貨號	規格	價格	上海	北京	武漢	南京
S84280-5mg	≥99%	￥1440.00 S84280-5mg ￥1440.00 2-3天	0 貨期：2-3天	-	-	-
S84280-10mg	≥99%	￥1870.00 S84280-10mg ￥1870.00 2-3天	0 貨期：2-3天	-	-	-
S84280-50mg	≥99%	￥4500.00 S84280-50mg ￥4500.00 2-3天	0 貨期：2-3天	-	-	-
S84280-100mg	≥99%	￥7000.00 S84280-100mg ￥7000.00 2-3天	0 貨期：2-3天	-	-	-

產品介紹

Talarozole (R115866) is an oral systemic all-trans retinoic acid metabolism blocking agent (RAMBA) which increases intracellular levels of endogenous all-trans retinoic acid (RA). Talarozole inhibits both CYP26A1 and CYP26B1 with IC50s of 5.4 and 0.46 nM, respectively.

產品描述：

靶點：

CYP26;Others;?P450;?RetinoidReceptor;?Autophagy

體內研究：

A maximum 84% inhibition of CYP26 activity at 0.5 hours post-dose is predicted based on Talarozole (TLZ) Cmax of 80 nM and a Ki of 1 nM following a single dose of Talarozole. Due to the short Talarozole half-life (2.2 hrs) CYP26 activity is predicted to return to 100% by 12 hours. In agreement with the predictions, atRA concentrations are increased by 82, 63 and 60% at 4 hours post-dose in the serum, liver and testes, respectively, and concentrations returned to baseline by 24 hours. Following multiple doses of Talarozole, liver CYP26 mRNA and activity are increased suggesting autoinduction of CYP26 due to increased atRA concentrations. In agreement, atRA concentrations are elevated in serum and liver at all timepoints measured. This increase in atRA concentrations is associated with increased mRNA of the mitochondrial biogenesis markers PGC-1β and NRF-1 in comparison to control mice

參考文獻：

1. Diaz P, et al. Development and Characterization of Novel and Selective Inhibitors of Cytochrome P450 CYP26A1, theHuman Liver Retinoic Acid Hydroxylase. J Med Chem. 2016 Mar 24;59(6):2579-95. 2. Topletz AR, et al. Induction of CYP26A1 by metabolites of retinoic acid: evidence that CYP26A1 is an important enzyme in theelimination of active retinoids. Mol Pharmacol. 2015;87(3):430-41. 3. Faith Stevison, et al. CYP26 Inhibition Increases Retinoic Acid Concentrations in Target Tissues and Alters Retinoid Signaling 4. Tripathy S, et al.All-Trans-Retinoic Acid Enhances Mitochondrial Function in Models of Human Liver. Mol Pharmacol. 2016 May;89(5):560-74. 5. Bovenschen HJ, et al. Oral retinoic acid metabolism blocking agent Rambazole for plaque psoriasis: an immunohistochemical study. Br J Dermatol. 2007 Feb;156(2):263-70.

溶解性：

Soluble in DMSO

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.649 ml	13.245 ml	26.489 ml
5 mM	0.53 ml	2.649 ml	5.298 ml
10 mM	0.265 ml	1.324 ml	2.649 ml
50 mM	0.053 ml	0.265 ml	0.53 ml

注意：

部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

參考文獻

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