SML2092
R115866
≥98% (HPLC), RAMBA blocker, film
别名:
(B)-N-[4-[2-Ethyl-1-(1H-1,2,4-triazol-1-yl)butyl]phenyl]-2-benzothiazolamine, (R)-N-[4-[2-Ethyl-1-(1H-1,2,4-triazol(-1-yl)butyl]phenyl]-2-benzothiazolamine, TLZ, Talarozole
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关于此项目
经验公式（希尔记法）:
C21H23N5S
化学文摘社编号:
分子量:
377.51
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
产品名称
R115866, ≥98% (HPLC)
SMILES string
[s]1c2c(nc1Nc3ccc(cc3)[C@H]([n]4ncnc4)C(CC)CC)cccc2
InChI
1S/C21H23N5S/c1-3-15(4-2)20(26-14-22-13-23-26)16-9-11-17(12-10-16)24-21-25-18-7-5-6-8-19(18)27-21/h5-15,20H,3-4H2,1-2H3,(H,24,25)/t20-/m1/s1
InChI key
SNFYYXUGUBUECJ-HXUWFJFHSA-N
assay
≥98% (HPLC)
form
film
color
colorless
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Biochem/physiol Actions
Orally active retinoic acid (RA) metabolism blocking agent (RAMBA) with higher CYP26 specificity and potency than liarozole (R75251).
R115866 (Talarozole) is an orally active all-trans retinoic acid (RA) metabolism blocking agent (RAMBA; IC50 = 4 nM against RA metablism in yeast microsomes expressing human CYP26) with much reduced or little potency against CYP19 (aromatase), CYP17 (17,20-lyase), CYP2C11, CYP3A, and CYP2A1 (IC50 from 1.2 to >10 μM). Plasma and tissue RA upregulation via R115866 oral treatment exhibits in vivo efficacy in several retinoid-responsive rodent models, including vaginal keratinization suppression (ED50 = 1.0 mg/kg/day vs. 5.1 mg/kg/day with RA in rats), pinnal hyperplasia induction (ear epidermis thickness = 35.5 μm with 2.5 mg/kg/day R115866 vs. 16.5 μm in control mice), conversion of caudal para- to ortho-keratosis (90% with 1.25 mg/kg/day R115866 vs. 30.3% in control mice). Comparing to liarozole, R115866 is CYP26-selective and does not inhibit CYP-mediated biosynthesis of adrenal and gonadal steroid hormones.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Sasmita Tripathy et al.
Molecular pharmacology, 89(5), 560-574 (2016-02-28)
All-trans-retinoic acid (atRA) is the active metabolite of vitamin A. The liver is the main storage organ of vitamin A, but activation of the retinoic acid receptors (RARs) in mouse liver and in human liver cell lines has also been
João E Carvalho et al.
BMC evolutionary biology, 17(1), 24-24 (2017-01-21)
During embryogenesis, tight regulation of retinoic acid (RA) availability is fundamental for normal development. In parallel to RA synthesis, a negative feedback loop controlled by RA catabolizing enzymes of the cytochrome P450 subfamily 26 (CYP26) is crucial. In vertebrates, the
Richard W Naylor et al.
Nature communications, 7, 12197-12197 (2016-07-14)
Despite the fundamental importance of patterning along the dorsal-ventral (DV) and anterior-posterior (AP) axes during embryogenesis, uncertainty exists in the orientation of these axes for the mesoderm. Here we examine the origin and formation of the zebrafish kidney, a ventrolateral
Philippe Diaz et al.
Journal of medicinal chemistry, 59(6), 2579-2595 (2016-02-27)
Cytochrome P450 CYP26 enzymes are responsible for all-trans-retinoic acid (atRA) clearance. Inhibition of CYP26 enzymes will increase endogenous atRA concentrations and is an attractive therapeutic target. However, the selectivity and potency of the existing atRA metabolism inhibitors toward CYP26A1 and
Salvador Alonso et al.
The Journal of clinical investigation, 126(12), 4460-4468 (2016-10-25)
Interactions between multiple myeloma (MM) cells and the BM microenvironment play a critical role in bortezomib (BTZ) resistance. However, the mechanisms involved in these interactions are not completely understood. We previously showed that expression of CYP26 in BM stromal cells
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