1. Others Metabolic Enzyme/Protease Membrane Transporter/Ion Channel Apoptosis
  2. Biochemical Assay Reagents Endogenous Metabolite OAT Ferroptosis
  3. 6-Hydroxyindole

6-Hydroxyindole is an orally active, endogenous long-acting OATP1B1 inhibitor. 6-Hydroxyindole does not alter the cell surface expression or subcellular localization of OATP1B1. 6-Hydroxyindole protects cells against Ferroptosis. 6-Hydroxyindole possesses intrinsic radical-trapping antioxidant activity. 6-Hydroxyindole serves as a component of oxidative hair dyes. 6-Hydroxyindole can be used in research related to renal failure and neurodegenerative diseases.

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6-Hydroxyindole

6-Hydroxyindole Chemical Structure

CAS No. : 2380-86-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO In-stock
Solid
1 g In-stock
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Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

6-Hydroxyindole is an orally active, endogenous long-acting OATP1B1 inhibitor. 6-Hydroxyindole does not alter the cell surface expression or subcellular localization of OATP1B1. 6-Hydroxyindole protects cells against Ferroptosis. 6-Hydroxyindole possesses intrinsic radical-trapping antioxidant activity. 6-Hydroxyindole serves as a component of oxidative hair dyes. 6-Hydroxyindole can be used in research related to renal failure and neurodegenerative diseases[1][2][3].

IC50 & Target[1]

Human Endogenous Metabolite

 

OATP1B1

 

In Vitro

6-Hydroxyindole (0.1-100 μM; 0.5 min-24 h) potently inhibits OATP1B1-mediated substrate uptake in HEK293/OATP1B1 cells via two mechanisms: direct action and long-lasting action, with an IC50 value ranging from 4.52 μM to 43.8 μM[1].
6-Hydroxyindole (100 μM; 3 h) does not alter the cell surface expression or subcellular localization of OATP1B1 in HEK293/OATP1B1 cells[1].
6-Hydroxyindole (20 μM; 22-24 h) protects HT-22 mouse hippocampal neurons against Erastin-induced ferroptosis[2].
6-Hydroxyindole (24 h) inhibits ferroptosis in HT-22 mouse hippocampal neurons, with an EC50 value of 15.8 μM against RSL3 and 8.4 μM against FINO2, and exerts partial protective effects against Erastin-induced ferroptosis[2].
6-Hydroxyindole (24 h) inhibits ferroptosis in N27 rat dopaminergic neurons, with an EC50 value of 9.1 μM against RSL3 and 8.1 μM against FINO2[2].
6-Hydroxyindole (0-103 μM; 7-15 min) exhibits dose-dependent free radical-scavenging antioxidant activity in cell-free ABTS assays[2].
6-Hydroxyindole (8-5000 μg/plate) exhibits mutagenicity towards *Salmonella typhimurium* strain TA 1535 under both metabolic activation and non-metabolic activation conditions[3].

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

Cell Viability Assay[2]

Cell Line: HT-22 mouse hippocampal neurons
Concentration: Dose-range
Incubation Time: 24 h
Result: Provided partial protection against Erastin-induced cytotoxicity (maximum protection was around 50%).
Exhibited EC50 values of 15.8 μM against RSL3 and 8.4 μM against FINO2; no EC50 was reported for Erastin.
In Vivo

6-Hydroxyindole (600 mg/kg; p.o.; single administration) causes death and acute toxicity symptoms in rats. Its maximum tolerated dose is lower than 600 mg/kg, and the LD50 in rats is greater than 600 mg/kg[3].
6-Hydroxyindole (2000 mg/kg; percutaneous; single administration) does not cause death in rats, with a maximum non-lethal dose greater than 2000 mg/kg[3].
6-Hydroxyindole (15-240 mg/kg/d; p.o.; daily; gestational days 6-19) causes no maternal toxicity in rats, with only mild fetal ossification retardation observed at high doses[3].

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

Animal Model: Crl:CD(Sprague Dawley [SD])BR (male and female)[3]
Dosage: 600 mg/kg
Administration: p.o.; single dose
Result: Caused 20% mortality (2 of 10 rats, both males).
Induced acute clinical signs (hunched posture, hypoactivity, prostration) on dosing day, with no signs in surviving animals after dosing day.
Resulted in no abnormal weight gain.
Caused spleen abnormalities in 1 male and uterine abnormalities in 1 female at necropsy.
Animal Model: Crl:CD(SD)BR (female mated, 24 per dose group)[3]
Dosage: 15-240 mg/kg/d
Administration: p.o.; daily; gestation days 6-19
Result: Resulted in no mortalities, with ptyalism observed in 4 dams at 240 mg/kg/d.
Showed no treatment-related changes in body weight, body weight gain, or feed consumption.
Caused statistically significantly lower preimplantation loss in 60 and 240 mg/kg/d groups compared to controls, with numbers of resorptions, dead fetuses, and fetal sex ratio comparable to controls.
Led to slightly lower (not statistically significant) mean fetal body weight at 240 mg/kg/d, with no treatment-related visceral anomalies.
Resulted in retardation of general fetal ossification at 240 mg/kg/d, with no bone malformations.
Molecular Weight

133.15

Formula

C8H7NO

CAS No.
Appearance

Solid

Color

White to yellow

SMILES

OC1=CC2=C(C=C1)C=CN2

Structure Classification
Initial Source
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 : 100 mg/mL (751.03 mM; Need ultrasonic; 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 7.5103 mL 37.5516 mL 75.1033 mL
5 mM 1.5021 mL 7.5103 mL 15.0207 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (18.78 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (18.78 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.98%

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 7.5103 mL 37.5516 mL 75.1033 mL 187.7582 mL
5 mM 1.5021 mL 7.5103 mL 15.0207 mL 37.5516 mL
10 mM 0.7510 mL 3.7552 mL 7.5103 mL 18.7758 mL
15 mM 0.5007 mL 2.5034 mL 5.0069 mL 12.5172 mL
20 mM 0.3755 mL 1.8776 mL 3.7552 mL 9.3879 mL
25 mM 0.3004 mL 1.5021 mL 3.0041 mL 7.5103 mL
30 mM 0.2503 mL 1.2517 mL 2.5034 mL 6.2586 mL
40 mM 0.1878 mL 0.9388 mL 1.8776 mL 4.6940 mL
50 mM 0.1502 mL 0.7510 mL 1.5021 mL 3.7552 mL
60 mM 0.1252 mL 0.6259 mL 1.2517 mL 3.1293 mL
80 mM 0.0939 mL 0.4694 mL 0.9388 mL 2.3470 mL
100 mM 0.0751 mL 0.3755 mL 0.7510 mL 1.8776 mL
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Product Name:
6-Hydroxyindole
Cat. No.:
HY-W002438
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