HX 531
目录号 : GC16814HX 531是一种强效的视黄醇X受体（RXR）拮抗剂。
Cas No.:188844-34-0
Sample solution is provided at 25 µL, 10mM.
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HX 531 is a potent retinoid X receptor (RXR) antagonist[1].
In vitro, Pre-treatment with HX 531 (2.5μM; 30min) attenuated the anti-apoptotic effect of all-trans retinoic acid (t-RA) in protecting mesangial cells from H₂O₂-induced apoptosis via the inhibition of the activator protein 1 (AP-1) pathway[2]. HX 531 (0.1μM; 45-60min) significantly inhibits Benzophenone-3 (BP-3)-induced neuronal apoptosis and partially reverses the effects of BP-3 on the expression of RXR receptors and epigenetic status[3].
In vivo, Wild-type mice treated with HX 531(2 weeks; p.o.) were protected from high-fat (HF) diet-induced hyperglycemia and insulin resistance[4]. The weight gain of OLETF rats treated with HX 531 (10mg/kg/day; 22 weeks; p.o.) was significantly suppressed, and the fat pad weight was significantly reduced, comparable to that of non-diabetic LETO rats[5].
References:
[1] Alique M, Lucio FJ, Herrero JF. Vitamin A active metabolite, all-trans retinoic acid, induces spinal cord sensitization. II. Effects after intrathecal administration. Br J Pharmacol. 2006 Sep;149(1):65-72.
[2] Konta T, Xu Q, Furusu A, et al. Selective roles of retinoic acid receptor and retinoid x receptor in the suppression of apoptosis by all-trans-retinoic acid. J Biol Chem. 2001 Apr 20;276(16):12697-701.
[3] Wnuk A, Rzemieniec J, Lasoń W, et al. Benzophenone-3 Impairs Autophagy, Alters Epigenetic Status, and Disrupts Retinoid X Receptor Signaling in Apoptotic Neuronal Cells. Mol Neurobiol. 2018 Jun;55(6):5059-5074.
[4] Yamauchi T, Waki H, Kamon J, et al. Inhibition of RXR and PPARgamma ameliorates diet-induced obesity and type 2 diabetes. J Clin Invest. 2001 Oct;108(7):1001-13.
[5] Nakatsuka A, Wada J, Hida K, et al. RXR antagonism induces G0 /G1 cell cycle arrest and ameliorates obesity by up-regulating the p53-p21(Cip1) pathway in adipocytes. J Pathol. 2012 Apr;226(5):784-95.
HX 531是一种强效的视黄醇X受体（RXR）拮抗剂[1]。
在体外实验中，用HX 531（2.5μM; 30分钟）预处理可减弱全反式维甲酸（t-RA）通过抑制激活蛋白1（AP-1）通路保护系膜细胞免受H₂O₂诱导的凋亡的抗凋亡作用[2]。HX 531（0.1μM; 45-60分钟）显著抑制苯甲酮-3（BP-3）诱导的神经元凋亡，并部分逆转BP-3对RXR受体表达和表观遗传状态的影响[3]。
在体内实验中，野生型小鼠经HX 531（2周; 口服）处理后，可免受高脂（HF）饮食诱导的高血糖和胰岛素抵抗[4]。用HX 531（10mg/kg/天; 22周; 口服）处理的OLETF大鼠体重增长显著受到抑制，脂肪垫重量显著减少，与非糖尿病LETO大鼠相当[5]。
| Cell experiment [1]: | |
Cell lines | RBL-2H3 cells |
Preparation Method | Primary neuronal cell cultures were exposed to BP-3 (10-100μM) for 6 or 24h. The involvement of RXR signaling in BP-3-induced effects was verified with the high-affinity RXR antagonist HX 531 (0.1μM) and the RXR agonist DHA (1μM). Specific ligands were added to the culture media 45-60min before BP-3. Apoptotic cells were detected via Hoechst 33342 staining at 24h after treatment. Neocortical cells that were cultured on glass coverslips were washed with 10mM phosphate-buffered saline (PBS) and stained with Hoechst 33342 (0.6mg/ml) at room temperature (RT) for 5min. The cells containing bright blue fragmented nuclei, indicative of condensed chromatin, were identified as apoptotic cells. Qualitative analysis was performed using a fluorescence microscope. The level of cellular fluorescence from fluorescence microscopy images was determined using ImageJ software. |
Reaction Conditions | 0.1μM; 45-60min |
Applications | HX 531 significantly inhibits Benzophenone-3 (BP-3)-induced neuronal apoptosis and partially reverses the effects of BP-3 on the expression of RXR receptors and epigenetic status. |
| Animal experiment [2]: | |
Animal models | Eight-week-old male Otsuka Long–Evans Tokushima Fatty (OLETF) rats |
Preparation Method | Eight-week-old male Otsuka Long–Evans Tokushima Fatty (OLETF) rats, which serve as a model for obesity and type 2 diabetes, were divided into three groups: OLETF rats (OLETF group); OLETF rats treated with pioglitazone (PIO group); and OLETF rats treated with HX 531 (HX 531 group). Non-diabetic Long–Evans Tokushima Otsuka (LETO) rats were fed a chow diet and served as the control group (LETO group). Pioglitazone and HX 531 were mixed into the diet, and each group orally received 1mg pioglitazone/kg body weight/day and 10mg HX 531/kg body weight/day throughout the experimental period. After conducting the described studies, the rats were sacrificed at 30 weeks of age. |
Dosage form | 10mg/kg/day; 22 weeks; p.o. |
Applications | The weight gain of OLETF rats treated with HX 531 was significantly suppressed, and the fat pad weight was significantly reduced, comparable to that of non-diabetic LETO rats. |
References: | |
| Cas No. | 188844-34-0 | SDF | |
| 化学名 | 4-(5,7,7,10,10-pentamethyl-2-nitro-7,8,9,10-tetrahydro-5H-benzo[b]naphtho[2,3-e][1,4]diazepin-12-yl)benzoic acid | ||
| Canonical SMILES | CC(CCC1(C)C)(C2=CC(C(C3=CC=C(C(O)=O)C=C3)=NC4=C(N5C)C=CC(N(=O)=O)=C4)=C5C=C21)C | ||
| 分子式 | C29H29N3O4 | 分子量 | 483.56 |
| 溶解度 | 0.12mg/mL in ethanol, 10mg/mL in DMSO, 15mg/mL in DMF | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.068 mL | 10.34 mL | 20.68 mL |
| 5 mM | 413.6 μL | 2.068 mL | 4.136 mL |
| 10 mM | 206.8 μL | 1.034 mL | 2.068 mL |
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动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度： mg/ml；
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2.
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Quality Control & SDS
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- Purity: >97.00%
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