L-748,337A selective competitive β3-adrenoceptor antagonist

L-748,337 (CAS 244192-94-7)

L-748,337 | CAS 244192-94-7 is rated 5.0 out of 5 by 1.
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Synonym: N-[[3-[(2S)-2-Hydroxy-3-[[2-[4-[(phenylsulfonyl)amino]phenyl]ethyl]amino]propoxy]phenyl]methyl]-acetamide
Application: A selective competitive β3-adrenoceptor antagonist
CAS Number: 244192-94-7
Purity: ≥98%
Molecular Weight: 497.61
Molecular Formula: C26H31N3O5S
* Refer to Certificate of Analysis for lot specific data (including water content).
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L 748337 is a selective, competitive β3-AR (β3-adrenoceptor ) antagonist that displays selectivity over β1 and β2 receptors (Ki values are 4.0, 204 and 390 nM for β3-, β2- and β1-adrenoceptors respectively). Inhibits cAMP accumulation in response to isoproterenol (IC50 = 6 nM).


References

. Candelore, M.R. et al. 1999. J. Pharmacol. Exp. Ther. 290(2): 649-655. PMID: 10411574
2. Sarma, D.N. et al. 2003. J. Pharmacol. Exp. Ther. 304(1): 48-55. PMID: 12490574
3. Neidhold, S. et al. 2007. Br. J. Pharmacol. 150(3): 261-270. PMID: 17179950

Physical State :
Solid
Solubility :
Soluble in DMSO (100 mM), and ethanol (25 mM).
Storage :
Store at 4° C
Melting Point :
312.66° C (Predicted)
Boiling Point :
714.21° C (Predicted)
Density :
~1.3 g/cm3 (Predicted)
Refractive Index :
n20D 1.61 (Predicted)
Optical Activity :
α20/D -3.2°, c = 1 in ethanol; α20/D +6°±2°, c = 4 in DMSO
IC50 :
cAMP accumulation: IC50 = 6 nM
Ki Data :
β3--adrenoceptors: Ki= 4.0 nM; β2-adrenoceptors: Ki= 204 nM; β1-adrenoceptors: Ki= 390 nM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
10028830
MDL Number :
MFCD10687097
SMILES :
CC(=O)NCC1=CC(=CC=C1)OC[C@H](CNCCC2=CC=C(C=C2)NS(=O)(=O)C3=CC=CC=C3)O

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Certificate of Analysis

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L-748,337  Product Citations

See how others have used L-748,337. Click on the entry to view the PubMed entry .

Citations 1 to 2 of 2 total

PMID: # 27485040  Lamkin, DM. et al. 2016. Brain Behav. Immun. 57: 338-46.

PMID: # 27206969  Procino, G. et al. 2016. Kidney Int. 90: 555-67.

Citations 1 to 2 of 2 total
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Rated 5 out of 5 by from Masutani Masutani, S. et al. (PubMed 23873794) investigated the effect of L-748,337, a selective and competitive 3-adrenoceptor antagonist, on left ventricular (LV) dynamics during exercise in dogs with pacing-induced heart failure. They found that after heart failure, L-748,337 improved LV diastolic filling; increased LV contractility, LV arterial coupling, and mechanical efficiency; improving exercise performance. -SCBT Publication Review
Date published: 2015-07-10
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