CL 316,243 (disodium salt) |
| Katalog-Nr.GC43276 |
Ein murin-selektiver β3-Adrenozeptor-Agonist
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 151126-84-0,138908-40-4
Sample solution is provided at 25 µL, 10mM.
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.
| Cell experiment [1]: | |
Cell lines | White and brown preadipocytes |
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. |
Reaction Conditions | CL 316,243 (disodium salt) ( 10 nM ); 7 days |
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]: | |
Animal models | Insulin resistance model |
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 | |
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. |
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. | |
| Cas No. | 151126-84-0,138908-40-4 | SDF | |
| Chemical Name | 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+] | ||
| Formula | C20H18ClNO7•2Na | M.Wt | 465.8 |
| Löslichkeit | 0.5mg/ml in DMSO, PBS (pH 7.2): 3 mg/ml | Storage | Desiccate at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
-
Related Biological Data
NIR-II fluorescence imaging and quantitative analysis of the ROI in normal mice and CL-treated mice. CL-treated mice were injected 20 μg CL316,243 (CL) intraperitoneally for 7 days.(b,c) ROI analysis of the iBAT-to-background and iBAT-to-liver ratios of normal mice and CL-treated mice
CL316,243(CL)-treated mice were kept at 22 °C and injected 20 μg CL316,243 (GLPBIO) intraperitoneally for 7 days.
ACS Applied Materials & Interfaces (2023). PMID: 37289581 IF: 10.3831 -
Related Biological Data
Geniposide negatively regulates UCP1 via suppressing transcription activity of UCP1. (A) Representative images of GFP intensity in HEK293T cells treated with DMSO, CL316243, or geniposide.(B) Relative level of GFP intensity in HEK293T cells treated with DMSO, CL316243, or geniposide (10 and 20 mg/ml) .
Relative level of GFP intensity in HEK293T cells treated with DMSO, CL316243(GlpBio), or geniposide (10 and 20 mg/ml) .
Toxicology (2021): 153014. PMID: 34718029 IF: 4.221 -
Related Biological Data
Letmd1 is critical for thermogenesis in BAT. (B-C) Relative mRNA expression of Ucp1 and Letmd1 in BAT following cold exposure or CL316,243 for 7 d or 10 d, b-actin was used as the internal control. WT mice following CL316,243 were kept at 22 ℃.
For NE and CL316,243(GlpBio) treatment,differentiated brown adipocytes were treated with 10 mM CL316,243 or 1 mM NE for 6 h.
Biochimie 201 (2022): 100-115. PMID: 35817133 IF: 3.9003
Average Rating: 5 (Based on Reviews and 20 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *