CL 316,243
| Code | Size | Price |
|---|
| AG-CR1-3699-M001 | 1 mg | £60.00 |
Quantity:
| AG-CR1-3699-M005 | 5 mg | £140.00 |
Quantity:
Prices exclude any Taxes / VAT
Overview
Regulatory Status: RUO
Shipping:
Ambient
Storage:
+4°C
Documents
Further Information
Alternate Names/Synonyms:
5-[(2R)-2-[[(2R)-2-(3-Chlorophenyl)-2-hydroxyethyl]amino] propyl]-1,3-benzodioxole-2,2-dicarboxylic acid disodium salt
Appearance:
White to off-white powder.
CAS:
138908-40-4
EClass:
32160000
Form (Short):
liquid
Handling Advice:
Keep cool and dry.
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
InChiKey:
FUZBPOHHSBDTJQ-CFOQQKEYSA-L
Long Description:
Chemical. CAS: 138908-40-4. Formula: C20H18ClNO7 . 2Na. MW: 419.8 . 46.0. Potent and selective beta3-adrenoceptor agonist (EC50=3nM) that is >10,000-fold selective over beta1 and beta2. Antidiabetic and antiobesity agent. Causes a rapid decrease in blood glucose level in mice. Increases brown adipose tissue thermogenesis. Induces functionally active mitochondrial uncoupling protein (UCP) in white fat. Restores the expression of down-regulated fatty acid oxidation genes in type 2 diabetic mice.
MDL:
MFCD00907153
Molecular Formula:
C20H18ClNO7 . 2Na
Molecular Weight:
419.8 . 46.0
Package Type:
Vial
Product Description:
Potent and selective beta3-adrenoceptor agonist (EC50=3nM) that is >10,000-fold selective over beta1 and beta2. Antidiabetic and antiobesity agent. Causes a rapid decrease in blood glucose level in mice. Increases brown adipose tissue thermogenesis. Induces functionally active mitochondrial uncoupling protein (UCP) in white fat. Restores the expression of down-regulated fatty acid oxidation genes in type 2 diabetic mice.
Purity:
>98%
SMILES:
ClC1=CC=CC([C@@H](O)CN[C@H](C)CC2=CC=C(OC(C([O-])=O)(C([O-])=O)O3)C3=C2)=C1.[Na+].[Na+]
Solubility Chemicals:
Soluble in water (5mg/ml). Slightly soluble in DMSO (0.5mg/ml).
Transportation:
Non-hazardous
UNSPSC Category:
Biochemical Reagents
UNSPSC Number:
12352200
Use & Stability:
Stable for at least 2 years after receipt when stored at -20°C.
References
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.D. Bloom, et al.; J. Med. Chem. 35, 3081 (1992) | Anti-obesity and anti-diabetic effects of CL 316,243, a highly specific beta 3-adrenoceptor agonist, in yellow KK mice: T. Yoshida, et al.; Life Sci. 54, 491 (1994) | Effect of CL-316,243, a thermogenic beta 3-agonist, on energy balance and brown and white adipose tissues in rats: J. Himms-Hagen, et al.; Am. J. Physiol. 266, R1371 (1994) | Appearance of brown adipocytes in white adipose tissue during CL 316,243-induced reversal of obesity and diabetes in Zucker fa/fa rats: M. Ghorbani & J. Himms-Hagen; Int. J. Obes. Relat. Metab. Disord. 21, 465 (1997) | Increase in insulin action and fat oxidation after treatment with CL 316,243, a highly selective beta3-adrenoceptor agonist in humans: C. Weyer, et al.; Diabetes 47, 1555 (1998) | The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors: J.G. Baker; Br. J. Pharmacol. 144, 317 (2005) | The effects of beta(3)-adrenoceptor agonist CL-316,243 on adiponectin, adiponectin receptors and tumor necrosis factor-alpha expressions in adipose tissues of obese diabetic KKAy mice: L. Fu, et al.; Eur. J. Pharmacol. 584, 202 (2008) | Anti diabetic effect of CL 316,243 (a beta3-adrenergic agonist) by down regulation of tumour necrosis factor (TNF-alpha) expression: M. Ghorbani, et al.; PLoS One 7, e45874 (2012) | The beta3-adrenergic receptor is dispensable for browning of adipose tissues: J.M.A. de Jong, et al.; Am. J. Physiol. Endocrinol. Metab. 312, E508 (2017) | Browning of white adipose tissue induced by the ?3 agonist CL-316,243 after local and systemic treatment - PK-PD relationship: W. Danysz, et al.; Biochim. Biophys. Acta 1864, 2972 (2018) | Deconstructing adipogenesis induced by beta3-adrenergic receptor activation with single-cell expression profiling: R.B. Burl, et al.; Cell Metab. 28, 300 (2018) | NOTUM promotes thermogenic capacity and protects against diet-induced obesity in male mice: F. Guo, et al.; Nature Sci. Rep. 11, 16409 (2021)
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