HX 531 - CAS:188844-34-0

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HX 531

目录号 : KCM12228 CAS No. : 188844-34-0 纯度 : ≥95%

Data Sheet 产品使用指南

HX 531 is an antagonist of the retinoid X receptor (RXR) with an IC value of 18 nM that inhibits 9-cis retinoic acid -induced transactivation of RXR. It has been shown to reduce triglyceride content in white adipose tissue, skeletal muscle, and the liver of mice on a high fat diet.

规格	价格	是否有货	数量
10 mM * 1 mL in DMSO		In-stock
1mg		In-stock
5mg		In-stock
10mg		In-stock
25mg		In-stock
50mg		In-stock

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生物活性

HX 531 is an orally active RXR antagonist with an IC50 of 18 nM. HX531 upregulates the p53-p21Cip1 pathway. HX531 abrogates the anti-apoptotic effect of t-RA. HX531 exerts anti-obesity, anti-diabetic and anti-melanoma activities.

体外研究

HX531 (2.5 μM, 30 min) eliminates the anti apoptotic effect of t-RA.
HX531 (0-10 μM, 24 h) had no significant effect on PPAR α/RXR agonist induced transcriptional activation and PPAR γ agonist induced molecular expression.
HX531 (2.5 μM, 0-10 days) upregulates the p53-p21 Cip1 pathway to induce G0/G1 cell cycle arrest and inhibit HPV differentiation in human visceral preadipocytes.
HX531 (2.5 μM, 0-10 days) reversed high glucose induced G0/G1 cell cycle arrest to normal glucose levels in normal human mesangial cell NHMCs.
HX531 delays melanoma drug resistance and prevents polarization of M2 macrophages in the tumor microenvironment.

Apoptosis Analysis

Cell Line:	Mesangial cells
Concentration:	2.5 μM
Incubation Time:	30 min
Result:	Increased the activity of AP-1, eliminating the anti-apoptotic effect of t-RA.

Western Blot Analysis

Cell Line:	FAO
Concentration:	0, 1, 10 μM
Incubation Time:	24 hours
Result:	Had no significant effect on transcriptional activation induced by PPARα/RXR agonists and molecular expression induced by PPARγ agonists.

Western Blot Analysis

Cell Line:	HVP; NHMCs
Concentration:	2.5 μM
Incubation Time:	0, 2, 4, 6, 8, 10 days
Result:	Reduced the number and size of lipid droplets, upregulated cell cycle regulators p53, p21Cip1, cyclin D1, Fbxw7, and Skp2, and enhanced the expression of pAMPKα in HVP. ShRNA lentivirus knockdown of p53 reversed the HX531-induced upregulation of p21Cip1 in HVP. Suppressed the expression of p21Cip1, p27Kip1, p53, and cyclin D1, while the phosphorylation levels of p44/42 MAPK and p38 MAPK returned to baseline levels under normal glucose conditions in NHMCs.

Cell Cycle Analysis

Cell Line:	NHMCs
Concentration:	2.5 μM
Incubation Time:	0, 2, 4, 6, 8, 10 days
Result:	Reversed high sugar-induced G0/G1 cell cycle arrest back to normal glucose levels.

体内研究

HX531 (0.1% and 0.3% food additive, oral, two weeks) prevents weight gain in mice with HF diet and prevents HF diet induced hyperglycemia and hyperinsulinemia, and increases leptin levels.

HX531 (0.1% and 0.3% food additive, oral, two weeks) prevents adipocyte hypertrophy and reduces insulin resistance. HX531 (0.1% and 0.3% food additive, oral, two weeks) directly antagonizes PPAR γ/RXR, reduces molecules involved in fatty acid influx and fat production in skeletal muscle, and increases molecules involved in energy expenditure.

HX531 (0.1% and 0.3% food additive, oral, 3-4 weeks) leads to the recurrence of hyperglycemia and insulin resistance associated with fat atrophy.

HX531 (10 mg/kg, orally, daily, 30 weeks) reduces body weight, inhibits adipocyte hypertrophy, and induces G0/G1 cell cycle arrest in rats.

Animal Model:	KKAy mouse induced by HF or HC
Dosage:	0.1% and 0.3% food additive, 2 weeks
Administration:	Oral
Result:	Reduced the body weight of mice, fasting blood glucose, fasting plasma insulin, and insulin tolerance. Increased Rectal temperature, rosed oxygen consumption , and serum leptin levels went up. Lowered the expression of fatty acid translocase/CD36, increased the expression of β3-adrenergic receptors (β3-AR), and decreased free fatty acids (FFA), TNF-α, and resistin. Reduced the expression of lipogenic enzymes SREBP1 and SCD1, increased the expression of molecules involved in fatty acid burning like ACO, and molecules that dissipate energy like UCP2, lowered long-chain FA-CoA and triglyceride levels in muscle.

Animal Model:	PPARγ deficient mice
Dosage:	0.1% and 0.3% food additive, 3 and 4 weeks
Administration:	Oral
Result:	Prevented the reoccurrence of high blood sugar and insulin resistance associated with fatty atrophy.

Animal Model:	LETO and OLETF rats
Dosage:	10 mg/kg, daily, 30 weeks
Administration:	Oral
Result:	Suppressed weight gain and reduced the excretion of urinary albumin.Led to G0/G1 cell cycle arrest, inhibited adipocyte hypertrophy, and suppressed the proliferation activity of fat cells.

分子式

C₂₉H₂₉N₃O₄

分子量

483.56

CAS号

188844-34-0

中文名称

4-(7,8,9,10-四氢-5,7,7,10,10-五甲基-2-硝基-5H-苯并[b]萘并[2,3-e][1,4]二氮杂卓-12-基)苯甲酸

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 33.33 mg/mL (68.93 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0680 mL	10.3400 mL	20.6800 mL
5 mM	0.4136 mL	2.0680 mL	4.1360 mL
10 mM	0.2068 mL	1.0340 mL	2.0680 mL

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, 6 months; -20°C, 1 month。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂：10% DMSO → 40% PEG300 → 5% Tween-80 → 45% saline

Solubility: ≥ 2.5 mg/mL (5.17 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.17 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
2.

请依序添加每种溶剂： 10% DMSO → 90% (20% SBE-β-CD in saline)

Solubility: 2.5 mg/mL (5.17 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (5.17 mM) 的均匀悬浊液，悬浊液可⽤于⼝服和腹腔注射。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD ⽣理盐⽔⽔溶液中，混合均匀。

纯度： ≥95%

Data Sheet

产品使用指南

Yamauchi T, et al. Inhibition of RXR and PPARgamma ameliorates diet-induced obesity and type 2 diabetes. J Clin Invest. 2001 Oct;108(7):1001-13.

Atsuko Nakatsuka, 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.

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量

浓度

体积

分子量*

重置计算

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度

体积

浓度

体积

重置计算

动物实验计算换算器

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量

mg/kg

动物平均体重

每只动物给药体积

动物数量

只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系客服为您提供正确的澄清溶液配方）

% DMSO

% Tween 80

% ddH₂O

% DMSO

计算重置

计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系客服）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

配置后的溶液总体积：

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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KKL 顾客使用本产品发表的 0 篇科研文献

The molarity calculator equation

The dilution calculator equation

动物实验计算换算器