SR-1903
SR-1903 is an inverse agonist of RORγ and PPARγ (IC50 of ∼100 nM and 209 nM for RORγ and PPARγ, respectively) and a LXR agonist. SR-1903 exhibits anti-inflammatory and anti-diabetic efficacy in collagen-induced arthritis and diet-induced obesity mouse models.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1414248-06-8
- 分子式: C27H27F6N3O
- 分子量:523.51
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
製品説明
IC50 & Target
[1]|
RORγ ~100 nM (IC50) |
PPARγ 209 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | IC50 |
70 nM
Compound: 16
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Displacement of [3H]T0901317 from human RoRc expressed in HepG2 cells by scintillation proximity binding assay
Displacement of [3H]T0901317 from human RoRc expressed in HepG2 cells by scintillation proximity binding assay
|
[PMID: 24502334] |
体外実験
SR1903 (10 μM) attenuates LPS (HY-D1056) signaling in macrophages, with suppression of TREM-1 gene expression[1].
SR1903 increases expression of LXR target genes, including genes involved in macrophage cholesterol efflux (ABCG1 and SCD) and lipid metabolism (ACACA and FASN) in macrophage RAW264.7[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
SR1903 (20 mg/kg, i.p., 14 days) improves metabolic parameters and protects against obesity-associated thymic degeneration in diet-induced obese (DIO) mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Collagen-induced arthritis (female DBA/1J mice were injected with chicken type II collagen on day 1, and then each animal received a boost injection of collagen on day 21)[1]
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Dosage:20 mg/kg
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Administration:Intraperitoneal injection (i.p.), twice-a-day for a total of 16 days
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Result:Demonstrated a reduction in arthritis clinic score at the conclusion of the study (day 34).
Did not cause enlargement of the liver.
Had enhanced thymocyte differentiation and survival compared to mice treated with either the selective LXR agonist GW3965 or the dual LXR agonist/RORγ inverse agonist T0901317.
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Animal Model:Diet-induced obese (DIO) mouse (Male, 22 weeks of age, fed a high fat diet (60% kCal % fat))[1]
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Dosage:20 mg/kg
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Administration:Intraperitoneal injection (i.p.), 14 days
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Result:Improved fasting glucose levels and reduced total cholesterol and low density lipoprotein (LDL).
Improved both fasting and fed insulin levels.
Showed 15% weight loss and 17% reduction in fat mass after 14 days.
Reduced food intake.
Reduced leptin resistance and repressed Socs3 (suppressor of cytokine signaling-3) expression.
化学情報
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CAS 番号 1414248-06-8
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分子量 523.51
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分子式 C27H27F6N3O
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SMILES
OC(C(F)(F)F)(C(F)(F)F)C1=CC=C(C2=CC=C(CN3CCN(CC4=CC=NC=C4)CC3)C=C2C)C=C1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
SR-1903 関連分類
HY-138007 関連分類
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