CL 316243
Based on 24 publication(s) in Google Scholar
CL316243 is a highly potent selective β3-adrenoceptor agonist with a EC50 of 3 nM, but is an extremely poor to β1/2- receptors.CL316243 is a effective stimulant of adipocyte lipolysis and increases brown adipose tissue thermogenesis and metabolic rate. CL316243 has the potential for the treatment obesity, diabetes and urge urinary incontinence.
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- Purity: 99.98%
- CAS No.: 138908-40-4
- 화학식: C20H18ClNNa2O7
- 분자량:465.79
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보관:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Publications Citing Use of MedChemExpress (MCE) CL 316243
More- Cell Metab. 2024 Dec 21:S1550-4131(24)00456-X. [Abstract]
- Cell Stem Cell. 2026 Apr 2;33(4):605-621.e6. [Abstract]
- Nat Commun. 2025 Aug 11;16(1):7414. [Abstract]
- Nat Commun. 2025 Jul 4;16(1):6151. [Abstract]
- J Adv Res. 2026 Feb 12:S2090-1232(26)00137-2. [Abstract]
- J Adv Res. 2025 Nov 22:S2090-1232(25)00935-X. [Abstract]
- Redox Biol. 2024 Feb:69:103013. [Abstract]
- Phytomedicine. 2025 Oct 11:148:157400. [Abstract]
- Phytomedicine. 2023 Jan:109:154563. [Abstract]
- Food Res Int. 2023 Jan:163:112198. [Abstract]
- Diabetes. 2023 May 1;72(5):611-626. [Abstract]
- Mol Metab. 2024 Oct 29:102053. [Abstract]
- Mol Metab. 2022 Feb:56:101423. [Abstract]
- Biochem Pharmacol. 2025 Apr 10:237:116929. [Abstract]
- Am J Chin Med. 2025;53(3):863-888. [Abstract]
- iScience. 2025 Jan 19;28(2):111833. [Abstract]
- J Lipid Res. 2024 Aug 16:100623. [Abstract]
- Metabolites. 2025 Dec 23;16(1):12.
- Integr Zool. 2025 Dec 8. [Abstract]
- Cell Signal. 2024 Aug 7:111340. [Abstract]
- Cell Signal. 2023 Nov:111:110875. [Abstract]
- J Anim Sci. 2026 Jan 8:104:skag016. [Abstract]
- bioRxiv. 2025 Sep 10.
- bioRxiv. 2024 August 25.
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All Adrenergic Receptor Isoforms
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Biological Activity
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β adrenergic receptor |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
1.15 μM
Compound: CL-316243
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Agonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptor
Agonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptor
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[PMID: 11277513] |
| CHO | EC50 |
111 μM
Compound: CL-316243
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Agonistic activity as cAMP accumulation in CHO cells expressing human beta-1-adrenergic receptor
Agonistic activity as cAMP accumulation in CHO cells expressing human beta-1-adrenergic receptor
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[PMID: 11277513] |
| CHO | EC50 |
262 μM
Compound: CL-316243
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Agonistic activity was assessed by measurement of cAMP accumulation levels in CHO cells expressing human beta-2-adrenergic receptor
Agonistic activity was assessed by measurement of cAMP accumulation levels in CHO cells expressing human beta-2-adrenergic receptor
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[PMID: 11277513] |
CL 316243 displays binding affinities with IC50 values of 0.6 μM and 1 μM for rat heart and rat soleus muscle respectively[1]. CL 316243 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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6J mice fed with high-fat diets (HFD; 45%-kcal fat) or a control diet (ND; 10%-kcal fat) for 14 weeks[2]
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Dosage:0.1 mg/kg/day
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Administration:once a day; 1 weeks
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Result:Exhibited a premium effect of obesity in mice.
Chemical Information
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CAS No. 138908-40-4
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Appearance Solid
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분자량 465.79
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화학식 C20H18ClNNa2O7
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Color White to yellow
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SMILES
O=C(C1(C(O[Na])=O)OC2=CC=C(C[C@H](NC[C@@H](C3=CC=CC(Cl)=C3)O)C)C=C2O1)O[Na]
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
Publications (24)
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Journal Impact Factor
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Most Recent
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Cell Metab
2024 Dec 21:S1550-4131(24)00456-X. PMID: 39729998 -
Cell Stem Cell
Auditory activity sustains adult neurogenesis and cognition through the locus coeruleus-norepinephrine system. [Abstract]2026 Apr 2;33(4):605-621.e6. PMID: 41861826 -
Nat Commun
Adipocyte RNA-binding protein CELF1 promotes beiging of white fat through stabilizing Dio2 mRNA. [Abstract]2025 Aug 11;16(1):7414. PMID: 40789858
CL 316243 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Aug 11;16(1):7414. [Abstract]
WT mice were injected with CL316,243 (1 mg/kg) intraperitoneally twice, once per 12 h.
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Nat Commun
Adipocyte CLDN5 promotes thermogenesis and energy expenditure through regulation of IL10 expression. [Abstract]2025 Jul 4;16(1):6151. PMID: 40610440
CL 316243 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Jul 4;16(1):6151. [Abstract]
Treatment with β3-selective adrenergic agonist CL-316,243 ( 1 mg/kg/day) for 10 days also resulted in a significant increase in the expression of CLDN5 as well as UCP1 in both BAT and iWAT.
CL 316243 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Jul 4;16(1):6151. [Abstract]
Western blot analysis (t, n = 3) of PGC1α and UCP1 in Cldn5flox/flox and Cldn5flox/flox; Fabp4-Cre mice treated with saline/CL-316,243 (1 mg/kg)
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J Adv Res
A novel GIPR/GLP-1R dual agonist improves systemic metabolism through differentially regulating inflammation and lipid metabolism in obesity. [Abstract]2026 Feb 12:S2090-1232(26)00137-2. PMID: 41690462 -
J Adv Res
ANXA1 improves mitochondrial homeostasis through uncoupling protein 1 in diabetic nephropathy. [Abstract]2025 Nov 22:S2090-1232(25)00935-X. PMID: 41275961
CL 316243 purchased from MedChemExpress. Usage Cited in: J Adv Res. 2025 Nov 22:S2090-1232(25)00935-X. [Abstract]
Relative mRNA and protein levels of MFF and DRP1 among 3 groups. CL316243 (3mg/kg)/vehicle (methylcellulose) for 4 weeks (every 9:00 a.m., gavage).
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Redox Biol
Endothelial TET2 regulates the white adipose browning and metabolism via fatty acid oxidation in obesity. [Abstract]2024 Feb:69:103013. PMID: 38168657 -
Phytomedicine
Perillyl alcohol ameliorates high-fat diet-induced obesity in mice by modulating gut microbiota and activating IRF4-mediated brown fat thermogenesis. [Abstract]2025 Oct 11:148:157400. PMID: 41138577 -
Phytomedicine
Curcumin treatment suppresses cachexia-associated adipose wasting in mice by blocking the cAMP/PKA/CREB signaling pathway. [Abstract]2023 Jan:109:154563. PMID: 36610148 -
Food Res Int
Quercetin 3-O-glucuronide-rich lotus leaf extract promotes a Brown-fat-phenotype in C3H10T1/2 mesenchymal stem cells. [Abstract]2023 Jan:163:112198. PMID: 36596137
CL 316243 purchased from MedChemExpress. Usage Cited in: Food Res Int. 2023 Jan:163:112198. [Abstract]
CL316243 increases p-AMPKα/AMPKα ratio and UCP1 protein expression in LLE-treated cells.
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Diabetes
Metrnl alleviates lipid accumulation by modulating mitochondrial homeostasis in diabetic nephropathy. [Abstract]2023 May 1;72(5):611-626. PMID: 36812572 -
Mol Metab
RNA-binding protein YBX3 promotes PPARγ-SLC3A2 mediated BCAA metabolism fueling brown adipogenesis and thermogenesis. [Abstract]2024 Oct 29:102053. PMID: 39481849 -
Mol Metab
Ablation of ORMDL3 impairs adipose tissue thermogenesis and insulin sensitivity by increasing ceramide generation. [Abstract]2022 Feb:56:101423. PMID: 34954108 -
Biochem Pharmacol
UCP1 prevents the formation of thoracic aortic aneurysms and dissection by inhibiting the TLR4/NLRP3/IL-1β signaling pathway and VSMC phenotype switching in mice. [Abstract]2025 Apr 10:237:116929. PMID: 40216265 -
Am J Chin Med
Puerarin Alleviates Alcoholic Liver Disease via Suppressing Lipolysis Induced by Sympathetic Outflow. [Abstract]2025;53(3):863-888. PMID: 40374377 -
iScience
2025 Jan 19;28(2):111833. PMID: 39949963 -
J Lipid Res
Natriuretic peptide receptor-C perturbs mitochondrial respiration in white adipose tissue. [Abstract]2024 Aug 16:100623. PMID: 39154732 -
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Integr Zool
Blubber Thickening Driven by UCP1 Inactivation: Insights from a Cetacean-Like Transgenic Mouse Model. [Abstract]2025 Dec 8. PMID: 41358834 -
Cell Signal
Ndufa8 promotes white fat Browning by improving mitochondrial respiratory chain complex I function to ameliorate obesity by in vitro and in vivo. [Abstract]2024 Aug 7:111340. PMID: 39127135 -
Cell Signal
HDAC1 inhibits beige adipocyte-mediated thermogenesis through histone crotonylation of Pgc1a/Ucp1. [Abstract]2023 Nov:111:110875. PMID: 37640195 -
J Anim Sci
From selection signatures in cattle to functional validation in mice: HSPA12B negatively regulates adipose browning and thermogenesis. [Abstract]2026 Jan 8:104:skag016. PMID: 41615431 -
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용액&용해도
DMSO : 17.5 mg/mL (37.57 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 4.55 mg/mL (9.77 mM; ultrasonic and warming and adjust pH to 12 with 1 M NaOH and heat to 60°C)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (214.69 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
순도&문서
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Data Sheet (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Bloom JD, et al. 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. [Content Brief]
[2]. Shin W, et al. Impaired adrenergic agonist-dependent beige adipocyte induction in obese mice.J Vet Med Sci. 2019 Jun 6;81(6):799-807. [Content Brief]
[3]. Woods M, et al. 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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.1469 mL | 10.7345 mL | 21.4689 mL | 53.6723 mL |
| 5 mM | 0.4294 mL | 2.1469 mL | 4.2938 mL | 10.7345 mL | |
| DMSO | 10 mM | 0.2147 mL | 1.0734 mL | 2.1469 mL | 5.3672 mL |
| 15 mM | 0.1431 mL | 0.7156 mL | 1.4313 mL | 3.5782 mL | |
| 20 mM | 0.1073 mL | 0.5367 mL | 1.0734 mL | 2.6836 mL | |
| 25 mM | 0.0859 mL | 0.4294 mL | 0.8588 mL | 2.1469 mL | |
| 30 mM | 0.0716 mL | 0.3578 mL | 0.7156 mL | 1.7891 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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