INCB38579 |
Catalog No.GC65937
One-Click Copy Product Info
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INCB38579 is an orally active, highly brain penetrable, and selective histamine H4 receptor (HH4R) antagonist (hH4R IC50=4.8 nM, mH4R IC50=42 nM, rH4R IC50=32 nM). INCB38579 shows anti-inflammatory pain and anti-pruritic activities.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1246207-65-7
Sample solution is provided at 25 µL, 10mM.
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INCB38579 is an orally active, highly brain penetrable, and selective histamine H4 receptor (HH4R) antagonist (hH4R IC50=4.8 nM, mH4R IC50=42 nM, rH4R IC50=32 nM). INCB38579 shows anti-inflammatory pain and anti-pruritic activities[1].
INCB38579 (0.1 nM-10 μM; 1.5 h) inhibits histamine binding to the recombinant human and rodent histamine H4 receptors[1].
INCB38579 (0.1 nM-10 μM; 20 min) blocks histamine-induced migration of dendritic cells differentiated from human monocytes and mouse bone marrow cells[1].
NCB38579 (0-30 nM; 1.5 h) inhibits histamine-induced cell shape change and migration of purified human eosinophils dose-dependently[1].
Cell Viability Assay[1]
| Cell Line: | HEK293 cells |
| Concentration: | 0.1 nM-10 μM |
| Incubation Time: | 1.5 hours |
| Result: | Showed the IC50 values of 4.8, 42 and 21 nM for the human, mouse and rat histamine H4 receptors, respectively. |
Cell Viability Assay[1]
| Cell Line: | Human monocytes, mouse bone marrow cells, and human eosinophils |
| Concentration: | 0.1 nM-10 μM |
| Incubation Time: | 20 min |
| Result: | Showed IC50s of 13.2 and 77 nM for human monocytes and mouse bone marrow cells??respectively. Showed IC50 values of approximately 20-30 nM for purified human eosinophils. |
Cell Viability Assay[1]
| Cell Line: | HEK293 cells |
| Concentration: | 0-30 nM |
| Incubation Time: | 1.5 hours |
| Result: | Showed the IC50 values of 4.8, 42 and 21 nM for the human, mouse and rat histamine H4 receptors, respectively. |
INCB38579 (oral gavage; 100 mg/kg; once) inhibits histamine-mediated pruritus in mice[1].
INCB38579 (oral gavage; 100 mg/kg; once) shows antinociceptive functions in this acute model of inflammatory pain[1].
INCB38579 (oral gavage; 3, 10, 30, and 100 mg/kg; once) inhibits formalin-induced pain in rats and mice[1].
| Animal Model: | Female CD-1 mice histamine-induced pruritus[1] |
| Dosage: | 100 mg/kg |
| Administration: | Oral gavage; 100 mg/kg; once |
| Result: | Reduced the number of scratching bouts significantly (P<0.05). |
| Animal Model: | Sprague-Dawley rats injected with carrageenan[1] |
| Dosage: | 100 mg/kg |
| Administration: | Oral gavage; 100 mg/kg; once |
| Result: | Increased the paw withdrawal threshold from a baseline of 61 g to approximately 100 g, achieving approximately 60% in maximal possible effect. |
| Animal Model: | Male Sprague-Dawley rats and male ICR mice injected with formalin into the hind paws[1] |
| Dosage: | 3, 10, 30, and 100 mg/kg |
| Administration: | Oral gavage; 3, 10, 30, and 100 mg/kg; once |
| Result: | Showed a significant dose-dependent analgesic effect from 10 to 100 mg/kg in the phase 1 response and 30 to 100 mg/kg in the phase 2 response in the mouse formalin test. Observed a dose-dependent and statistically significant effect in the phase 1 response, ranging from10 to 100 mg/kg, in the rat formalin test. |
| Cas No. | 1246207-65-7 | SDF | |
| Formula | C25H34N6O | M.Wt | 434.58 |
| Solubility | DMSO : 230 mg/mL (529.25 mM; ultrasonic and warming and heat to 60°C) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3011 mL | 11.5054 mL | 23.0107 mL |
| 5 mM | 460.2 μL | 2.3011 mL | 4.6021 mL |
| 10 mM | 230.1 μL | 1.1505 mL | 2.3011 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)