Cat. No.: HY-109148

Izencitinib

(Synonyms: TD-1473; JNJ-8398)

고객리뷰

Based on 1 Customer Validation

Izencitinib (TD-1473) is an orally active, non-selective and gut-restricted JAK inhibitor. Izencitinib (TD-1473) can be used in the study for ulcerative colitis.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

Purity: 99.47%
CAS No.: 2051918-33-1
화학식: C₂₂H₂₆N₈
분자량:402.50

보관:

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

Izencitinib Chemical Structure

CAS No.: 2051918-33-1

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Biological Activity
- 제품 설명
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
용액&용해도
- In Vitro
- In Vivo
순도&문서
References
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

Izencitinib (TD-1473) is an orally active, non-selective and gut-restricted JAK inhibitor. Izencitinib (TD-1473) can be used in the study for ulcerative colitis^[1].

All JAK Isoforms :

In Vitro

Izencitinib (TD-1473) inhibits cytokine-evoked STAT phosphorylation in human peripheral blood mononuclear cells (PBMCs) and in a human colonic epithelial cell line (pIC₅₀ ≥ 6.7)^[1].
? Izencitinib (TD-1473) is a potent JAK1, JAK2, JAK3, and TYK2 inhibitor at the human JAK kinase domains (pKi values of 10.0, 10.0, 8.8, and 9.5, respectively)^[1].

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

In Vivo

Izencitinib (TD-1473, 1 mg/kg BID) preserves body weight and reduced occult blood scores in a mouse oxazolone colitis model^[1].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 2051918-33-1
Appearance Solid
분자량 402.50
화학식 C₂₂H₂₆N₈
Color Yellow to orange
SMILES

CC1=CC(NC2=CC3=C(C=CC=N3)C(N[C@@H]4C[C@@H](CC5)N(CCC#N)[C@@H]5C4)=N2)=NN1
Synonyms

TD-1473; JNJ-8398
선적

Room temperature in continental US; may vary elsewhere.

보관

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

용액&용해도

In Vitro:

DMSO : 50 mg/mL (124.22 mM; Need ultrasonic; 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

2.4845 mL

12.4224 mL

24.8447 mL

5 mM

0.4969 mL

2.4845 mL

4.9689 mL

10 mM

0.2484 mL

1.2422 mL

2.4845 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.

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (6.21 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.

Protocol 2

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

Solubility: ≥ 2.5 mg/mL (6.21 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.

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

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 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)

References

[1]. Kevin S Currie, et al. Small-molecule agents for the treatment of inflammatory bowel disease. Bioorg Med Chem Lett. 2019 Aug 15;29(16):2034-2041. [Content Brief]

[2]. William J Sandborn, et al. Development of Gut-Selective Pan-Janus Kinase Inhibitor TD-1473 for Ulcerative Colitis: A Translational Medicine Programme. J Crohns Colitis. 2020 Sep 16;14(9):1202-1213. [Content Brief]

[3]. D. Beattie, et al. TD-1473, a novel, potent, and orally administered, GI-targeted, pan-Janus kinase (JAK) inhibitor. Journal of Crohn's and Colitis, Volume 10, Issue suppl_1, March 2016, Page S123.

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	2.4845 mL	12.4224 mL	24.8447 mL	62.1118 mL
	5 mM	0.4969 mL	2.4845 mL	4.9689 mL	12.4224 mL
	10 mM	0.2484 mL	1.2422 mL	2.4845 mL	6.2112 mL
	15 mM	0.1656 mL	0.8282 mL	1.6563 mL	4.1408 mL
	20 mM	0.1242 mL	0.6211 mL	1.2422 mL	3.1056 mL
	25 mM	0.0994 mL	0.4969 mL	0.9938 mL	2.4845 mL
	30 mM	0.0828 mL	0.4141 mL	0.8282 mL	2.0704 mL
	40 mM	0.0621 mL	0.3106 mL	0.6211 mL	1.5528 mL
	50 mM	0.0497 mL	0.2484 mL	0.4969 mL	1.2422 mL
	60 mM	0.0414 mL	0.2070 mL	0.4141 mL	1.0352 mL
	80 mM	0.0311 mL	0.1553 mL	0.3106 mL	0.7764 mL
	100 mM	0.0248 mL	0.1242 mL	0.2484 mL	0.6211 mL

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Izencitinib

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All JAK Isoforms

Biological Activity

Chemical Information

용액&용해도

순도&문서

References

Help & FAQs

Complete Stock Solution Preparation Table

Izencitinib Related Classifications

HY-109148 Related Classifications