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CL-316243 disodium

Alias: CL316243 CL 316243 CL-316243
Cat No.:V18448 Purity: ≥98%
CL-316243 disodium (CL316243) is a novel and potent β3-adrenoceptor agonistwith the potential for the treatment obesity, diabetes and urge urinary incontinence.
CL-316243 disodium
CL-316243 disodium Chemical Structure CAS No.: 138908-40-4
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
50mg
Other Sizes
Official Supplier of:
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Product Description

CL-316243 disodium (CL316243) is a novel and potent β3-adrenoceptor agonist with the potential for the treatment obesity, diabetes and urge urinary incontinence. It activates β3-adrenoceptor with a EC50 of 3 nM.

Biological Activity I Assay Protocols (From Reference)
Targets

EC50: 3 nM (β3-adrenoceptor)[1]

ln Vitro
Clenidine 316243 has IC50 values of 0.6 μM and 1 μM, respectively, against the rat heart and soleus muscle[1]. Based on concentration-dependent inhibition, CL 316243 prevents 50% of the maximal response from spontaneous contractions in isolated rat detrusor muscle strips at an average dose of 2.65 nM [3].
ln Vivo
Unaffected by food, CL316243 disodium (subcutaneous injection; 0.1 mg/kg/d; once daily; 1 week) raises BAT's levels of UCP1 mRNA and protein expression [2].
Animal Protocol
Animal/Disease Models: 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]
Doses: 0.1 mg/kg/day
Route of Administration: one time/day; 1 weeks
Experimental Results: demonstrated a premium effect of obesity in mice.
References

[1]. 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]. Impaired adrenergic agonist-dependent beige adipocyte induction in obese mice.J Vet Med Sci. 2019 Jun 6;81(6):799-807.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C20H18CLNNA2O7
Molecular Weight
465.7935
Exact Mass
465.057
CAS #
138908-40-4
PubChem CID
5312115
Appearance
White to yellow solid powder
Boiling Point
689.5ºC at 760 mmHg
Flash Point
370.8ºC
Vapour Pressure
5.86E-20mmHg at 25°C
Hydrogen Bond Donor Count
2
Hydrogen Bond Acceptor Count
8
Rotatable Bond Count
6
Heavy Atom Count
31
Complexity
578
Defined Atom Stereocenter Count
2
SMILES
C[C@H](CC1=CC2=C(C=C1)OC(O2)(C(=O)[O-])C(=O)[O-])NC[C@@H](C3=CC(=CC=C3)Cl)O.[Na+].[Na+]
InChi Key
FUZBPOHHSBDTJQ-CFOQQKEYSA-L
InChi Code
InChI=1S/C20H20ClNO7.2Na/c1-11(22-10-15(23)13-3-2-4-14(21)9-13)7-12-5-6-16-17(8-12)29-20(28-16,18(24)25)19(26)27;;/h2-6,8-9,11,15,22-23H,7,10H2,1H3,(H,24,25)(H,26,27);;/q;2*+1/p-2/t11-,15+;;/m1../s1
Chemical Name
disodium;5-[(2R)-2-[[(2R)-2-(3-chlorophenyl)-2-hydroxyethyl]amino]propyl]-1,3-benzodioxole-2,2-dicarboxylate
Synonyms
CL316243 CL 316243 CL-316243
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
H2O : ~20 mg/mL (~42.94 mM)
Solubility (In Vivo)
Solubility in Formulation 1: 100 mg/mL (214.69 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication (<60°C).

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 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

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

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