Art. -Nr.: HY-162231

HY-078020

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HY-078020 (compound III-4) is a selective, orally active antagonist for histamine H1 receptor with an IC₅₀ of 24.12 nM. HY-078020 exhibits an anti-inflammatory effect in allergic diseases.

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Reinheit: 98.87%
CAS. Nr.: 2756222-90-7
Formel: C₃₂H₃₅ClN₂O₂
Molecular Weight:515.09

Speicherung:

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

HY-078020 Chemical Structure

CAS. Nr.: 2756222-90-7

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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

H₁ Receptor

24.12 nM (IC₅₀)

mAChR3

Alle Histamine Receptor Isoform-spezifische Produkte anzeigen :

Alle mAChR Isoform-spezifische Produkte anzeigen :

In Vitro

HY-078020 reveals a potent inhibitory activity towards H1R (IC₅₀ is 24.12 nM) and weak inhibition against M3R and hERG, with IC₅₀s of >10 and 17.6 μM, respectively^[1].
HY-078020 exhibits moderate permeability (efflux ratio rate <2), liver microsomes stability with long half-life in human, beagles and mice (T1/2 = 86.625 min) ^[1].
HY-078020 exhibits inhibitory activity against cytochrome P450 (CYP) isozymes CYP3A4 of rates^[1].

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

In Vivo

HY-078020 (5 mg/kg, i.g.) inhibits the histamine induced skin vasodilation and capillary permeability in ICR/KM mice, with a vascular permeability inhibition rates of 58.71 %^[1].
HY-078020 (10 mg/kg, i.v.) exhibits aweak anticholinergic activity with an inhibition rate of salivary secretion of 10.8% in Wistar mice^[1].
HY-078020 reveals a pharmacokinetic profils in mice^[1]:

Pharmacokinetic Analysis of HY-078020 in wistar male rats^[1]

route	Dose (mg/kg)	T_1/2 (h)	T_max (h)	C_max (ng/mL)	AUC_0-t (ng·h/mL)	AUC_0-inf (ng·h/mL)	V_d (L/kg)	CL (mL/h/kg)	MRT_0-inf(h)	F (%)
iv	4	0.653 ± 0.12	-	-	1678 ± 152.59	1822.38 ± 224.97	1.77 ± 0.22	37.00 ± 4.62	0.70 ± 0.14	59.55
po	25	4.05 ± 0.81	0.38 ± 0.16	1722.06 ± 337.11	6246.92 ± 1443.28	7209.70 ± 1419.01	21.26 ± 7.42	59.35 ± 10.59	6.01 ± 1.42	-

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

Animal Model:

histamine-induced vascular permeability in ICR and Kunming mice^[1]
Dosage:

5 mg/kg
Administration:

i.g.
Result:

Reduced the vascular permeability with an inhibition rate of 58.71%.

Animal Model:

Wistar mice^[1]
Dosage:

10 mg/kg
Administration:

i.v., once a day
Result:

Inhibited salivary secretion with an inhibition rate of 10.8%.

Chemical Information

CAS. Nr. 2756222-90-7
Appearance Solid
Molecular Weight 515.09
Formel C₃₂H₃₅ClN₂O₂
Color Off-white to pink
SMILES

ClC(C=C1)=CC(CCC2=C/3N=CC=C2)=C1C3=C4CCN(CCCC5=CC(C(C)(C(O)=O)C)=CC=C5)CC/4
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 (194.14 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

1.9414 mL

9.7070 mL

19.4141 mL

5 mM

0.3883 mL

1.9414 mL

3.8828 mL

10 mM

0.1941 mL

0.9707 mL

1.9414 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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 6.25 mg/mL (12.13 mM); Clear solution

This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 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: ≥ 6.25 mg/mL (12.13 mM); Clear solution

This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 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: ≥ 6.25 mg/mL (12.13 mM); Clear solution

This protocol yields a clear solution of ≥ 6.25 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 (62.5 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]. Chu Z, et al., Discovery of the novel and potent histamine H1 receptor antagonists for treatment of allergic diseases. Eur J Med Chem. 2024 Feb 3;268:116197. [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	1.9414 mL	9.7070 mL	19.4141 mL	48.5352 mL
	5 mM	0.3883 mL	1.9414 mL	3.8828 mL	9.7070 mL
	10 mM	0.1941 mL	0.9707 mL	1.9414 mL	4.8535 mL
	15 mM	0.1294 mL	0.6471 mL	1.2943 mL	3.2357 mL
	20 mM	0.0971 mL	0.4854 mL	0.9707 mL	2.4268 mL
	25 mM	0.0777 mL	0.3883 mL	0.7766 mL	1.9414 mL
	30 mM	0.0647 mL	0.3236 mL	0.6471 mL	1.6178 mL
	40 mM	0.0485 mL	0.2427 mL	0.4854 mL	1.2134 mL
	50 mM	0.0388 mL	0.1941 mL	0.3883 mL	0.9707 mL
	60 mM	0.0324 mL	0.1618 mL	0.3236 mL	0.8089 mL
	80 mM	0.0243 mL	0.1213 mL	0.2427 mL	0.6067 mL
	100 mM	0.0194 mL	0.0971 mL	0.1941 mL	0.4854 mL

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HY-078020

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

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

Alle mAChR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

HY-078020

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

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

Alle mAChR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

HY-078020 Related Classifications

HY-162231 Related Classifications