PF-04634817 |
Katalog-Nr.GC36880
One-Click Copy Product Info
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PF-0463481 ist ein potenter und oral aktiver dualer CCR2/CCR5-Antagonist mit vergleichbarer CCR2-Potenz bei Mensch und Nagetier (IC50 = 20,8 nM bei Ratten) und einer 10- bis 20-fach geringeren CCR5-Potenz bei Nagetieren (IC50 bei Ratte = 470 nM).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1228111-63-4
Sample solution is provided at 25 µL, 10mM.
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PF-0463481, an oral CCR2/5 dual antagonist, with a favorable ocular safety profile versus intravitreal therapies[1]. PF-0463481 is safe and well-tolerated and being developed for the treatment of diabetic nephropathy[2]. CCR2 CCR5
[1]. Gale JD, et al. A CCR2/5 Inhibitor, PF-04634817, Is Inferior to Monthly Ranibizumab in the Treatment of Diabetic Macular Edema. Invest Ophthalmol Vis Sci. 2018 May 1;59(6):2659-2669. [2]. Gale JD, et al. Effect of PF-04634817, an Oral CCR2/5 Chemokine Receptor Antagonist, on Albuminuria in Adults with Overt Diabetic Nephropathy. Kidney Int Rep. 2018 Aug 3;3(6):1316-1327.
| Cas No. | 1228111-63-4 | SDF | |
| Canonical SMILES | O=C(N1[C@@]2([H])C[C@@]([H])(C1)N(C3=NC=NC(C(F)(F)F)=C3)C2)[C@@]4(C[C@@H](CC4)N[C@@H]5[C@@H](COCC5)OC)C(C)C | ||
| Formula | C25H36F3N5O3 | M.Wt | 511.58 |
| Löslichkeit | DMSO: 50 mg/mL (97.74 mM) | 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 | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.9547 mL | 9.7736 mL | 19.5473 mL |
| 5 mM | 390.9 μL | 1.9547 mL | 3.9095 mL |
| 10 mM | 195.5 μL | 977.4 μL | 1.9547 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: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 29 reference(s) in Google Scholar.)