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BIRT-377

Name: BIRT-377
Brand: TargetMol
SKU: T23796
Price: 50 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T23796Cas No. 213211-10-0

Alias BIRT377, BIRT 377

BIRT-377 is a negative allosteric and orally bioavailable inhibitor of ICAM-1 and LFA-1(Ki = 25.8 nM). BIRT-377 inhibits the production of IL-2 and can be used in studies about inflammatory and immune disorders.

BIRT-377

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Purity: 99.93%

Catalog No. T23796Alias BIRT377, BIRT 377Cas No. 213211-10-0

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$50	In Stock	In Stock
5 mg	$122	In Stock	In Stock
10 mg	$197	In Stock	In Stock
25 mg	$455	In Stock	In Stock
50 mg	$672	In Stock	In Stock
100 mg	$956	-	In Stock
500 mg	$1,920	6-8 weeks	6-8 weeks

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.93%

Appearance:Solid

Color:White

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COA LCMS HNMR

Product Introduction

BIRT-377 AI Summary

BIRT-377 is a potent inhibitor of leukocyte function-associated antigen-1 (LFA-1) with critical bioactivities including an IC50 of 26.0 nM in HSB-2 human lymphoblast and H1HeLa cell adhesion assays. It has a dissociation constant (Kd) of 20.0 nM in LFA-1/ICAM-1 binding assays and inhibits aggregation of JY cells with an IC50 of 240.0 nM. Furthermore, it demonstrates irreversible binding to human liver microsomes with an activity rate of 141.0 pM/min/mg. Additionally, BIRT-377 shows antiviral activity against SARS-CoV-2, reducing cytotoxicity in Caco-2 and VERO-6 cells at a concentration of 10 µM, though with modest inhibition rates of 7.96% and 1.85% respectively, and an IC50 value greater than 20,000.0 nM, indicating limited potency as an antiviral agent. This compound also exhibits HDAC6 inhibition, showing 18.99% inhibition in an enzyme assay using a commercial peptide substrate, but less activity with a custom substrate at -0.75% inhibition..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	BIRT-377 is a negative allosteric and orally bioavailable inhibitor of ICAM-1 and LFA-1(Ki = 25.8 nM). BIRT-377 inhibits the production of IL-2 and can be used in studies about inflammatory and immune disorders.
Synonyms	BIRT377, BIRT 377

Chemical Properties

Molecular Weight	442.13
Formula	C₁₈H₁₅BrCl₂N₂O₂
Cas No.	213211-10-0
Smiles	CN1C(=O)N(C(=O)[C@@]1(C)Cc1ccc(Br)cc1)c1cc(Cl)cc(Cl)c1
Relative Density.	1.552 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 90 mg/mL (203.56 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.2618 mL	11.3089 mL	22.6178 mL	113.0889 mL
5 mM	0.4524 mL	2.2618 mL	4.5236 mL	22.6178 mL
10 mM	0.2262 mL	1.1309 mL	2.2618 mL	11.3089 mL
20 mM	0.1131 mL	0.5654 mL	1.1309 mL	5.6544 mL
50 mM	0.0452 mL	0.2262 mL	0.4524 mL	2.2618 mL
100 mM	0.0226 mL	0.1131 mL	0.2262 mL	1.1309 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc