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作靶點(diǎn): Apoptosis; JNK; Akt; Caspase; FXR作通路: Apoptosis; MAPK/ERK Pathway; PI3K/Akt/mTOR; MetabolicEnzyme/Protease儲(chǔ)存式: 4C, protect from

2、light* In solvent : -80C, 6 months; -20C, 1 month (protect fromlight)溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 20.83 mg/mL (66.67 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液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請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配

3、制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前?qǐng)先配制澄清的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (6.66 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)

4、Solubility: 2.08 mg/mL (6.66 mM); Clear solution3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oil1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 2.08 mg/mL (6.66 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Guggulsterone種植物甾醇，來(lái) Commiphora wightii 樹(shù)的樹(shù)膠脂。 Guggulsterone 通過(guò)下調(diào)抗細(xì)胞凋亡 (apoptosis) 因產(chǎn)物 (IAP1，xIAP

5、，Bfl-1/A1，Bcl-2，cFLIP，survivin)，調(diào)節(jié)細(xì)胞周 期蛋 (cyclin D1，c-Myc)，激活 caspases，JNK，抑制 Akt，抑制多種腫瘤細(xì)胞的長(zhǎng)并誘導(dǎo)細(xì)胞凋亡。Guggulsterone 通過(guò)調(diào)節(jié)種轉(zhuǎn)錄因介導(dǎo) 因表達(dá)，包括 NF-B，STAT3，C /EBP，雄激素受體 (androgen receptor) 和糖質(zhì)激素受體(glucocorticoid receptors)。Guggulsterone，種法尼醇 X 受體 (FXR) 拮抗劑，可降低 CDCA 誘導(dǎo)的FXR 活化，Z- 和 E-Guggulsterone 的 IC50 分別為 17 和

6、15 M。IC50 & Target JNK Akt Caspase體外研究 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.體內(nèi)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 您邊的抑制劑師www.MedChemECaution: Product has not been fully validated for medical