Physicochemical Properties
| CAS # | 2756222-90-7 |
| Appearance | Off-white to pink solid powder |
| HS Tariff Code | 2934.99.9001 |
| Storage |
Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition | Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs) |
Biological Activity
| Targets | H1 Receptor 24.12 nM (IC50) mAChR3 |
| ln Vitro | HY-078020 has strong inhibitory activity on H1R (IC50 is 24.12 nM), but weak inhibitory effect on M3R and hERG, with IC50 of >10 and 17.6 μM respectively [1]. HY-078020 has moderate permeability (efflux rate <2), liver microsomal stability, and exhibits a long half-life in humans, beagle dogs, and mice (T1/2 = 86.625 min) [1]. HY-078020 has an inhibitory effect on rat cytochrome P450 (CYP) isoenzyme CYP3A4 [1]. |
| ln Vivo | HY-078020 (5 mg/kg, oral administration) inhibited histamine-induced skin vasodilation and capillary permeability in ICR/KM mice, with a vascular permeability inhibition rate of 58.71%[1]. HY-078020 (10 mg/kg, intravenous injection) showed weak anticholinergic activity, with a 10.8% inhibition rate on saliva secretion in Wistar 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 - |
| Animal Protocol |
Animal/Disease Models: histamine-induced vascular permeability in ICR and Kunming mice[1] Doses: 5 mg/kg Route of Administration: i.g. Experimental Results: Reduced the vascular permeability with an inhibition rate of 58.71%. Animal/Disease Models: Wistar mice[1] Doses: 10 mg/kg Route of Administration: i.v., once a day Experimental Results: Inhibited salivary secretion with an inhibition rate of 10.8%. |
| References |
[1].Discovery of the novel and potent histamine H1 receptor antagonists for treatment of allergic diseases. Eur J Med Chem. 2024 Feb 3;268:116197. |
Solubility Data
| Solubility (In Vitro) | Typically soluble in DMSO (e.g. 10 mM) |
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples. Injection Formulations (e.g. IP/IV/IM/SC) Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] *Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline) Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline) Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline) Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil) Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Oral Formulations Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). Oral Formulation 3: Dissolved in PEG400 Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose Oral Formulation 6: Mixing with food powders Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently. (Please use freshly prepared in vivo formulations for optimal results.) |