Guggulsterone-Z-E-Guggulsterone-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEGuggulsteroneCat. No.: HY-107738CAS No.: 95975-55-6Synonyms: Z/E-Guggulsterone分式: CHO分量: 312.45作靶点: Apoptosis; JNK; Akt; Caspase; FXR作通路: Apoptosis; MAPK/ERK Pathway; PI3K/Akt/mTOR; MetabolicEnzyme/Protease储存式: 4C, protect from

2、light* In solvent : -80C, 6 months; -20C, 1 month (protect fromlight)溶解性数据体外实验 DMSO : 20.83 mg/mL (66.67 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.2005 mL 16.0026 mL 32.0051 mL5 mM 0.6401 mL 3.2005 mL 6.4010 mL10 mM 0.3201 mL 1.6003 mL 3.2005 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配

3、制储备液，并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (6.66 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)

4、Solubility: 2.08 mg/mL (6.66 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oil1/2 Master of Small Molecules 您边的抑制剂师www.MedChemESolubility: 2.08 mg/mL (6.66 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Guggulsterone种植物甾醇，来 Commiphora wightii 树的树胶脂。 Guggulsterone 通过下调抗细胞凋亡 (apoptosis) 因产物 (IAP1，xIAP

5、，Bfl-1/A1，Bcl-2，cFLIP，survivin)，调节细胞周 期蛋 (cyclin D1，c-Myc)，激活 caspases，JNK，抑制 Akt，抑制多种肿瘤细胞的长并诱导细胞凋亡。Guggulsterone 通过调节种转录因介导 因表达，包括 NF-B，STAT3，C /EBP，雄激素受体 (androgen receptor) 和糖质激素受体(glucocorticoid receptors)。Guggulsterone，种法尼醇 X 受体 (FXR) 拮抗剂，可降低 CDCA 诱导的FXR 活化，Z- 和 E-Guggulsterone 的 IC50 分别为 17 和

6、15 M。IC50 & Target JNK Akt Caspase体外研究 Guggulsterone (0.5-20 M; 24 hours) suppresses TREM-1, TLR4 and TNF- expression as well as thephosphorylation of IB and NF-B p65 by LPS 2.Western Blot Analysis 1Cell Line: RAW 264.7 murine macrophage cellsConcentration: 0.5, 5, 10, 20 MIncubation Time: 24 hoursR

7、esult: Suppressed TREM-1, TLR4, and TNF- expression as well as the phosphorylation of IB and NF-B p65 by LPS.体内研究 Guggulsterone (orally; 100 mg/kg once per day for 8 days) significantly improved the survival rates of wild-type mice with TNBS-induced colitis 2.Animal Model: Wild-type mice with TNBS-i

8、nduced colitis 2Dosage: 100 mg/kgAdministration: Orally; once per day; for 8 daysResult: Improved the survival rates of wild-type mice with TNBS-induced colitis.REFERENCES1. Shishodia S, et al. Guggulsterone for Chemoprevention of Cancer. Curr Pharm Des. 2016;22(3):294-306.2. Che X, et al. Protectiv

9、e effects of guggulsterone against colitis are associated with the suppression of TREM-1 and modulation ofmacrophages. Am J Physiol Gastrointest Liver Physiol. 2018 Jul 1;315(1):G128-G139.McePdfHeight2/2 Master of Small Molecules 您边的抑制剂师www.MedChemECaution: Product has not been fully validated for medical