| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg | |||
| Other Sizes |
| Targets |
EC50: 3 nM (β3-adrenoceptor)[1]
CL-316243 targets the beta-3 adrenergic receptor (β3-AR), which is predominantly expressed in white and brown adipose tissue, the gallbladder, and the urinary bladder. Activation of this receptor plays a crucial role in regulating energy expenditure and lipid metabolism. The compound exhibits remarkable selectivity for β3-AR over β1 and β2 subtypes, which is crucial for minimizing off-target effects such as cardiovascular stimulation (β1) and muscle tremors (β2). It also shows activity in rat heart (predominantly β1-AR) with an IC50 of 0.6 μM and rat soleus muscle (predominantly β2-AR) with an IC50 of 1 μM. |
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| 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].
In vitro, CL-316243 is a potent agonist of the β3-adrenoceptor with an EC50 of 3 nM. In human β3-AR cAMP accumulation assays, it shows an EC50 of 1.15 μM, while its EC50 for human β1-AR is 111 μM, demonstrating its high selectivity. It has been used in studies of rat epididymal adipocytes at 1 μM to investigate effects on PI(3,4,5)P3 production and cAMP accumulation. The compound is also effective in isolated rat and human detrusor strip assays (pD2=8.61). |
| 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].
In vivo, CL-316243 possesses anti-obesity and anti-diabetic effects due to increasing brown adipose tissue thermogenesis and metabolic rate. It may be useful for treating obesity as well as non-insulin-dependent diabetes mellitus in obese persons, without causing excessive side effects. It is orally bioavailable with well-characterized in vivo pharmacokinetics. The daily oral dose for rats was 1 mg/kg body weight for 4 weeks. It is used in BAT thermogenesis models at 0.1 mg/kg/day via subcutaneous administration. |
| Enzyme Assay |
CL-316243 is evaluated in cell-free receptor binding assays using membrane preparations expressing β3-adrenoceptors. Radioligand binding displacement assays are performed to determine its affinity and selectivity. The compound's potency is demonstrated by its low nanomolar effective concentration for β3-AR activation. cAMP accumulation assays using purified enzymes or cell membranes can also be employed to quantify its agonistic activity.
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| Cell Assay |
CL-316243 is assessed in cell-based assays using rat epididymal adipocytes. [32P]orthophosphate-labeled adipocytes are treated with or without CL-316243 (1 μM) for 1 minute, and the radioactivity of PI(3,4,5)P3 separated by TLC and the accumulation of cAMP are determined. The compound is also used in studies with human embryonic kidney (HEK) cells expressing β3-adrenoceptors to measure cAMP accumulation.
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| 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. CL-316243 is administered orally or subcutaneously in animal models. In rats, the daily dose for was 1 mg/kg body weight for 4 weeks via oral administration. In BAT thermogenesis models, it is used at 0.1 mg/kg/day via subcutaneous injection. Efficacy is assessed by measuring metabolic rate, body weight, adipose tissue thermogenesis, and glucose tolerance. |
| ADME/Pharmacokinetics |
CL-316243 is orally bioavailable with well-characterized in vivo pharmacokinetics. It is formulated for in vivo use, often as a solution in saline or other suitable vehicles. The compound has a molecular weight of 465.8 g/mol and a CAS number of 138908-40-4. It is typically stored as a desiccated powder at -20°C.
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| Toxicity/Toxicokinetics |
No detailed toxicity data is available for CL-316243 beyond its known pharmacological profile. It is a research compound and is not intended for human therapeutic use. Its high selectivity for β3-AR suggests a favorable safety profile with minimal cardiovascular or muscle-related side effects.
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| References |
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| Additional Infomation |
CL-316243 is also known as Disodium (R,R)-5-[2-[[2-(3-chlorophenyl)-2-hydroxyethyl]-amino] propyl]-1,3-benzodioxole-2,2-dicarboxylate. It is a promising antidiabetic and antiobesity agent. The compound pairs definitively with selective antagonists SR 59230A and L-748337. It is not approved for clinical use.
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| Molecular Formula |
C20H18CLNNA2O7
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|---|---|
| Molecular Weight |
465.7935
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| Exact Mass |
465.057
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| CAS # |
138908-40-4
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| PubChem CID |
5312115
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| Appearance |
White to yellow solid powder
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| Boiling Point |
689.5ºC at 760 mmHg
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| Flash Point |
370.8ºC
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| Vapour Pressure |
5.86E-20mmHg at 25°C
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
31
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| Complexity |
578
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| Defined Atom Stereocenter Count |
2
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| 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+]
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| InChi Key |
FUZBPOHHSBDTJQ-CFOQQKEYSA-L
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| 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
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| Chemical Name |
disodium;5-[(2R)-2-[[(2R)-2-(3-chlorophenyl)-2-hydroxyethyl]amino]propyl]-1,3-benzodioxole-2,2-dicarboxylate
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| Synonyms |
CL316243 CL 316243 CL-316243
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
H2O : ~20 mg/mL (~42.94 mM)
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|---|---|
| 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.
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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