2. Others Metabolic Enzyme/Protease
  3. Fluorescent Dye UGT
  4. UGT1A1-IN-1

UGT1A1-IN-1 is a UGT1A1 inhibitor and fluorescent probe (Ex=370 nm, Em=520 nm), with an IC50 of 1.33 μM and a Ki of 5.02 μM. UGT1A1-IN-1 is selectively glucuronidated by UGT1A1 at the bilirubin homologous binding site, and its PET effect is blocked along with this reaction, triggering fluorescence changes. UGT1A1-IN-1 can serve as a substitute for bilirubin to detect UGT1A1 activity and perform high-throughput screening of UGT1A1 modulators.

For research use only. We do not sell to patients.

UGT1A1-IN-1

UGT1A1-IN-1 Chemical Structure

CAS No. : 2097024-37-6

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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UGT1A1-IN-1 Related Antibodies

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Description

UGT1A1-IN-1 is a UGT1A1 inhibitor and fluorescent probe (Ex=370 nm, Em=520 nm), with an IC50 of 1.33 μM and a Ki of 5.02 μM. UGT1A1-IN-1 is selectively glucuronidated by UGT1A1 at the bilirubin homologous binding site, and its PET effect is blocked along with this reaction, triggering fluorescence changes. UGT1A1-IN-1 can serve as a substitute for bilirubin to detect UGT1A1 activity and perform high-throughput screening of UGT1A1 modulators[1].

IC50 & Target[1]

UGT1A1

1.33 μM (IC50)

UGT1A1

5.02 μM (Ki)

In Vitro

UGT1A1-IN-1 (compound 2) (10-100 μM; 60 min) shows excellent selectivity for recombinant human UGT1A1 over other human UGT isoforms[1].
UGT1A1-IN-1 noncompetitively inhibits UGT1A1-mediated 1-O-glucuronidation in human liver microsomes, with a Ki of 5.02 μM and an IC50 of 1.33 μM[1].
UGT1A1-IN-1 is a high-affinity substrate for recombinant human UGT1A1 (S50 = 0.7 μM) and human liver microsomes (S50 = 4.3 μM), displaying sigmoidal enzymatic kinetics in both systems[1].
UGT1A1-IN-1 (5 μM) acts as a 'turn-on' fluorescent probe for recombinant human UGT1A1, with over 20-fold fluorescence enhancement upon glucuronidation, a linear response to incubation time and enzyme concentration, and a detection limit of 0.48 μg/mL[1].
UGT1A1-IN-1 binds to the same ligand-binding site (site I) on a human UGT1A1 homology model as bilirubin, confirming it can serve as a surrogate for bilirubin in UGT1A1-ligand interaction studies[1].
UGT1A1-IN-1 (5 μM; 30 min) accurately measures UGT1A1 activity in individual human liver microsomes, with activity varying 9-fold across samples and strong correlations with established UGT1A1 probe substrates and protein levels[1].
UGT1A1-IN-1 (5 μM; 30 min) effectively measures UGT1A1 activity in HepG2 cell homogenates[1].

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

UGT1A1-IN-1 Related Antibodies
Molecular Weight

345.39

Formula

C22H19NO3
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1C2=CC=CC3=C2C(C(N1CCCC)=O)=CC=C3C4=CC=C(O)C=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 17.5 mg/mL (50.67 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8953 mL 14.4764 mL 28.9528 mL
5 mM 0.5791 mL 2.8953 mL 5.7906 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8953 mL 14.4764 mL 28.9528 mL 72.3819 mL
5 mM 0.5791 mL 2.8953 mL 5.7906 mL 14.4764 mL
10 mM 0.2895 mL 1.4476 mL 2.8953 mL 7.2382 mL
15 mM 0.1930 mL 0.9651 mL 1.9302 mL 4.8255 mL
20 mM 0.1448 mL 0.7238 mL 1.4476 mL 3.6191 mL
25 mM 0.1158 mL 0.5791 mL 1.1581 mL 2.8953 mL
30 mM 0.0965 mL 0.4825 mL 0.9651 mL 2.4127 mL
40 mM 0.0724 mL 0.3619 mL 0.7238 mL 1.8095 mL
50 mM 0.0579 mL 0.2895 mL 0.5791 mL 1.4476 mL
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UGT1A1-IN-1 Related Classifications

Help & FAQs
  • 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:

UGT1A1-IN-12097024-37-6Fluorescent DyeUGTUDP-glucuronosyltransferaseUridine diphosphate glucuronosyltransferaseUGT1A1recombinant human UGT1A1O-glucuronidationglucuronidationhuman liver microsomesligand-binding sitebilirubinfluorescent probe substrateHepG2 cell homogenateschrysinInhibitorinhibitorinhibit

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