CL 316243
目录号 : GC68879CL 316,243 (disodium salt) 是一种高效的 β3 肾上腺素受体选择性激动剂，EC50 为 3 nM。它是一种有效的脂肪细胞脂解刺激剂，可增加棕色脂肪组织的产热和代谢率，具有治疗肥胖症、糖尿病和急迫性尿失禁的潜力。
Cas No.:138908-40-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
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Cell lines |
White and brown preadipocytes |
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Preparation Method |
At the third day of culture CL 316,243 (disodium salt)（10 nM） or isoproterenol （1mM） was added to the culture medium . Cells were harvested at day 10 and analysed. |
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Reaction Conditions |
CL 316,243 (disodium salt) ( 10 nM ); 7 days |
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Applications |
In both types of adipocyte culture lipid accumulation was first detectable at day 6 (around confluence) . Until day 10 an almost linear increase in lipid content occurred. overall lipid accumulation was about 30% higher in white adipocyte cultures than in brown ones. |
| Animal experiment [2]: | |
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Animal models |
Insulin resistance model |
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Preparation Method |
Nine to ten week old male WT and MKR mice were injected intraperitoneally with CL-316,243 (1 mg/kg /day) or with an equivalent volume of vehicle (sterile water and phosphate buffered saline) for three weeks. |
| CL 316,243 (disodium salt) ( 1 mg/kg ; ip ), 3 weeks | |
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Applications |
After treatment with CL-316,243, the circulating glucose and insulin concentrations in the MKR mice improved, an increase in the expression of peroxisomal fatty acid oxidation genes was observed in addition to a decrease in the expression of retinaldehyde dehydrogenases. |
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References: [1]. Klaus S, Seivert A, Boeuf S. Effect of the beta(3)-adrenergic agonist Cl316,243 on functional differentiation of white and brown adipocytes in primary cell culture. Biochim Biophys Acta. 2001 May 28;1539(1-2):85-92. |
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CL 316,243 (disodium salt)is a highly potent β3-adrenoceptor selective agonist with an EC50 of 3 nM. It is a potent adipocyte lipolysis stimulator that increases thermogenesis and metabolic rate of brown adipose tissue and has the potential to treat obesity, diabetes, and urge urinary incontinence[1].
CL 316,243 (disodium salt)(10 nM, 10 days) treated with white and brown adipocytes, lipid accumulation was first detected on day 6 (confluence) and lipid content increased almost linearly until day 10. Overall lipid accumulation in white adipocyte cultures was approximately 30% higher than in brown adipocyte cultures[2].CL 316,243 (disodium salt) inhibits spontaneously contracting, isolated rat detrusor strips in a concentration dependent manner with a mean concentration inhibiting 50% of maximal response of 2.65 nM[3].
Following treatment with CL 316,243 (disodium salt) (1 mg/kg; i.p.; 3 weeks), expression of peroxisomal FA oxidases ACAA1 and HSD17b4 was increased in adipose tissue of MKR mice[4].CL 316,243 (disodium salt) (1 mg/kg; SC; 2 weeks) reduced serum levels of glucose, insulin, triglycerides, free fatty acids, and tumor necrosis factor-α (TNF-α), and increased adiponectin[5]. CL 316,243 (disodium salt) (0.3 and 1 mg/kg; 2 weeks; subcutaneous injection) dose-dependently reduced the weight/volume of the inguinal fat pad [6].
[1].Bloom JD, Dutia MD, Johnson BD, Wissner A, Burns MG, Largis EE, Dolan JA, Claus TH. Disodium (R,R)-5-[2-[[2-(3-chlorophenyl)-2-hydroxyethyl]-amino] propyl]-1,3-benzodioxole-2,2-dicarboxylate (CL 316,243). A potent beta-adrenergic agonist virtually specific for beta 3 receptors. A promising antidiabetic and antiobesity agent. J Med Chem. 1992 Aug 7;35(16):3081-4.
[2]. Klaus S, Seivert A, Boeuf S. Effect of the beta(3)-adrenergic agonist Cl316,243 on functional differentiation of white and brown adipocytes in primary cell culture. Biochim Biophys Acta. 2001 May 28;1539(1-2):85-92.
[3]Woods M, Carson N, Norton NW, Sheldon JH, Argentieri TM. Efficacy of the beta3-adrenergic receptor agonist CL-316243 on experimental bladder hyperreflexia and detrusor instability in the rat. J Urol. 2001 Sep;166(3):1142-7.
[4]. Kumar A, Shiloach J, Betenbaugh MJ, Gallagher EJ. The beta-3 adrenergic agonist (CL-316,243) restores the expression of down-regulated fatty acid oxidation genes in type 2 diabetic mice. Nutr Metab (Lond). 2015 Mar 8;12:8.
[5]. Shin W, Okamatsu-Ogura Y, Matsuoka S, Tsubota A, Kimura K. Impaired adrenergic agonist-dependent beige adipocyte induction in obese mice. J Vet Med Sci. 2019 Jun 6;81(6):799-807.
[6]Danysz W, Han Y, Li F, Nicoll J, Buch P, Hengl T, Ruitenberg M, Parsons C. Browning of white adipose tissue induced by the ß3 agonist CL-316,243 after local and systemic treatment - PK-PD relationship. Biochim Biophys Acta Mol Basis Dis. 2018 Sep;1864(9 Pt B):2972-2982.
CL 316,243 (disodium salt) 是一种高效的 β3 肾上腺素受体选择性激动剂，EC50 为 3 nM。它是一种有效的脂肪细胞脂解刺激剂，可增加棕色脂肪组织的产热和代谢率，具有治疗肥胖症、糖尿病和急迫性尿失禁的潜力[1]。
CL 316,243 (disodium salt) ( 10 nM, 10 days )处理白色和棕色脂肪细胞，在第 6 天（汇合）首次检测到脂质积累。直到第 10 天，脂质含量几乎呈线性增加。白色脂肪细胞培养物中的总体脂质积累比棕色脂肪细胞培养物中高出约 30%[2]。CL 316243 以浓度依赖性方式抑制自发收缩的孤立大鼠逼尿肌条带，平均浓度抑制 2.65 nM 最大反应的 50% [3]。
CL 316,243 (disodium salt) (1mg/kg；ip；3周)治疗后，MKR小鼠脂肪组织中过氧化物酶体脂肪酸氧化酶ACAA1和HSD17b4的表达增加[4]。CL 316,243 (disodium salt)（1mg/kg；SC；2周）降低血清葡萄糖、胰岛素、甘油三酯、游离脂肪酸和肿瘤坏死因子-α（TNF-α）的水平，并升高脂联素[5]。CL 316,243 (disodium salt) ( 0.3 and 1mg/kg ；2周；SC) 剂量依赖性减少腹股沟脂肪垫重量/体积[6]。
| Cas No. | 138908-40-4 | SDF | Download SDF |
| 分子式 | C20H18ClNNa2O7 | 分子量 | 465.79 |
| 溶解度 | H2O : 20 mg/mL (42.94 mM; Need ultrasonic) | 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 | 2.1469 mL | 10.7345 mL | 21.4689 mL |
| 5 mM | 0.4294 mL | 2.1469 mL | 4.2938 mL |
| 10 mM | 0.2147 mL | 1.0734 mL | 2.1469 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。