UNC7467
目录号 : GC67791UNC7467 是一种有效的 IP6K抑制剂，IP6K2、IP6K1 和 IP6K6 的 IC50 值分别为 4.9、8.9 和1320 nM。UNC7467 可降低肌醇焦磷酸盐的水平。UNC7467 可用于肥胖研究。
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
UNC7467 is a potent IP6K inhibitor with values of 4.9, 8.9 and 1320 nM for IP6K2, IP6K1 and IP6K6, respectively. UNC7467 reduces levels of inositol pyrophosphates. UNC7467 can be used for obesity research[1].
UNC7467 (2.5 μM; 3 hours; HCT116 cells) reduces levels of inositol pyrophosphates. UNC7467 reduces 5-InsP7 levels by 81% and 5-InsP8 levels by 63%[1].
UNC7467 (5 mg/kg; i.p.; daily, for 4 weeks; diet-induced obesity mice) ameliorated diet induced obesity, insulin resistance, and hepatic steatosis[1].
UNC7467 (1-5 mg/kg; i.v. and i.p.; diet-induced obesity mice) exhibits low clearance (13.7 (mL/min)/kg) and large AUClast (6054 h•ng/mL for intra venous (i.v.) and 2527 h•ng/mL for intraperitoneal (i.p.)) in mice at 5 mg/kg dose[1].
| Animal Model: | Diet-induced obesity (DIO) mice[1] |
| Dosage: | 5 mg/kg |
| Administration: | Intraperitoneal injection; daily, for 4 weeks |
| Result: | Improved glycemic profiles, ameliorated hepatic steatosis, and reduced weight gain without altering food intake. |
| Animal Model: | Diet-induced obesity (DIO) mice[1] | ||||||||||||
| Dosage: | 5 mg/kg (Pharmacokinetic Analysis) | ||||||||||||
| Administration: | Intravenous injection and intraperitoneal injection | ||||||||||||
| Result: |
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[1]. Zhou Y, et, al. Development of Novel IP6K Inhibitors for the Treatment of Obesity and Obesity-Induced Metabolic Dysfunctions. J Med Chem. 2022 May 12;65(9):6869-6887.
| Cas No. | SDF | Download SDF | |
| 分子式 | C20H13NO3 | 分子量 | 315.32 |
| 溶解度 | DMSO : 14.29 mg/mL (45.32 mM; ultrasonic and warming and heat to 60°C) | 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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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.1714 mL | 15.8569 mL | 31.7138 mL |
| 5 mM | 0.6343 mL | 3.1714 mL | 6.3428 mL |
| 10 mM | 0.3171 mL | 1.5857 mL | 3.1714 mL |
| 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 | g | |
每只动物给药体积 | ul | |
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GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 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，
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 saline，混匀澄清。
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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Development of Novel IP6K Inhibitors for the Treatment of Obesity and Obesity-Induced Metabolic Dysfunctions
J Med Chem 2022 May 12;65(9):6869-6887.PMID:35467861DOI:10.1021/acs.jmedchem.2c00220
Obesity and obesity-induced metabolic dysfunctions are significant risk factors for nonalcoholic fatty liver disease and cardiovascular diseases. Thus, obesity is an economic and social burden in developed countries. Blocking the synthesis of inositol pyrophosphates by inositol hexakisphosphate kinase (IP6K) has been identified as a potential therapeutic strategy for obesity and related diseases. We have developed a novel and potent IP6K inhibitor 20 (UNC7467) (IC50 values: IP6K1 8.9 nM; IP6K2 4.9 nM; IP6K3 1320 nM). Inositol phosphate profiling of the HCT116 colon cancer cell line demonstrates that 20 reduced levels of inositol pyrophosphates by 66-81%, without significantly perturbing levels of other inositol phosphates. Furthermore, intraperitoneal injection of 20 in diet-induced obese mice improved glycemic profiles, ameliorated hepatic steatosis, and reduced weight gain without altering food intake. Thus, inhibitor 20 can be used as an in vivo probe for IP6K-related research. Moreover, it may have therapeutic relevance in treating obesity and related diseases.