Art. -Nr.: HY-147276

Izuforant

(Synonyms: JW1601)

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Izuforant (JW1601) (Compound 24) is an orally active histamine H4 receptor (H4R) antagonist with an IC₅₀ of 36 nM against human H4R. Izuforant also shows binding affinity of human serotonin 3 receptor (h5-HT3R) with an IC₅₀ of 9.1 μM. Izuforant exhibits strong anti-pruritic and anti-inflammatory efficacies.

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Reinheit: 98.88%
CAS. Nr.: 1429374-83-3
Formel: C₁₂H₁₂BrN₇
Molecular Weight:334.17

Speicherung:

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

Izuforant Chemical Structure

CAS. Nr.: 1429374-83-3

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

Human H₄ Receptor

36 nM (IC₅₀)

h5-HT3R

9.1 μM (IC₅₀)

Alle Histamine Receptor Isoform-spezifische Produkte anzeigen :

In Vitro

Izuforant (JW1601) (Compound 24) shows metabolic stability with CL_h,int values of 3.05 and 1.33 mL/min/mg in mouse and human, respectively^[1].

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

In Vivo

Izuforant (JW1601) (50 mg/kg; p.o.; once) decreases histamine-and substance P-induced itching in mice^[1].
Izuforant (100 mg/kg; p.o.; twice a day for 3 weeks) inhibits oxazolone-induced atopic dermatitis in mice^[1].

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

Animal Model:

Female, ICR mice (8 weeks old)^[1]
Dosage:

50 mg/kg
Administration:

Oral administration, once
Result:

Decreased histamine-and substance P-induced itching.

Animal Model:

Female, Balb/c mice (6 weeks old, 20±3 g)^[1]
Dosage:

100 mg/kg
Administration:

Oral administration, twice a day for 3 weeks
Result:

Inhibited oxazolone-induced atopic dermatitis (51.2% inhibition).

Animal Model:

ICR mouse (20~30 g) and SD rat (200~300 g)^[1]
Dosage:

50 mg/kg for mice and 10 mg/kg for rats
Administration:

Oral administration (Pharmacokinetic Analysis)

Result:

Pharmacokinetics parameter of Izuforant (Compound 24)^[1]

Compound		Mouse			Rat
	t_1/2 (h)	C_max (μg/mL)	AUC_inf (μg•hr/mL)	t_1/2 (h)	C_max (μg/mL)	AUC_inf (μg•hr/mL)
Izuforant	0.96	18.87	32.17	1.30	2.42	4.51

Chemical Information

CAS. Nr. 1429374-83-3
Appearance Solid
Molecular Weight 334.17
Formel C₁₂H₁₂BrN₇
Color Off-white to light green
SMILES

CNC1CN(C2=NC3=NC=C(Br)C=C3N4C2=NN=C4)C1
Synonyms

JW1601
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 : 100 mg/mL (299.25 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

2.9925 mL

14.9624 mL

29.9249 mL

5 mM

0.5985 mL

2.9925 mL

5.9850 mL

10 mM

0.2992 mL

1.4962 mL

2.9925 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: 5 mg/mL (14.96 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

This protocol yields a clear solution of 5 mg/mL.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (14.96 mM); Clear solution

This protocol yields a clear solution of ≥ 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 (50.0 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 (276 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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]. Pil Su Ho, et al. Novel heterocyclic derivatives and their uses. WO2013048214A2.

[2]. Jin M, et al. From Bench to Clinic: the Potential of Therapeutic Targeting of the IL-22 Signaling Pathway in Atopic Dermatitis. Immune Netw. 2018 Dec 19;18(6):e42. [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	2.9925 mL	14.9624 mL	29.9249 mL	74.8122 mL
	5 mM	0.5985 mL	2.9925 mL	5.9850 mL	14.9624 mL
	10 mM	0.2992 mL	1.4962 mL	2.9925 mL	7.4812 mL
	15 mM	0.1995 mL	0.9975 mL	1.9950 mL	4.9875 mL
	20 mM	0.1496 mL	0.7481 mL	1.4962 mL	3.7406 mL
	25 mM	0.1197 mL	0.5985 mL	1.1970 mL	2.9925 mL
	30 mM	0.0997 mL	0.4987 mL	0.9975 mL	2.4937 mL
	40 mM	0.0748 mL	0.3741 mL	0.7481 mL	1.8703 mL
	50 mM	0.0598 mL	0.2992 mL	0.5985 mL	1.4962 mL
	60 mM	0.0499 mL	0.2494 mL	0.4987 mL	1.2469 mL
	80 mM	0.0374 mL	0.1870 mL	0.3741 mL	0.9352 mL
	100 mM	0.0299 mL	0.1496 mL	0.2992 mL	0.7481 mL

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Izuforant

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

Neuronal Signaling Compound Library

Orally Active Compound Library

Neurotransmitter Receptor Compound Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Anti-Obesity Compound Library

Coagulation and Anti-coagulation Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Alle Histamine Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Izuforant

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

Neuronal Signaling Compound Library

Orally Active Compound Library

Neurotransmitter Receptor Compound Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Anti-Obesity Compound Library

Coagulation and Anti-coagulation Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Alle Histamine Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Izuforant Related Classifications

HY-147276 Related Classifications