Art. -Nr.: HY-170522

Garutadustat

Name: Garutadustat
Brand: MedChemExpress
SKU: HY-170522
Price: 724.00 USD
Availability: InStock
Rating: 5 (1 reviews)

(Synonyms: ISM012-042)

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Garutadustat (ISM012-042) is an orally active, selective inhibitor of PHD1 and PHD2, with IC₅₀ values of 1.9 nM and 2.5 nM, respectively. Garutadustat stabilizes HIF1α protein in intestinal epithelial cells, thereby activating gene transcription programs associated with mucus production, tight junction formation, anti-inflammatory mediator generation and wound healing, which fundamentally promotes mucosal barrier repair and regulates intestinal immunity. Garutadustat can be used for the research of inflammatory bowel disease.

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Reinheit: 98.78%
CAS. Nr.: 2924181-80-4
Formel: C₂₅H₂₇N₇O₄
Molecular Weight:489.53

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Garutadustat Chemical Structure

CAS. Nr.: 2924181-80-4

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle HIF/HIF Prolyl-Hydroxylase Isoform-spezifische Produkte anzeigen :

In Vitro

Garutadustat (ISM012-042) (6 h) stabilizes HIF1α in Caco-2 HIF1α-HiBit cells with an EC₅₀ value of 2.0 to 3.5 μM, and retains activity under different extracellular iron concentrations^[1].
Garutadustat (2.5 μM; 0-96 h) protects Caco-2 cell monolayers against DSS (HY-116282C)-induced intestinal barrier disruption^[1].
Garutadustat 2 (1-10 μM; 24 h) dose-dependently reduces the mRNA expression of proinflammatory cytokines IL-12p35 and TNF in LPS-stimulated mouse bone marrow-derived dendritic cells (BMDCs)^[1].
Garutadustat (3 μM; 25 h) maintains the localization of ZO1 at intercellular junctions in Caco-2 cells and protects against DSS-induced tight junction disruption^[1].

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

Real Time qPCR^[1]

Cell Line:

Murine bone marrow-derived dendritic cells (BMDCs) stimulated with lipopolysaccharide (LPS)
Concentration:

1, 3, 10 μM
Incubation Time:

24 h (concurrent with LPS stimulation)
Result:

Dose-dependently reduced IL-12p35 mRNA expression relative to LPS-stimulated vehicle controls.
Dose-dependently reduced TNF mRNA expression relative to LPS-stimulated vehicle controls.

Immunofluorescence^[1]

Cell Line:

Caco-2 cells treated with DSS
Concentration:

3 μM
Incubation Time:

1 h pretreatment, then 24 h concurrent with DSS
Result:

Retained ZO1 at cell-cell contacts, preventing DSS-induced tight-junction disruption.

In Vivo

Garutadustat (ISM012-042) (1-10 mg/kg; p.o.; daily; 6-9 days) dose-dependently alleviates TNBS-induced murine colitis by restoring intestinal barrier function and reducing gut inflammation^[1].
Garutadustat (1-10 mg/kg; p.o.; daily; 6-9 days) dose-dependently alleviates Oxazolone (HY-126360)-induced murine colitis (a model of T helper 2-driven disease) by reducing gut inflammation and restoring intestinal barrier function, with no systemic effects on EPO or VEGF levels^[1].

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

Animal Model:

BALB/c (female, 8 weeks old, ~19-21 g body weight, TNBS-induced colitis)^[1]
Dosage:

1 mg/kg (prevention mode); 3 mg/kg (prevention mode; therapeutic mode); 10 mg/kg (prevention mode; therapeutic mode)
Administration:

p.o.; daily; 9 days (prevention mode: day -1 to day 7); 6 days (therapeutic mode: day 2 to day 7)
Result:

Reduced disease activity index (DAI) scores to levels comparable to 100 mg/kg mesalamine (3 and 10 mg/kg, prevention mode).
Reduced body weight loss, colon shortening, and colon weight (3 and 10 mg/kg, prevention mode).
Improved colonic histopathology scores (3 and 10 mg/kg, prevention mode).
Dose-dependently increased colon HIF1α staining intensity and mRNA expression of barrier-protective genes Tff3, Tjp1 and Nt5e (prevention mode).
Reduced plasma levels of proinflammatory cytokines IL-6 and TNF (prevention mode).
Reduced fecal lipocalin 2 (LCN2) and calprotectin levels (prevention mode).
Promoted weight gain and ameliorated disease severity within 48 hours (3 and 10 mg/kg, therapeutic mode).
Improved colonic gross pathology (3 and 10 mg/kg, therapeutic mode).
Reduced plasma fluorescein isothiocyanate (FITC)-dextran levels, indicating restored intestinal barrier function (3 and 10 mg/kg, therapeutic mode).
Reduced proportions of colonic lamina propria monocytes, neutrophils, and proinflammatory CD3+ T cell subsets (TNF+, IFNγ+, IL-17A+) relative to vehicle controls (3 and 10 mg/kg, therapeutic mode).

Animal Model:

BALB/c (female, 8 weeks old, ~18-20 g body weight, oxazolone-induced colitis)^[1]
Dosage:

1 mg/kg (prevention mode); 3 mg/kg (prevention mode; therapeutic mode); 10 mg/kg (prevention mode; therapeutic mode)
Administration:

p.o.; daily; 9 days (prevention mode: day -1 to day 7); 6 days (therapeutic mode: day 2 to day 7)
Result:

Dose-dependently prevented body weight loss, improved DAI scores, improved colon density, and reduced fecal LCN2 levels (prevention mode).
Reduced colon tissue levels of proinflammatory chemokines (KC/GRO, MCP1, MIP1α, MIP2) and cytokines (IL-33, IL-5, IL-12p70, TNF) (prevention mode).
Reduced plasma IL-1β levels while leaving systemic EPO and VEGF levels unchanged (prevention mode).
Promoted disease remission, improved DAI scores, reduced plasma FITC-dextran levels (restored intestinal permeability), and normalized colon weight and length relative to vehicle controls (3 and 10 mg/kg, therapeutic mode).

Chemical Information

CAS. Nr. 2924181-80-4
Appearance Solid
Molecular Weight 489.53
Formel C₂₅H₂₇N₇O₄
Color White to off-white
SMILES

CC(C)(OC(N1CCN(C2=CC=C3C(C=NC(C(NCC4=CN=C(C#N)C=C4)=O)=C3O)=N2)CC1)=O)C
Synonyms

ISM012-042
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 25 mg/mL (51.07 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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0428 mL

10.2139 mL

20.4278 mL

5 mM

0.4086 mL

2.0428 mL

4.0856 mL

10 mM

0.2043 mL

1.0214 mL

2.0428 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.11 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.11 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Fu Y, et al. Intestinal mucosal barrier repair and immune regulation with an AI-developed gut-restricted PHD inhibitor. Nat Biotechnol. 2025;43(11):1772-1777. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	2.0428 mL	10.2139 mL	20.4278 mL	51.0694 mL
	5 mM	0.4086 mL	2.0428 mL	4.0856 mL	10.2139 mL
	10 mM	0.2043 mL	1.0214 mL	2.0428 mL	5.1069 mL
	15 mM	0.1362 mL	0.6809 mL	1.3619 mL	3.4046 mL
	20 mM	0.1021 mL	0.5107 mL	1.0214 mL	2.5535 mL
	25 mM	0.0817 mL	0.4086 mL	0.8171 mL	2.0428 mL
	30 mM	0.0681 mL	0.3405 mL	0.6809 mL	1.7023 mL
	40 mM	0.0511 mL	0.2553 mL	0.5107 mL	1.2767 mL
	50 mM	0.0409 mL	0.2043 mL	0.4086 mL	1.0214 mL

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Garutadustat

Alle HIF/HIF Prolyl-Hydroxylase Isoform-spezifische Produkte anzeigen