2-APBA TRP activator that also blocks IP3R

2-APB (CAS 524-95-8)

2-APB | CAS 524-95-8 is rated 5.0 out of 5 by 1.
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Synonym: 2-Aminoethyl diphenylborinate
Application: A TRP activator that also blocks IP3R
CAS Number: 524-95-8
Purity: ≥98%
Molecular Weight: 225.09
Molecular Formula: C14H16BNO
* Refer to Certificate of Analysis for lot specific data (including water content).
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2-APB is a transient receptor potential (TRP) activator. The compound also directly blocks the mitochondrial permeability transition pore, sarco/endoplasmic reticulum Ca2+-ATPase pumps, and native store operated channels, as well as other ion channels. 2-APB does not activate the subfamily transient receptor potential vanilloids (TRPVs) TRPV4, TRPV5, and TRPV6, but can activate VR1 (TRPV1), VRL-1 (TRPV2), and TRPV3. 2-ABP was first used as an inhibitor of IP3R (inositol 1,4,5-triphosphate receptor) with the ability to permeate the membrane. 2-ABP can induce Ca2+entry without activating exocytosis. In pancreatic acinar cells 2-ABP can inhibit calcium mobilization. 2-APB is an activator of Orai3.


References

1. Hu, H.Z., et al. 2004. J. Biol. Chem. 279: 35741-35748. PMID: 15194687
2. Xu, S.Z., et al. 2005. Br. J. Pharmacol. 145: 405-414. PMID: 15806115
3. Usmani, S.M., et al. 2010. Cell. Physiol. Biochem. 25: 91-102. PMID: 20054148
4. Choi, K.J., et al. 2010. Korean J. Physiol. Pharmacol. 14: 105-111. PMID: 20473382

Physical State :
Solid
Solubility :
Soluble in methanol (100 mg/ml), 95% ethanol (50 mg/ml), ethanol (10 mM), and DMSO (10 mM). Insoluble in water.
Storage :
Store at -20° C
Melting Point :
101.86° C (Predicted)
Boiling Point :
~325.3° C at 760 mmHg (Predicted)
Density :
~1.0 g/cm3 (Predicted)
Refractive Index :
n20D 1.56 (Predicted)
IC50 :
Thapsigargin-induced SOCE channel: IC50 = 15000 nM (fura-2 loaded human Jarkart T cells); D-myo-inositol 1,4,5-trisphosphate (IP3) receptor: IC50 = 42 µM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
RTECS :
ED6150000
PubChem CID :
1598
MDL Number :
MFCD00014823
EC Number :
208-366-5
Beilstein Registry :
2942273
SMILES :
B(C1=CC=CC=C1)(C2=CC=CC=C2)OCCN

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2-APB  Product Citations

See how others have used 2-APB. Click on the entry to view the PubMed entry .

Citations 1 to 10 of 12 total

PMID: # 31001087  Cabrera Zapata, LE.|Bollo, M.|Cambiasso, MJ.| et al. 2019. Front Cell Neurosci. 13: 122.

PMID: # 29175331  Fujita, T. et al. 2017. Biochemical and biophysical research communications.

PMID: # 27733612  Bellocchio, L. et al. 2016. J. Neurosci. 36: 10611-10624.

PMID: # 26631534  Zhong, W. et al. 2016. Neuropharmacology. 103: 195-210.

PMID: # 26675132  2015. Sci Rep. 5: 18325.

PMID: # 26099309  Özdemir, ÜS. et al. 2015. Mol. Neurobiol.

PMID: # 26690982  Kondo, K. et al. 2015. PLoS ONE. 10: e0144803.

PMID: # 25121483  Zhong, W. et al. 2014. PLoS ONE. 9: e104718.

PMID: # 24048853  DeMaria, S. et al. 2013. J. Neurosci. 33: 15235-47.

PMID: # 23458684  Masumoto, K. et al. 2013. Biochim. Biophys. Acta. 1830: 3382-90.

Citations 1 to 10 of 12 total
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Rated 5 out of 5 by from Kondo Kondo, et. al. (PubMed ID 15551003) found that by treating their samples 30 minutes prior to exposure to cockroach extract with the compound 2-APB that the calcium response was inhibited. In addition, this inhibition is demonstrated in a concentration based manner, that is - the level of inhibition is dependent on how much 2-APB was used. -SCBT Publication Review
Date published: 2015-01-15
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