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BMS 753
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BMS 753图片
CAS NO:215307-86-1
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
BMS 753 是一种同种型选择性视黄酸受体α (RARα) 激动剂,Ki 为 2 nM。
Cas No.215307-86-1
化学名4-(1,1,3,3-tetramethyl-2-oxo-2,3-dihydro-1H-indene-5-carboxamido)benzoic acid
Canonical SMILESCC(C1=C(C(C)2C)C=C(C(NC3=CC=C(C(O)=O)C=C3)=O)C=C1)(C2=O)C
分子式C21H21NO4
分子量351.4
溶解度<35.14mg/ml in ethanol;<35.14mg/ml in DMSO
储存条件Store at RT
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Ki : 2 nM for RARα

Three retinoic acid receptors (RARα, RARβ and RARγ and three retinoid X receptors, members of the nuclear receptor (NR) superfamily, mediate the biological effects of retinoic acids (all-tratis and 9-cis retinoic acids; t-RA and 9c-RA) upon development, cell differentiation and proliferation, and homeostasis. BMS 753 is identified as a RARα-selective agonist.

In vitro: Increasing concentrations of BMS 753 resulted in low levels of RARβ2 transcripts in WT cells, even at the highest concentration, while 100 nM BMS 753 efficiently induced RARβ2 transcripts in RARγ-/- cells. In contrast, no activation was seen in RARα-/- cells up to 100 nM BMS 753, demonstrating that it is specific for RARα [1].

In vivo: To investigate whether similar RARα-dependent events in Sertoli cells (SC) also operate in the reinitiation of spermatogenesis in a vitamin A-deficient (VAD) testis, Rbp4-null adult males fed a VAD diet for 14 wk were treated with BMS 753 or with its vehicle only. Interestingly, spermatogenesis did not initiate upon administration of BMS 753 to VAD Rbp4-null mutants; only SC and spermatogonia were present in their seminiferous epithelium, as in the vehicle-treated situation [2].

Clinical trial: Up to now, BMS 753 is still in the preclinical development stage.

Reference:
[1] RESHMA TANEJA, BIDYUT ROY, JEAN-Luc PLASSAT, CHRIS F.  ZuSIt, JACEK OSTROWSKIS, PETER R. RECZEKS, AND PIERRE CHAMBON. Cell-type and promoter-context dependent retinoic acid receptor (RAR) redundancies for RARβ2 and Hoxa-1 activation in F9 and P19 cells can be artefactually generated by gene knockouts. Proc. Natl. Acad. Sci. USA Vol. 93, pp. 6197-6202, June 1996.
[2] Raverdeau M, Gely-Pernot A, Féret B, Dennefeld C, Benoit G, Davidson I, Chambon P, Mark M, Ghyselinck NB.  Retinoic acid induces Sertoli cell paracrine signals for spermatogonia differentiation but cell autonomously drives spermatocyte meiosis. Proc Natl Acad Sci U S A. 2012 Oct 9;109(41):16582-7.