WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H510290
CAS#: 1515856-92-4
Description: XEN445 is potent and selective endothelial lipase inhibitor, that showed good ADME and PK properties, and demonstrated in vivo efficacy in raising plasma HDLc concentrations in mice. Endothelial lipase (EL) activity has been implicated in HDL metabolism and in atherosclerotic plaque development; inhibitors are proposed to be efficacious in the treatment of dyslipidemia related cardiovascular disease.
Hodoodo Cat#: H510290
Name: XEN445
CAS#: 1515856-92-4
Chemical Formula: C18H17F3N2O3
Exact Mass: 366.12
Molecular Weight: 366.330
Elemental Analysis: C, 59.02; H, 4.68; F, 15.56; N, 7.65; O, 13.10
Synonym: XEN445; XEN 445; XEN-445
IUPAC/Chemical Name: (S)-2-(3-(pyridin-2-ylmethoxy)pyrrolidin-1-yl)-5-(trifluoromethyl)benzoic acid
InChi Key: NBGRERFNOKZQLO-AWEZNQCLSA-N
InChi Code: InChI=1S/C18H17F3N2O3/c19-18(20,21)12-4-5-16(15(9-12)17(24)25)23-8-6-14(10-23)26-11-13-3-1-2-7-22-13/h1-5,7,9,14H,6,8,10-11H2,(H,24,25)/t14-/m0/s1
SMILES Code: O=C(O)C1=CC(C(F)(F)F)=CC=C1N2C[C@@H](OCC3=NC=CC=C3)CC2
Appearance: White to off-white solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
Biological target: | |
In vitro activity: | |
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The following data is based on the product molecular weight 366.33 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
Formulation protocol: | |
In vitro protocol: | |
In vivo protocol: |
1: Sun S, Dean R, Jia Q, Zenova A, Zhong J, Grayson C, Xie C, Lindgren A, Samra P, Sojo L, van Heek M, Lin L, Percival D, Fu JM, Winther MD, Zhang Z. Discovery of XEN445: a potent and selective endothelial lipase inhibitor raises plasma HDL-cholesterol concentration in mice. Bioorg Med Chem. 2013 Dec 15;21(24):7724-34. doi: 10.1016/j.bmc.2013.10.023. Epub 2013 Oct 28. PubMed PMID: 24211162.
2: Kim YT, Lee HJ, Lee SW, Kim JY, Wi HC, Park SJ, Bae SJ, Kang HJ. Pre-treatment of porcine pulmonary xenograft with desmopressin: a novel strategy to attenuate platelet activation and systemic intravascular coagulation in an ex-vivo model of swine-to-human pulmonary xenotransplantation. Xenotransplantation. 2008 Feb;15(1):27-35. doi: 10.1111/j.1399-3089.2008.00445.x. PubMed PMID: 18333911.