1. GPCR/G Protein Neuronal Signaling
  2. Adrenergic Receptor
  3. CL 316243

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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CAS No. : 138908-40-4

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Based on 24 publication(s) in Google Scholar

Other Forms of CL 316243:

Top Publications Citing Use of Products

    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 Aug 11;16(1):7414.  [Abstract]

    WT mice were injected with CL316,243 (1 mg/kg) intraperitoneally twice, once per 12 h.

    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)

    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).

    CL 316243 purchased from MedChemExpress. Usage Cited in: Food Res Int. 2023 Jan:163:112198.

    CL316243 increases p-AMPKα/AMPKα ratio and UCP1 protein expression in LLE-treated cells.

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    Description

    CL316243 is a highly potent selective β3-adrenoceptor agonist with a EC50 of 3 nM, but is an extremely poor to β1/2- receptors[1].CL316243 is a effective stimulant of adipocyte lipolysis and increases brown adipose tissue thermogenesis and metabolic rate[2]. CL316243 has the potential for the treatment obesity, diabetes and urge urinary incontinence[3].

    IC50 & Target

    β adrenergic receptor

     

    Cellular Effect
    Cell Line Type Value Description References
    CHO EC50
    111 3
    Compound: CL-316243
    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
    [PMID: 11277513]
    CHO EC50
    262 3
    Compound: CL-316243
    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
    [PMID: 11277513]
    CHO EC50
    1.15 3
    Compound: CL-316243
    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
    [PMID: 11277513]
    CHO EC50
    1.15 3
    Compound: CL-316243
    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
    [PMID: 11277513]
    CHO EC50
    111 3
    Compound: CL-316243
    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
    [PMID: 11277513]
    CHO EC50
    262 3
    Compound: CL-316243
    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
    [PMID: 11277513]
    CHO EC50
    262 3
    Compound: CL-316243
    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
    [PMID: 11277513]
    In Vitro

    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.

    In Vivo

    CL316243 disodium (subcutaneously injection; 0.1 mg/kg/day; once a day; 1 weeks) elevates the mRNA and protein expression levels of UCP1 in BAT, irrespective of diet[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    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]
    Dosage: 0.1 mg/kg/day
    Administration: once a day; 1 weeks
    Result: Exhibited a premium effect of obesity in mice.
    Masse moléculaire

    465.79

    Formule

    C20H18ClNNa2O7

    CAS No.
    Appearance

    Solid

    Color

    White to yellow

    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]

    Livraison

    Room temperature in continental US; may vary elsewhere.

    Stockage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

    Solvant et solubilité
    In Vitro: 

    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)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    View the 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.

    * 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.

    • Calculateur de molarité

    • Calculateur de dilution

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    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.

    • Protocol 1

      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

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    Pureté et documentation

    Purity: 99.98%

    Références

    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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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Nom du produit:
    CL 316243
    Cat. No.:
    HY-116771A
    Quantité:
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