UE2316

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 466151

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.

Chemical Structure

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UE2316
CAS# 1274933-58-2
Instruction

Theoretical Analysis

MedKoo Cat#: 466151
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

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

Request quote for custom synthesis

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:

Preparing Stock Solutions

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.

Recalculate based on batch purity %
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:

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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.