2-Aminoethoxydiphenyl borate

[2-APB]



ALX-400-045-M100	100 mg	30.00 USD

Replaces Prod. #: BML-CA238

Cell permeable modulator of Ins(1,4,5)-P₃-induced Ca²⁺ release. A prototype drug for a group of structurally related calcium channel blockers in human platelets. Has been shown, in the absence of other stimuli, to activate TRPV1, V2 and V3, but not TRPV4, V5 and V6 expressed in HEK 293 cells. Potentiates the effect of capsaicin, protons and heat on TRPV1. It was originally introduced as an IP3 receptor blocker and subsequently as an inhibitor of store-operated Ca²⁺ entry (75µM).

Product Specification

Formula:	C₁₄H₁₆BNO

MW:	225.1

Purity:	≥98%

Appearance:	White to off-white crystalline solid.

CAS:	524-95-8

RTECS:	ED6150000

Solubility:	Soluble in DMSO (20mg/ml), dimethyl formamide (20mg/ml) or 100% ethanol (5mg/ml); slightly soluble in PBS, pH 7.2 (50μg/ml).

Shipping:	SHIPPED ON BLUE ICE

Long Term Storage:	-20°C

Use/Stability:	Stable for at least 1 year after receipt when stored at -20°C. Stock solutions are stable for up to 2 months when stored at -20°C. We do not recommend storing aqueous solutions for more than one day.

Handling:	After reconstitution, prepare aliquots and store at -20°C. Hygroscopic. Packaged under inert gas.

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Product Literature References

2APB, 2-aminoethoxydiphenyl borate, a membrane-penetrable modulator of Ins(1,4,5)P3-induced Ca2+ release: T. Maruyama, et al.; J. Biochem. 122, 498 (1997), Abstract;

2-aminoethoxydiphenyl borate (2-APB) is a reliable blocker of store-operated Ca2+ entry but an inconsistent inhibitor of InsP3-induced Ca2+ release: M.D. Bootman, et al.; FASEB J. 16, 1145 (2002), Abstract;

Activation of TRPV4 channels (hVRL-2/mTRP12) by phorbol derivatives: H. Watanabe, et al.; J. Biol. Chem. 277, 13569 (2002), Abstract;

Inhibition of SERCA Ca2+ pumps by 2-aminoethoxydiphenyl borate (2-APB). 2-APB reduces both Ca2+ binding and phosphoryl transfer from ATP, by interfering with the pathway leading to the Ca2+-binding sites: J.G. Bilmen, et al.; Eur. J. Biochem. 269, 3678 (2002), Abstract;

2-aminoethoxydiphenyl borate activates and sensitizes the heat-gated ion channel TRPV3: M.K. Chung, et al.; J. Neurosci. 24, 5177 (2004), Abstract; Full Text

2-aminoethoxydiphenyl borate inhibits agonist-induced Ca2+ signals by blocking inositol trisphosphate formation in acutely dissociated mouse pancreatic acinar cells: J. Wu, et al.; Pflugers Arch. 448, 592 (2004), Abstract;

2-Aminoethoxydiphenyl borate is a common activator of TRPV1, TRPV2 and TRPV3: H.Z. Hu, et al.; J. Biol. Chem. 279, 35741 (2004), Abstract; Full Text

2APB- and JTV519(K201)-sensitive micro Ca2+ waves in arrhythmogenic Purkinje cells that survive in infarcted canine heart: P.A. Boyden, et al.; Heart Rhythm 1, 218 (2004), Abstract;

Induction of cholestasis in the perfused rat liver by 2-aminoethyl diphenylborate, an inhibitor of the hepatocyte plasma membrane Ca2+ channels: R.B. Gregory, et al.; J. Gastroenterol. Hepatol. 19, 1128 (2004), Abstract;

Inhibition of glutamate-induced delayed calcium deregulation by 2-APB and La3+ in cultured cortical neurones: C. Chinopoulos, et al.; J. Neurochem. 91, 471 (2004), Abstract;

The blocking of capacitative calcium entry by 2-aminoethyl diphenylborate (2-APB) and carboxyamidotriazole (CAI) inhibits proliferation in Hep G2 and Huh-7 human hepatoma cells: A. Enfissi, et al.; Cell Calcium 36, 459 (2004), Abstract;

TRPV4 calcium entry channel: a paradigm for gating diversity: B. Nilius, et al.; Am. J. Physiol. Cell Physiol. 286, C195 (2004), Abstract;

2-Aminoethoxydiphenyl borate perturbs hormone-sensitive calcium stores and blocks store-operated calcium influx pathways independent of cytoskeletal disruption in human A549 lung cancer cells: S. Padar, et al.; Biochem. Pharmacol. 69, 1177 (2005), Abstract;

2-aminoethoxydiphenyl borate stimulates pulmonary C neurons via the activation of TRPV channels: Q. Gu, et al.; Am. J. Physiol. Lung Cell Mol. Physiol. 288, L392 (2005), Abstract;

Block of TRPC5 channels by 2-aminoethoxydiphenyl borate: a differential, extracellular and voltage-dependent effect: S.Z. Xu, et al.; Br. J. Pharmacol. 145, 405 (2005), Abstract; Full Text

2-Aminoethoxydiphenyl borate (2-APB) stimulates a conformationally coupled calcium release pathway in the NG115-401L neuronal cell line: D.D. Bose & D.W. Thomas; Neuropharmacology 50, 532 (2006), Abstract;

2-aminoethoxydiphenyl borate as a prototype drug for a group of structurally related calcium channel blockers in human platelets: Y. Dobrydneva, et al.; Mol. Pharmacol. 69, 247 (2006), Abstract;