Toxicokinetics |
SR-0987 is a RORγt agonist with a well-characterized mechanism of action. As with any nuclear receptor agonist, potential toxicity may include effects on immune function and inflammation. The compound's safety profile should be evaluated in preclinical toxicology studies. SR-0987 is for research use only and is not approved for human therapeutic use. It represents a valuable tool for studying RORγt biology and T-cell function.
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| References | |
| Additional Infomation |
SR-0987 (CAS# 303126-97-8) is a T cell-specific RORγ (RORγt) agonist with an EC50 of 800 nM in a gene reporter assay. It induces IL-17 expression and decreases PD-1 expression in T cells in vitro. SR-0987 is a SR1078 analog and has potential for cancer treatment. The compound is for research use only and not for human therapeutic use.
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| Molecular Formula |
C16H10CLF6NO2
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|---|---|
| Molecular Weight |
397.7
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| Exact Mass |
397.03
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| CAS # |
303126-97-8
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| Related CAS # |
303126-97-8
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| PubChem CID |
2323435
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
378.8±42.0 °C at 760 mmHg
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| Flash Point |
182.9±27.9 °C
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| Vapour Pressure |
0.0±0.9 mmHg at 25°C
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| Index of Refraction |
1.541
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| LogP |
4.36
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
26
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| Complexity |
488
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
IZVBONMVWLTLNT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H10ClF6NO2/c17-12-4-2-1-3-11(12)13(25)24-10-7-5-9(6-8-10)14(26,15(18,19)20)16(21,22)23/h1-8,26H,(H,24,25)
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| Chemical Name |
2-Chloro-N-[4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]-benzamide
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| Synonyms |
SR-0987 SR0987 SR 0987
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| HS Tariff Code |
2934.99.9001
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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 : ≥ 150 mg/mL (~377.17 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.29 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 25.0 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: ≥ 2.5 mg/mL (6.29 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 25.0 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: ≥ 2.5 mg/mL (6.29 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 | 2.5145 mL | 12.5723 mL | 25.1446 mL | |
| 5 mM | 0.5029 mL | 2.5145 mL | 5.0289 mL | |
| 10 mM | 0.2514 mL | 1.2572 mL | 2.5145 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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