(±)-1-[(3aR*,4S*,9bS*)-4-(6-Bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl]-ethanone

그림문자(GHS)

• 그림문자(GHS)

  

• 신호 어

  Danger

• 유해·위험 문구

  H302：삼키면 유해함

  H372：장기간 또는 반복 노출되면 장기(또는, 영향을 받은 알려진 모든 장기를 명시)에 손상을 일으킴

  H400：수생생물에 매우 유독함

• 예방조치문구

  P264：취급 후에는 손을 철저히 씻으시오.

  P264：취급 후에는 손을 철저히 씻으시오.

  P270：이 제품을 사용할 때에는 먹거나, 마시거나 흡연하지 마시오.

  P273：환경으로 배출하지 마시오.

  P301+P312：삼켜서 불편함을 느끼면 의료기관(의사)의 진찰을 받으시오.

  P330：입을 씻어내시오.

  P391：누출물을 모으시오.

  P501：...에 내용물 / 용기를 폐기 하시오.

(±)-1-[(3aR*,4S*,9bS*)-4-(6-Bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl]-ethanone 화학적 특성, 용도, 생산

• 개요

  GPR30 is a transmembrane G protein-coupled receptor (GPCR) localized to endoplasmic reticulum (ER) that binds estradiol with high affinity, activating multiple intracellular signaling pathways. G-1 is a nonsteroidal, high-affinity, selective agonist of GPR30 that binds with a K_i value of 11 nM. Competitive binding studies in estrogen receptor α- (ERα-) and ERβ-expressing cells yielded K_i values for estradiol of 0.30 and 0.38 nM, respectively, with no substantial binding of G-1 at 1 μM. The discovery of G-1, a compound that does not bind classical ERs, should facilitate further physiological experiments to define the role of GPR30 in vivo.

• 용도

  G-1 is a potent and selective G protein-coupled estrogen receptor (GPER) agonist (Ki = 11 nM, EC50 = 2 nM); displays no activity at ERα and ERβ at concentrations up to 10 μM. Increases cytosolic Ca2+ and inhibits migration of SKBr3 cells and MCF-7 cells in response to chemoattractants (IC50 values are 0.7 and 1.6 nM respectively) in vitro. Blocks MCF-1 cell cycle progression at the G1 phase. Displays therapeutic effects in the mouse EAE model of multiple sclerosis.

(±)-1-[(3aR*,4S*,9bS*)-4-(6-Bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl]-ethanone 공급 업체

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