| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
Histamine binding to recombinant codont-bearing histamine H4 receptors is inhibited by INCB38579 (0.1 nM-10 μM; 1.5 hours) [1]. The human eosinophil migration produced by histamine is blocked by INCB38579 (0.1 nM-10 μM; 20 min). Human eosinophil movement is inhibited and histamine-induced alterations in cell shape are blocked in a dose-dependent manner by NCB38579 (0-30 nM; 1.5 h) [1].
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| ln Vivo |
INCB38579, a bacteriostatic histamine-mediated anesthetic pruritus treatment (chamber gavage; 100 mg/kg; once) [1]. In this acute model of narcotic pain, mice Formalin-induced pain function and fluorescence adsorption are used to study INCB38579 (chamber gavage; 100 mg/kg; once) [1].
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| Cell Assay |
Cell Viability Assay [1]
Cell Types: HEK293 cells Tested Concentrations: 0.1 nM-10 μM Incubation Duration: 1.5 hrs (hours) Experimental Results: Shows IC50 values for human, mouse and rat histamine H4 receptors of 4.8, 42 and 21 nM, respectively. Cell viability assay[1] Cell Types: human monocytes, mouse bone marrow cells and human eosinophils Tested Concentrations: 0.1 nM-10 μM Incubation Duration: 20 minutes Experimental Results: IC50 of human monocytes and mouse bone marrow cells respectively are 13.2 and 77 nM, respectively. The IC50 value of purified human eosinophils was shown to be approximately 20-30 nM. Cell viability assay [1] Cell Types: HEK293 Cell Tested Concentrations: 0-30 nM Incubation Duration: 1.5 hrs (hours) Experimental Results: IC50 values for human, mouse and rat histamine H4 receptors were 4.8, 42 and 21 nM respectively. |
| Animal Protocol |
Animal/Disease Models: Female. Itching caused by histamine in CD-1 mice [1]
Doses: 100 mg/kg Route of Administration: po (oral gavage); 100 mg/kg; one-time Experimental Results:Dramatically diminished scratching times (P<0.05). Animal/Disease Models: SD (SD (Sprague-Dawley)) rats injected with carrageenan [1] Doses: 100 mg/kg Route of Administration: po (oral gavage); 100 mg/kg; Experimental Results: Increased paw withdrawal threshold from baseline of 61 g to approx. 100 g, achieving approximately 60% of the maximum possible effect. Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rats and male ICR mice were injected with formalin in the hind paws [1] Doses: 3, 10, 30 and 100 mg/kg Route of Administration: po (oral gavage); 3, 10, 30 and 100 mg/kg; Experimental Results: In the mouse formalin test, 10 to 100 mg/kg in the first phase response and 30 to 100 mg/kg in the second phase response demonstrated significant dose-dependent antidote. pain effect. In the rat formalin test, a dose-dependent and statistically significant phase 1 response was observed at 10 to 100 mg/kg. |
| References |
| Molecular Formula |
C25H34N6O
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|---|---|
| Molecular Weight |
434.577064990997
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| Exact Mass |
434.279
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| CAS # |
1246207-65-7
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| PubChem CID |
59496762
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
3.2
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
32
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| Complexity |
632
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(=O)(N1CCC2=C(C1)C=C(C1C=C(N3CCN(C)CC3)N=C(N)N=1)C=C2)CC1CCCC1
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| InChi Key |
LZOCXAJJOQPLKB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H34N6O/c1-29-10-12-30(13-11-29)23-16-22(27-25(26)28-23)20-7-6-19-8-9-31(17-21(19)15-20)24(32)14-18-4-2-3-5-18/h6-7,15-16,18H,2-5,8-14,17H2,1H3,(H2,26,27,28)
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| Chemical Name |
1-[7-[2-amino-6-(4-methylpiperazin-1-yl)pyrimidin-4-yl]-3,4-dihydro-1H-isoquinolin-2-yl]-2-cyclopentylethanone
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ~230 mg/mL (~529.25 mM)
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| 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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3011 mL | 11.5054 mL | 23.0107 mL | |
| 5 mM | 0.4602 mL | 2.3011 mL | 4.6021 mL | |
| 10 mM | 0.2301 mL | 1.1505 mL | 2.3011 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
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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