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CL 316,243 (disodium salt)

目录号 : GC43276

一种仅对小鼠有效的β3肾上腺素受体激动剂。

CL 316,243 (disodium salt) Chemical Structure

Cas No.:151126-84-0,138908-40-4

规格 价格 库存 购买数量
500μg
¥416.00
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1mg
¥715.00
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5mg
¥1,880.00
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10mg
¥2,911.00
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Sample solution is provided at 25 µL, 10mM.

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Quality Control & SDS

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实验参考方法

In vitro experiment [1]:

Samples

LES smooth muscles

Preparation method

The solubility of this compound in sterile water is 100 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.

Reacting condition

0.01 ~ 300 μM

Applications

CL 316243 concentration-dependently decreased the basal tension of the LES smooth muscle, with an ECmax value of 1 × 10-4 M. At corresponding ECmax values, the smooth muscle relaxation induced by CL 316243 was significantly longer than that triggered by isoproterenol. The smooth muscle relaxation in the isoproterenol group began to recover within 5 mins but it cost 1 hr in the case of CL 316243.

Animal experiment [2]:

Animal models

Nonobese and nondiabetic Sprague-Dawley rats

Dosage form

1 mg/kg/day; s.c.; for 10 ~ 12 days

Applications

After 7 days of treatment, CL 316243 significantly increased food consumption, resting metabolic rates, as well as body core temperatures in rats. Besides, CL 316243 decreased the respiratory quotient by 14%. On day 11, an oral glucose load (2 g/kg) did not alter plasma glucose and insulin excursions. In addition, CL 316243 reduced abdominal and epididymal white fat pad weights, but doubled interscapular brown adipose tissue weight at the same time.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Sarma DN, Banwait K, Basak A, DiMarino AJ, Rattan S. Inhibitory effect of beta3-adrenoceptor agonist in lower esophageal sphincter smooth muscle: in vitro studies. J Pharmacol Exp Ther. 2003 Jan;304(1):48-55.

[2]. de Souza CJ, Hirshman MF, Horton ES. CL-316,243, a beta3-specific adrenoceptor agonist, enhances insulin-stimulated glucose disposal in nonobese rats. Diabetes. 1997 Aug;46(8):1257-63.

产品描述

EC50: (3.0±0.3) X 10-8 M for β3 adrenoceptor [1].

Benzodioxole-containing phenethanolamine CL-316,243 is a murine-selective β3 adrenoceptor agonist which can correct obesity and elevated blood glucose in diabetic rodents, which offers an exciting possibility for the treatment of non-insulin-dependent diabetes as well as obesity without undesired β-mediated side effects [3]. β3 adrenoceptor is located mainly in adipose tissue and is involved in the regulation of lipolysis and thermogenesis.

In vitro: The compound was a potent stimulant of rat adipocyte lipolysis (β3 effect, EC50 = (3.0±0.3) X 10-8 M), had no effect on the rate of contraction of guinea pig atria (β1 effect, EC50 > 10-4 M), and had only a very limited ability to inhibit insulin-stimulated [14C] glucose incorporation into glycogen in isolated rat soleus muacle (β2 effect, IC50 = (3.0±1.0) X 10-5 M) [1].

In vivo: In rat, CL-316,243 treatment resulted in increased growth rates and significant changes in food consumption at the end of the 10-day treatment period. CL-316,243 treatment increased insulin responsiveness and sensitivity in non-insulin-resistant rodent species. The CL-316,243 induced increases in whole-body glucose disposal were due entirely to increases in adipose tissue glucose uptake, while muscle glucose uptake remained unaltered [2].

Clinical trial: So far, no clinical study has been conducted.

β3肾上腺素受体的EC50为(3.0±0.3) X 10-8 M [1]。

含苯并二氧杂环的苯乙醇胺CL-316,243是一种仅对小鼠选择性作用的β3肾上腺素受体激动剂,可以纠正肥胖和糖尿病啮齿动物中升高的血糖水平。这为治疗非胰岛素依赖型糖尿病以及肥胖提供了一个令人兴奋的可能性,而不会产生不良的β介导副作用[3]。 β3 肾上腺素受体主要位于脂肪组织中,并参与调节脂解和产生热能。

在体外实验中,这种化合物是大鼠脂肪细胞脂解的强效刺激剂(β3效应,EC50 = (3.0±0.3) X 10-8 M),对豚鼠心房收缩速率没有影响(β1效应,EC50 > 10-4 M),并且只有非常有限的能力抑制孤立大鼠比目鱼肌内胰岛素刺激下[14C]葡萄糖转化为糖原的作用(β2效应,IC50 = (3.0±1.0) X 10-5 M)[1]。

在体内:在大鼠中,CL-316,243治疗导致增加生长速度和食物消耗的显著变化,在10天的治疗期结束时。 CL-316,243治疗增加了非胰岛素抵抗啮齿动物种类的胰岛素反应性和敏感性。 CL-316,243诱导的全身葡萄糖处理增加完全是由于脂肪组织葡萄糖摄取量的增加,而肌肉葡萄糖摄取量保持不变[2]。

临床试验:目前还没有进行任何临床研究。

Chemical Properties

Cas No. 151126-84-0,138908-40-4 SDF
化学名 5-[(2R)-2-[[(2R)-2-(3-chlorophenyl)-2-hydroxyethyl]amino]propyl]-1,3-benzodioxole-2,2-dicarboxylic acid, disodium salt
Canonical SMILES ClC1=CC=CC([C@@H](O)CN[C@H](C)CC2=CC=C(OC(C([O-])=O)(C([O-])=O)O3)C3=C2)=C1.[Na+].[Na+]
分子式 C20H18ClNO7•2Na 分子量 465.8
溶解度 0.5mg/ml in DMSO, PBS (pH 7.2): 3 mg/ml 储存条件 Desiccate 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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1 mM 2.1468 mL 10.7342 mL 21.4684 mL
5 mM 0.4294 mL 2.1468 mL 4.2937 mL
10 mM 0.2147 mL 1.0734 mL 2.1468 mL
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Research Update

18F-FDG PET/CT monitoring of β3 agonist-stimulated brown adipocyte recruitment in white adipose tissue

J Nucl Med 2015 Jan;56(1):153-8.PMID:25525187DOI:10.2967/jnumed.114.147603.

There is rising interest in recruitment of brown adipocytes into white adipose tissue (WAT) as a means to augment energy expenditure for weight reduction. We thus investigated the potential of (18)F-FDG uptake as an imaging biomarker that can monitor the process of WAT browning. Methods: C57BL/6 mice were treated daily with the β3 agonist CL316,243 (5-[(2R)-2-[[(2R)-2-(3-chlorophenyl)-2-hydroxyethyl]amino]propyl]-1,3-benzodioxole-2,2-dicarboxylic acid disodium salt), whereas controls received saline. (18)F-FDG small-animal PET/CT was serially performed at 1 h after CL316,243 injection. After sacrifice, interscapular brown adipose tissue (BAT) and WAT depots were extracted, weighed, and measured for (18)F-FDG uptake. Tissues underwent immunostaining, and UCP1 content was quantified by Western blotting. Results: PET/CT showed low (18)F-FDG uptake in both BAT and inguinal WAT at baseline. BAT uptake was substantially increased by a single stimulation with CL316,243. Uptake in inguinal WAT was only modestly elevated by the first stimulation uptake but gradually increased to BAT level by prolonged stimulation. Ex vivo measurements recapitulated the PET findings, and measured (18)F-FDG uptake in other WAT depots was similar to inguinal WAT. WAT browning by prolonged stimulation was confirmed by a substantial increase in uncoupling protein 1 (UCP1), cytochrome-c oxidase 4 (COX4), and PR domain containing 16 (PRDM16) staining as markers of brown adipocytes. UCP1 content, which served as a measure for extent of browning, was low in baseline inguinal WAT but linearly increased over 10 d of CL316,243 injection. Finally, image-based and ex vivo-measured (18)F-FDG uptake in inguinal WAT correlated well with UCP1 content. Conclusion: (18)F-FDG PET/CT has the capacity to monitor brown adipocyte recruitment into WAT depots in vivo and may thus be useful for screening the efficacy of strategies to promote WAT browning.