UK-157147

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UK-157147 is a substrate for UDP-glucuronosyltransferases (UGT1A1) with a K_m value of 105 μM.

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UK-157147 Chemical Structure

CAS No. : 162704-20-3

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Description	UK-157147 is a substrate for UDP-glucuronosyltransferases (UGT1A1) with a K_m value of 105 μM.
IC₅₀ & Target	Km: 105 μM (UGT1A1)^[1]
In Vitro	Glucuronidation is an important pathway for human drug metabolism. Four cloned and expressed human UDP-glucuronosyltransferases (UGT1A1, UGT1A6, UGT1A9, and UGT2B15) are used to screen a series of three potential drug substrates differing only in position of the phenol moiety. The para phenol UK-157147 (UK-157,147) is found to be a substrate for UGT1A1 with a K_m value of 105 μM^[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. UK-157147 Related Antibodies
Molecular Weight	472.51
Formula	C₂₃H₂₄N₂O₇S
CAS No.	162704-20-3
SMILES	O=C1C=CC(O[C@H]2[C@](C)(O)C(C)(C)OC3=CC=C(S(=O)(C4=CC=CC(O)=C4)=O)C=C23)=NN1C
Shipping	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation	Data Sheet (274 KB) Handling Instructions (2659 KB)
References	[1]. Ethell BT, et al. Use of cloned and expressed human UDP-glucuronosyltransferases for the assessment of human drug conjugation and identification of potential drug interactions. Drug Metab Dispos. 2001 Jan;29(1):48-53. [Content Brief]

Kinase Assay
^[1]

UGT assays are performed. Assays are incubated in 100 mM Tris/maleate buffer (pH 7.4) containing 5 mM MgCl₂, typically 500 μM substrate, and 350 to 500 μg of cellular sonicate in a total volume of 100 μL. Screening assays are incubated for 60 min at 37°C at two concentrations of UDPGA: 50 μM and 2 mM (containing 0.1 μCi [¹⁴C]UDPGA). UDPGA (50 μM) assays allow higher levels of radiolabel incorporation into the glucuronide, which enhances assay sensitivity making this a useful tool for screening. Kinetic determinations are performed at 2 mM UDPGA or higher. The compounds screened are UK-157147 (UK-157,147), UK-156,037, and UK-157,261. Each batch of screening assays is accompanied by positive controls for the cell lines: UGT1A9, 500 μM propofol; UGT1A6, 500 μM 1-naphthol; UGT1A1, 250 μM 17α-ethinylestradiol; and UGT2B15, 500 μM 8-hydroxyquinoline. The unknown compounds are also assayed with human liver microsomes to establish a retention time for the radiolabeled conjugate on the radiochemical HPLC system^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

[1]. Ethell BT, et al. Use of cloned and expressed human UDP-glucuronosyltransferases for the assessment of human drug conjugation and identification of potential drug interactions. Drug Metab Dispos. 2001 Jan;29(1):48-53. [Content Brief]

UK-157147 Related Classifications

Metabolic Disease

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Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

UK-157147162704-20-3UK157147UK 157147UGTUDP-glucuronosyltransferaseUridine diphosphate glucuronosyltransferaseInhibitorinhibitorinhibit

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