| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| 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 |
| CAS # |
2756222-90-7
|
|---|---|
| Appearance |
Typically exists as solid at room temperature
|
| 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)
|
| 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
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *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). View More
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)] 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). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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