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.

Product information

CAS Number: 138908-40-4

Molecular Weight: 465.79

Formula: C20H18ClNNa2O7

Chemical Name: 2,2-disodium 5-[(2R)-2-{[(2R)-2-(3-chlorophenyl)-2-hydroxyethyl]amino}propyl]-2H-1,3-benzodioxole-2,2-dicarboxylate

Smiles: C[C@H](CC1C=C2OC(OC2=CC=1)(C(=O)O[Na])C(=O)O[Na])NC[C@H](O)C1C=C(Cl)C=CC=1

InChiKey: FUZBPOHHSBDTJQ-CFOQQKEYSA-L

InChi: 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

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: H2O : 62.5 mg/mL (134.18 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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. 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.

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.

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.
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.

Products are for research use only. Not for human use.