PF-3893787 hydrochloride (Synonyms: PF-3893787 hydrochloride) |
| رقم الكتالوجGC31790 |
هيدروكلوريد PF-3893787 (PF-3893787 هيدروكلوريد) هو ألفة ربط جديدة لمناهض مستقبلات الهيستامين H4 (Ki = 2.4 نانومتر) وهو أيضًا مضاد وظيفي (Ki = 1.56 نانومتر).
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Cas No.: 2096455-90-0
Sample solution is provided at 25 µL, 10mM.
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PF-3893787 hydrochloride is a novel histamine H4 receptor antagonist binding affinity (Ki=2.4 nM) and is also a functional (Ki=1.56 nM) antagonist.
PF-3893787 is tested and observed binding Ki=2.4 nM and functional Ki=1.56 nM for H4R. Data from functional assays produce convergent projections of the free plasma efficacious concentration and PF-3893787 (Compound 13) is fast on/fast off on rhH4R. The in vitro IC50 on human native isolated eosinophils assessing actin polymerisation is 1.16 nM and assuming need 10 times the IC50 for >90% receptor occupancy (and therefore near complete inhibition of the response) suggested a concentration of 12 nM. The data in the whole blood GAFS assay demonstrates that the imetit induced shape change is completely blocked at a total blood concentration of 30 nM (which correcting for PPB and blood partitioning equates to approximately 10 nM free). For the purpose of dose projection and safety margin calculation, a Ceff/Cmin concentration of 10-15 nM is used[1].
[1]. Mowbray CE, et al. Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: a novel histamine H4 receptor antagonist. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6596-602.
| Cas No. | 2096455-90-0 | SDF | |
| المرادفات | PF-3893787 hydrochloride | ||
| Canonical SMILES | NC1=NC(N2C[C@H](NC)CC2)=CC(NCC3CC3)=N1.[H]Cl.[H]Cl.[H]Cl | ||
| Formula | C13H25Cl3N6 | M.Wt | 371.74 |
| الذوبان | DMSO : ≥ 83.33 mg/mL (224.16 mM) | Storage | Store at 2-8°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 | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.6901 mL | 13.4503 mL | 26.9005 mL |
| 5 mM | 0.538 mL | 2.6901 mL | 5.3801 mL |
| 10 mM | 0.269 mL | 1.345 mL | 2.6901 mL |
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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 ddH2O, 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.
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3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 1 reference(s) in Google Scholar.)
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