1. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  2. Histamine Receptor mAChR
  3. HY-078020

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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HY-078020 Chemical Structure

HY-078020 Chemical Structure

CAS No. : 2756222-90-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
25 mg In-stock
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100 mg   Get quote  

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Description

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[1].

IC50 & Target

H1 Receptor

24.12 nM (IC50)

mAChR3

 

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) T1/2 (h) Tmax (h) Cmax (ng/mL) AUC0-t (ng·h/mL) AUC0-inf (ng·h/mL) Vd (L/kg) CL (mL/h/kg) MRT0-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%.
Molecular Weight

515.09

Formula

C32H35ClN2O2

CAS No.
Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9414 mL 9.7070 mL 19.4141 mL
5 mM 0.3883 mL 1.9414 mL 3.8828 mL
View the Complete Stock Solution Preparation Table

* 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.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* 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.

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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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
HY-078020
Cat. No.:
HY-162231
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