Cat. No.: HY-124686

ER-464195-01

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ER-464195-01 is an orally active calreticulin (CRT) and integrin α subunits (ITGAs) binding inhibitor. ER-464195-01 inhibits leukocyte infiltration and subsequent inflammatory cascade reactions by dissociating the binding between CRT and ITGA. ER-464195-01 down-regulates the expression of pro-inflammatory genes (such as TNF-α, IL-1β, IL-6, IL-17f) induced by DSS (HY-116282C), and inhibit the phosphorylation of STAT3 and the production of serum amyloid A (SAA). ER-464195-01 can be used for the study of inflammatory bowel disease (IBD).

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Pureté: 99.72%
CAS No.: 859218-37-4
Formule: C₂₃H₃₉ClN₂
Masse moléculaire:379.02

Stockage:

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

ER-464195-01 Chemical Structure

CAS No.: 859218-37-4

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Fluorescent Dye

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

Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Solvant et solubilité
- In Vitro
Pureté et documentation
Références
Help & FAQs
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]

STAT3

IL-1β

IL-6

IL-17F

Voir tous les produits spécifiques à Isoform STAT :

Voir tous les produits spécifiques à Isoform Interleukin Related :

Voir tous les produits spécifiques à Isoform TNF Receptor :

In Vitro

ER-464195-01 (5 μM) effectively inhibits the interaction between CRT and ITGA4 within the Jurkat cells and significantly reduces the level of CRT on the cell surface^[1].
ER-464195-01 (0.01-10 μM, 60 min) inhibits the adhesion ability of VCAM-1 cells stimulated by PMA (HY-18739) and ICAM-1 cells stimulated by fMLP (HY-P0224), with IC₅₀ values of 0.15 μM and 0.19 μM respectively, and has no inhibitory effect under MnCl₂ stimulation^[1].

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

In Vivo

ER-464195-01 (5-10 mg/kg, p.o., once daily for 6-32 days) ameliorates the severity of diseases in IBD mouse models through both prophylactic and therapeutic administration^[1].

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

Animal Model:

DSS induced IBD model established in female Balb/c mice (9- to 10-week-old)^[1]
Dosage:

10 mg/kg (preventive administration) and 5 mg/kg (therapeutic administration)
Administration:

Oral administration (p.o.), once daily for 6-7 days
Result:

Effectively alleviated the weight loss, increased DAI, and shortened colon in mice under both administration methods.
Reduced the interaction signal between CRT and ITGA4.
Inhibited the upregulation of key pro-inflammatory cytokine mRNAs such as TNF-α, IL1-b, IL-6, and IL-17f induced by DSS.
Inhibited the phosphorylation of STAT3 (p-STAT3) induced by DSS and the production of serum amyloid A (SAA).

Animal Model:

CD4+CD45RB^high T-cell transfer model established in female Balb/c mice (6-week-old)^[1]
Dosage:

10 mg/kg
Administration:

Oral administration (p.o.), once daily for 32 days
Result:

Significantly improved the weight loss in mice and the changes in their fecal characteristics (diarrhea).

Chemical Information

CAS No. 859218-37-4
Appearance Solid
Masse moléculaire 379.02
Formule C₂₃H₃₉ClN₂
Color White to off-white
SMILES

CC1(C)CC(C)(C)CC(C2=CC=CC=C2N3CCN(CCC)CC3)C1.Cl
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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

Solvant et solubilité

In Vitro:

DMSO : 5 mg/mL (13.19 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

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.6384 mL

13.1919 mL

26.3838 mL

5 mM

0.5277 mL

2.6384 mL

5.2768 mL

10 mM

0.2638 mL

1.3192 mL

2.6384 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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (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)
Instruction de manipulation (2659 KB)

Références

[1]. Ohkuro M, et al. Calreticulin and integrin alpha dissociation induces anti-inflammatory programming in animal models of inflammatory bowel disease. Nat Commun. 2018 May 17;9(1):1982. [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	2.6384 mL	13.1919 mL	26.3838 mL	65.9596 mL
	5 mM	0.5277 mL	2.6384 mL	5.2768 mL	13.1919 mL
	10 mM	0.2638 mL	1.3192 mL	2.6384 mL	6.5960 mL

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ER-464195-01

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Lactylation Compound Library

Voir tous les produits spécifiques à Isoform STAT

Voir tous les produits spécifiques à Isoform Interleukin Related

Voir tous les produits spécifiques à Isoform TNF Receptor

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

ER-464195-01 Related Classifications

Cat. No.: HY-124686