B7389-5mg | EIPA [1154-25-2] Clinisciences

Background

EIPA is a TRPP3 channel inhibitor with an IC50 value of 10.5 μM, EIPA also inhibits Sodium-hydrogen exchangers (NHE) and macropinocytosis[1].

In Chinese hamster ovary cells, EIPA is a Na⁺/Ca²⁺ exchange (NCX) inhibitor that inhibits ET-1-induced continuous increase of intracellular Ca²⁺ concentration. In Xenopus oocytes, EIPA can rapidly and reversibly block calcium ion-activated TRPP3 channel activation at -50mV and other membrane potentials[2].

References:

[1]. Dai X Q, et al. Inhibition of TRPP3 channel by MK-870 and analogs. Mol Pharmacol, 2007, 72(6): 1576-85.

[2]. Horinouchi T, Miyake Y, Nishiya T, et al. Functional Role of Na⁺/H⁺ Exchanger in Ca2+ Influx Mediated via Human Endothelin Type A Receptor Stably Expressed in Chinese Hamster Ovary Cells. Journal of Pharmacological Sciences, 2008, 107(4): 456-459.

Product Citation

1. Tiezhu Liu, Jiajia Li, et al. "Knockout of CLTC gene reduces but not completely block SFTSV infection." PLoS One. 2023 Aug 25;18(8):e0285673. PMID: 37624798
2. Jia Wen, Xiuge Gao, et al. "Optimization of Tilmicosin-Loaded Nanostructured Lipid Carriers Using Orthogonal Design for Overcoming Oral Administration Obstacle." Pharmaceutics. 2021 Feb 25;13(3):303. PMID:33669090
3. Zhang Q, Yang H, et al. "Nanostructured lipid carriers with exceptional gastrointestinal stability and inhibition of P-gp efflux for improved oral delivery of tilmicosin." Colloids Surf B Biointerfaces. 2019 Nov 17:110649. PMID:31767412
4. Li Y, Yang B, et al. "Oral delivery of imatinib through galactosylated polymeric nanoparticles to explore the contribution of a saccharide ligand to absorption." Int J Pharm. 2019 Jul 9;568:118508. PMID:31299337
5. Liu W, Zhang L, et al. "Alpl prevents bone ageing sensitivity by specifically regulating senescence and differentiation in mesenchymal stem cells." Bone Res. 2018 Sep 11;6:27. PMID:30210899
6. Siu FY, Ye S, et al. "Galactosylated PLGA nanoparticles for the oral delivery of resveratrol: enhanced bioavailability and in vitro anti-inflammatory activity." Int J Nanomedicine. 2018 Jul 13;13:4133-4144. PMID:30038494
7. Gao W, Ye G, et al. "Transferrin receptor-targeted pH-sensitive micellar system for diminution of drug resistance and targetable delivery in multidrug-resistant breast cancer." Int J Nanomedicine. 2017 Feb 7;12:1047-1064. PMID:28223798

Hide ↑↑

Chemical Properties

Physical Appearance	A crystalline solid
Storage	Store at -20°C
M.Wt	299.76
Cas No.	1154-25-2
Formula	C₁₁H₈ClN₇O
Solubility	Soluble in DMSO
Chemical Name	3-amino-6-chloro-N-(diaminomethylene)-5-(ethyl(isopropyl)amino)pyrazine-2-carboxamide
SDF	Download SDF
Canonical SMILES	ClC1=NC(C(/N=C(N)\N)=O)=C(N)N=C1N(CC)C(C)C
Shipping Condition	Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips	We do not recommend long-term storage for the solution, please use it up soon.

Protocol

Cell experiment [1]:
Cell lines	Chinese hamster ovary cells ; X. laevis oocytes expressed TRPP3
Preparation method	The solubility of this compound in DMSO is >10mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.
Reacting condition	Chinese hamster ovary cells were treated with 10 μM EIPA for 30 minOocytes were treated with 100μM EIPA.
Applications	In chinese hamster ovary Cells, EIPA ,a Na+/Ca2+ exchanger (NCX) inhibitor, inhibited ET-1-induced sustained increases in intracellular Ca2+ concentration ([Ca2+]i).In X. laevis oocytes, EIPA rapidly and reversibly blocked Ca2+ activated TRPP3 channel activation at -50 mV as well as at other membrane potentials.
References: [1] .Dai et al (2007) Inhibition of TRPP3 channel by amiloride and analogs. Mol.Pharmacol. 72 1576. PMID: 17804601. [2]. Horinouchi et al (2008) Functional role of Na+/H+ exchanger in Ca2+ influx mediated via human endothelin type A receptor stably expressed in Chinese hamster ovary cells. J.Pharm.Sci. 107 456. PMID: 18678984.