HY-078020
Based on 1 Customer Validation
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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- Pureté: 98.87%
- CAS No.: 2756222-90-7
- Formule: C32H35ClN2O2
- Masse moléculaire:515.09
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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H1 Receptor 24.12 nM (IC50) |
mAChR3 |
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.
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.
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Animal Model:histamine-induced vascular permeability in ICR and Kunming mice[1]
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Dosage:5 mg/kg
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Administration:i.g.
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Result:Reduced the vascular permeability with an inhibition rate of 58.71%.
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Animal Model:Wistar mice[1]
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Dosage:10 mg/kg
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Administration:i.v., once a day
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Result:Inhibited salivary secretion with an inhibition rate of 10.8%.
Chemical Information
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CAS No. 2756222-90-7
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Appearance Solid
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Masse moléculaire 515.09
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Formule C32H35ClN2O2
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Color Off-white to pink
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SMILES
ClC(C=C1)=CC(CCC2=C/3N=CC=C2)=C1C3=C4CCN(CCCC5=CC(C(C)(C(O)=O)C)=CC=C5)CC/4
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureté et documentation
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Fiche technique (276 KB)
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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)
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Instruction de manipulation (2659 KB)
Références
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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