EIPA [1154-25-2]
Référence B7389-5mg
Conditionnement : 5mg
Marque : APExBIO Technology
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EIPA
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.
- 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
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- 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
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 299.76 |
| Cas No. | 1154-25-2 |
| Formula | C11H8ClN7O |
| Solubility | ≥32.1 mg/mL in DMSO; ≥13.9 mg/mL in EtOH; insoluble in H2O |
| 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. |
| 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. | |
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