WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H466151
CAS#: 1274933-58-2
Description: UE2316 is a potent and selective 11ß-HSD1 inhibitor, improving memory, including after intracerebroventricular drug administration to the central nervous system alone.
Hodoodo Cat#: H466151
Name: UE2316
CAS#: 1274933-58-2
Chemical Formula: C19H17ClFN3OS
Exact Mass: 389.08
Molecular Weight: 389.873
Elemental Analysis: C, 58.53; H, 4.40; Cl, 9.09; F, 4.87; N, 10.78; O, 4.10; S, 8.22
This product is not in stock, which may be available by custom synthesis.
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Synonym: UE2316; UE 2316; UE-2316;
IUPAC/Chemical Name: (5-(1H-pyrazol-4-yl)thiophen-3-yl)(4-(2-chlorophenyl)-4-fluoropiperidin-1-yl)methanone
InChi Key: PLUFYVPRHFNYBR-UHFFFAOYSA-N
InChi Code: InChI=1S/C19H17ClFN3OS/c20-16-4-2-1-3-15(16)19(21)5-7-24(8-6-19)18(25)13-9-17(26-12-13)14-10-22-23-11-14/h1-4,9-12H,5-8H2,(H,22,23)
SMILES Code: O=C(N1CCC(F)(C2=CC=CC=C2Cl)CC1)C3=CSC(C4=CNN=C4)=C3
Appearance: 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: To be determined
Shelf Life: >2 years if stored properly
Drug Formulation: To be determined
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: | |
In vivo activity: |
The following data is based on the product molecular weight 389.87 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: Wu J, Miller E, Davidson C, Walker BR, Hadoke PWF. Enhanced Angiogenesis by 11βHSD1 Blockage Is Insufficient to Improve Reperfusion Following Hindlimb Ischaemia. Front Cardiovasc Med. 2022 Jan 12;8:795823. doi: 10.3389/fcvm.2021.795823. PMID: 35097015; PMCID: PMC8790072.
2: Bonhomme D, Alfos S, Webster SP, Wolff M, Pallet V, Touyarot K. Vitamin A deficiency impairs contextual fear memory in rats: Abnormalities in the glucocorticoid pathway. J Neuroendocrinol. 2019 Nov;31(11):e12802. doi: 10.1111/jne.12802. Epub 2019 Nov 13. PMID: 31613407.
3: Cobice DF, Livingstone DEW, McBride A, MacKay CL, Walker BR, Webster SP, Andrew R. Quantification of 11β-hydroxysteroid dehydrogenase 1 kinetics and pharmacodynamic effects of inhibitors in brain using mass spectrometry imaging and stable-isotope tracers in mice. Biochem Pharmacol. 2018 Feb;148:88-99. doi: 10.1016/j.bcp.2017.12.013. Epub 2017 Dec 15. PMID: 29248595; PMCID: PMC5821700.
4: Sooy K, Noble J, McBride A, Binnie M, Yau JL, Seckl JR, Walker BR, Webster SP. Cognitive and Disease-Modifying Effects of 11β-Hydroxysteroid Dehydrogenase Type 1 Inhibition in Male Tg2576 Mice, a Model of Alzheimer's Disease. Endocrinology. 2015 Dec;156(12):4592-603. doi: 10.1210/en.2015-1395. Epub 2015 Aug 25. PMID: 26305888; PMCID: PMC4655221.
5: Wheelan N, Webster SP, Kenyon CJ, Caughey S, Walker BR, Holmes MC, Seckl JR, Yau JL. Short-term inhibition of 11β-hydroxysteroid dehydrogenase type 1 reversibly improves spatial memory but persistently impairs contextual fear memory in aged mice. Neuropharmacology. 2015 Apr;91:71-6. doi: 10.1016/j.neuropharm.2014.12.005. Epub 2014 Dec 11. PMID: 25497454; PMCID: PMC4389269.
6: Yau JL, Wheelan N, Noble J, Walker BR, Webster SP, Kenyon CJ, Ludwig M, Seckl JR. Intrahippocampal glucocorticoids generated by 11β-HSD1 affect memory in aged mice. Neurobiol Aging. 2015 Jan;36(1):334-43. doi: 10.1016/j.neurobiolaging.2014.07.007. Epub 2014 Jul 15. PMID: 25109766; PMCID: PMC4706164.
7: Chapagain A, Caton PW, Kieswich J, Andrikopoulos P, Nayuni N, Long JH, Harwood SM, Webster SP, Raftery MJ, Thiemermann C, Walker BR, Seckl JR, Corder R, Yaqoob MM. Elevated hepatic 11β-hydroxysteroid dehydrogenase type 1 induces insulin resistance in uremia. Proc Natl Acad Sci U S A. 2014 Mar 11;111(10):3817-22. doi: 10.1073/pnas.1312436111. Epub 2014 Feb 25. PMID: 24569863; PMCID: PMC3956172.
8: Sarabdjitsingh RA, Zhou M, Yau JL, Webster SP, Walker BR, Seckl JR, Joëls M, Krugers HJ. Inhibiting 11β-hydroxysteroid dehydrogenase type 1 prevents stress effects on hippocampal synaptic plasticity and impairs contextual fear conditioning. Neuropharmacology. 2014 Jun;81:231-6. doi: 10.1016/j.neuropharm.2014.01.042. Epub 2014 Feb 1. PMID: 24495397.