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BMS 753

Catalog No.
B5438
RARα-selective agonist
Grouped product items
SizePriceStock Qty
1mg
$53.00
Ship with 5-10 days
50mg
$1,179.00
Ship with 5-10 days
5mg
$181.00
Ship with 5-10 days
10mg
$330.00
Ship with 5-10 days
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

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Background

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.

Chemical Properties

Physical AppearanceOff-white solid
StorageStore at RT
M.Wt351.4
Cas No.215307-86-1
FormulaC21H21NO4
Solubility<35.14mg/ml in ethanol; <35.14mg/ml in DMSO
Chemical Name4-(1,1,3,3-tetramethyl-2-oxo-2,3-dihydro-1H-indene-5-carboxamido)benzoic acid
SDFDownload SDF
Canonical SMILESCC(C1=C(C(C)2C)C=C(C(NC3=CC=C(C(O)=O)C=C3)=O)C=C1)(C2=O)C
Shipping ConditionSmall 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.

Quality Control

Quality Control & MSDS

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Chemical structure

BMS 753