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AtuFECT01
AtuFect01 is part of the lipid system AtuPLEX and shows more effective siRNA binding activity and delivery to vascular endothelial cells.
* Please kindly note that our products are not to be used for therapeutic purposes and cannot be sold to patients.
Ordering Information
| Catalog Number | Size | Price | Stock | Quantity |
|---|---|---|---|---|
| BRP-02120 | 10 mg | $3980 | In stock |
Catalog
BRP-02120
Synonyms
β-Alaninamide, L-arginyl-2-amino-N-hexadecyl-N-(9Z)-9-octadecenyl-, trihydrochloride, (2S)-; β-Alaninamide, L-arginyl-2-amino-N-hexadecyl-N-(9Z)-9-octadecen-1-yl-, hydrochloride (1:3), (2S)-; (S)-2-amino-N-((S)-2-amino-3-(hexadecyl((Z)-octadec-9-en-1-yl)amino)-3-oxopropyl)-5-guanidinopentanamide trihydrochloride
CAS
869094-19-9
IUPAC Name
[(4S)-4-azaniumyl-5-[[(2S)-2-azaniumyl-3-[hexadecyl-[(Z)-octadec-9-enyl]amino]-3-oxopropyl]amino]-5-oxopentyl]-(diaminomethylidene)azanium;trichloride
Molecular Weight
843.58
Molecular Formula
C43H87N7O2.3HCl
Canonical SMILES
CCCCCCCCCCCCCCCCN(CCCCCCCCC=CCCCCCCCC)C(=O)C(CNC(=O)C(CCC[NH+]=C(N)N)[NH3+])[NH3+].[Cl-].[Cl-].[Cl-]
InChI
InChI=1S/C43H87N7O2.3ClH/c1-3-5-7-9-11-13-15-17-19-20-22-24-26-28-30-32-37-50(36-31-29-27-25-23-21-18-16-14-12-10-8-6-4-2)42(52)40(45)38-49-41(51)39(44)34-33-35-48-43(46)47;;;/h17,19,39-40H,3-16,18,20-38,44-45H2,1-2H3,(H,49,51)(H4,46,47,48);3*1H/b19-17-;;;/t39-,40-;;;/m0.../s1
InChIKey
UPGACERKWPBHRP-BTYIVCGTSA-N
Purity
≥95%
Related CAS
869184-08-7 (free base)
Chemical Structure:
Reference Reading
1. Small interfering RNA for cancer treatment: overcoming hurdles in delivery
Nitin Bharat Charbe, Nikhil D Amnerkar, B Ramesh, Murtaza M Tambuwala, Hamid A Bakshi, Alaa A A Aljabali, Saurabh C Khadse, Rajendran Satheeshkumar, Saurabh Satija, Meenu Metha, Dinesh Kumar Chellappan, Garima Shrivastava 0, Gaurav Gupta, Poonam Negi, Kamal Dua, Flavia C Zacconi. Acta Pharm Sin B. 2020 Nov;10(11):2075-2109. doi: 10.1016/j.apsb.2020.10.005.
In many ways, cancer cells are different from healthy cells. A lot of tactical nano-based drug delivery systems are based on the difference between cancer and healthy cells. Currently, nanotechnology-based delivery systems are the most promising tool to deliver DNA-based products to cancer cells. This review aims to highlight the latest development in the lipids and polymeric nanocarrier for siRNA delivery to the cancer cells. It also provides the necessary information about siRNA development and its mechanism of action. Overall, this review gives us a clear picture of lipid and polymer-based drug delivery systems, which in the future could form the base to translate the basic siRNA biology into siRNA-based cancer therapies.
2. Dissecting the relative contribution of OATP1B1-mediated uptake of xenobiotics into human hepatocytes using siRNA
B Williamson, A C Soars, A Owen, P White, R J Riley, M G Soars. Xenobiotica. 2013 Oct;43(10):920-31. doi: 10.3109/00498254.2013.776194.
1. Organic anion transporting polypeptide 1B1 plays a pivotal role in the disposition of many anionic drugs. Significant overlap in substrate specificity between individual OATP isoforms has hampered the identification of the relative importance of individual isoforms for hepatic uptake of xenobiotics. 2. The present study focused on the use of siRNA technology to decrease OATP1B1 selectively in human hepatocytes. Following delivery of siRNA by the novel lipid, AtuFECT01, mRNA expression of OATP1B1 was reduced by 94%-98% with no significant toxicity. Off-target effects were also shown to be minimal as evidenced by the expression of common drug metabolizing enzymes, transporters, nuclear receptors and associated co-regulators. Uptake of estrone-3-sulfate (5 nM) by OATP1B1 was reduced by 82%-95%. This methodology was subsequently used to assess the relative contribution of OATP1B1 uptake in human hepatocytes for olmesartan (42%-62%), valsartan (28%-81%), rosuvastatin (64%-72%), pitavastatin (84%-98%) and lopinavir (64%-89%). These data are consistent with previous values obtained using a relative activity factor approach. 3. The siRNA approach provides a robust and reproducible method for assessing the relative contribution of OATP1B1 to hepatic uptake of new chemical entities. The technique also has potential utility in facilitating detailed characterization of drug-drug interactions involving hepatic drug transporters.
