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MRS 1477

Names

[ CAS No. ]:
212200-21-0

[ Name ]:
MRS 1477

[Synonym ]:
3-Pyridinecarboxylic acid, 4-ethyl-1,4-dihydro-5-[[(2-methoxyethyl)thio]carbonyl]-6-methyl-2-phenyl-, ethyl ester
Ethyl 4-ethyl-5-{[(2-methoxyethyl)sulfanyl]carbonyl}-6-methyl-2-phenyl-1,4-dihydro-3-pyridinecarboxylate

Biological Activity

[Description]:

MRS 1477, a dihydropyridine derivative, is a positive allosteric modulator of TRPV1 in the presence of capsaicin. MRS 1477 itself does not induce apoptosis, but the co-existence of MRS 1477 and capsaicin can induce apoptosis[1][2].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> TRP Channel
Research Areas >> Cancer

[In Vitro]

MRS1477 在 MCF7 乳腺癌细胞中激发 Ca2+ 信号，但在原代乳腺上皮细胞中没有[1]。 MRS1477 (2 μM; 72 h) 与 capsaicine (10 μM) 一起诱导细胞凋亡并增加活性氧的产生和半胱天冬酶活性[1]。 MRS1477 (2 μM) 增加 capsaicine 诱发的 TRPV1 介导的电流密度水平[1]。

[References]

[1]. Nazıroğlu M, et, al. Targeting breast cancer cells by MRS1477, a positive allosteric modulator of TRPV1 channels. PLoS One. 2017 Jun 22;12(6):e0179950.  

[2]. Kaszas K, et, al. Small molecule positive allosteric modulation of TRPV1 activation by vanilloids and acidic pH. J Pharmacol Exp Ther. 2012 Jan;340(1):152-60.  

Chemical & Physical Properties

[ Density]:
1.1±0.1 g/cm3

[ Boiling Point ]:
532.4±50.0 °C at 760 mmHg

[ Molecular Formula ]:
C21H27NO4S

[ Molecular Weight ]:
389.51

[ Flash Point ]:
275.8±30.1 °C

[ Exact Mass ]:
389.166077

[ LogP ]:
4.01

[ Vapour Pressure ]:
0.0±1.4 mmHg at 25°C

[ Index of Refraction ]:
1.544

Related Compounds