Cat. No.: HY-121356

Carebastine

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Carebastine is an Ebastine (HY-B0674) metabolite and H1-receptor antagonist. Carebastine inhibits VEGFR-2 and Akt phosphorylation. Carebastine exerts an anti-inflammatory effect by inhibiting MIF as well as TNF-α and IL-6 production. Carebastine shows anti-angiogenic activity

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Pureté: 99.23%
CAS No.: 90729-42-3
Formule: C₃₂H₃₇NO₄
Masse moléculaire:499.64

Stockage:

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

Carebastine Chemical Structure

CAS No.: 90729-42-3

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Fluorescent Dye

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

Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Publications (1)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[2]^[1]

H₁ Receptor

VEGFR2

IL-6

Voir tous les produits spécifiques à Isoform Histamine Receptor :

Voir tous les produits spécifiques à Isoform VEGFR :

Voir tous les produits spécifiques à Isoform Akt :

Voir tous les produits spécifiques à Isoform Interleukin Related :

In Vitro

Carebastine (0.01-30 μM; 24-72 h) inhibits VEGF-induced proliferation of HUVECs and HPAECs in a dose-dependent manner^[1].
Carebastine (1-20 μM; 18 h) inhibits VEGF-induced capillary network formation by HUVECs and HPAECs in a dose-dependent manner, causing 70-86% reduction in topological parameters at 20 μM^[1].
Carebastine (10-20 μM; 5 min-24 h) inhibits VEGF-induced phosphorylation of VEGFR-2 and Akt in HUVECs and HPAECs in a time- and dose-dependent manner^[1].
Carebastine (0.1-10 μmol/L; 24 h) dose-dependently reduces MIF protein secretion in costimulated human peripheral blood mononuclear cells^[2].

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

Cell Proliferation Assay^[1]

Cell Line:

human umbilical vein endothelial cells (HUVECs), human pulmonary artery endothelial cells (HPAECs)
Concentration:

0.01-30 μM
Incubation Time:

24 h, 48 h, 72 h
Result:

Inhibited HUVEC proliferation by 42% (48 h, p ≤ 0.03) and 64% (72 h, p ≤ 0.01) at 20 μM.
Inhibited HPAEC proliferation by 62% (48 h, p ≤ 0.03) and 75% (72 h, p ≤ 0.01) at 20 μM.
Inhibited HUVEC proliferation by 65% (72 h) at 30 μM.
Inhibited HPAEC proliferation by 80% (72 h) at 30 μM.

Chemical Information

CAS No. 90729-42-3
Appearance Solid
Masse moléculaire 499.64
Formule C₃₂H₃₇NO₄
Color White to light yellow
SMILES

O=C(CCCN1CCC(OC(C2=CC=CC=C2)C3=CC=CC=C3)CC1)C4=CC=C(C=C4)C(C)(C(O)=O)C
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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

Publications (1)

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Bioorg Chem

Identification of FTY720 and COH29 as novel topoisomerase I catalytic inhibitors by experimental and computational studies. [Abstract]

2024 Jun:147:107412. PMID: 38696845

Solvant et solubilité

In Vitro:

DMF : 25 mg/mL (50.04 mM; Need ultrasonic and warming)

DMSO : 2 mg/mL (4.00 mM; Need ultrasonic and warming; 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

2.0014 mL

10.0072 mL

20.0144 mL

5 mM

0.4003 mL

2.0014 mL

4.0029 mL

10 mM

0.2001 mL

1.0007 mL

2.0014 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)

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 (5.00 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

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 (5.00 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

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 3

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

Solubility: ≥ 2.5 mg/mL (5.00 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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (273 KB)
SDS (420 KB)
- English - EN (420 KB)
- Français - FR (420 KB)
- Deutsch - DE (420 KB)
- Norwegian - NO (420 KB)
- Español - ES (420 KB)
- Swedish - SV (420 KB)
- Italian - IT (420 KB)
- Korean - KR (420 KB)
- Portuguese - PT (420 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]. De Luisi A, et al. Anti-angiogenic activity of carebastine: a plausible mechanism affecting airway remodelling. Eur Respir J. 2009;34(4):958-966. [Content Brief]

[2]. Zhao Y, et al. Carebastine, an H1-receptor antagonist, suppresses the expression of macrophage migration inhibitory factor. Clin Exp Dermatol. 2008 Nov;33(6):785-7.

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 / DMF	1 mM	2.0014 mL	10.0072 mL	20.0144 mL	50.0360 mL
DMF	5 mM	0.4003 mL	2.0014 mL	4.0029 mL	10.0072 mL
	10 mM	0.2001 mL	1.0007 mL	2.0014 mL	5.0036 mL
	15 mM	0.1334 mL	0.6671 mL	1.3343 mL	3.3357 mL
	20 mM	0.1001 mL	0.5004 mL	1.0007 mL	2.5018 mL
	25 mM	0.0801 mL	0.4003 mL	0.8006 mL	2.0014 mL
	30 mM	0.0667 mL	0.3336 mL	0.6671 mL	1.6679 mL
	40 mM	0.0500 mL	0.2502 mL	0.5004 mL	1.2509 mL
	50 mM	0.0400 mL	0.2001 mL	0.4003 mL	1.0007 mL

Keywords

Carebastine

1 Cited Publications

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Carebastine

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Publications Citing Use of MedChemExpress (MCE) Carebastine

Voir tous les produits spécifiques à Isoform Histamine Receptor

Voir tous les produits spécifiques à Isoform VEGFR

Voir tous les produits spécifiques à Isoform Akt

Voir tous les produits spécifiques à Isoform Interleukin Related

Activité biologique

Chemical Information

Publications (1)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Carebastine Related Classifications

HY-121356 Related Classifications