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BOC Sciences
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Product Name:PF-04634817 succinate
CAS:2140301-98-8
Purity:>=95% Remarks:Reach out to us for more information about custom solutions.
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| Company Name: |
cjbscvictory
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13348960310 13348960310 |
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3003867561@qq.com |
| Products Intro: |
Product Name:PF-04634817 succinate
CAS:2140301-98-8
Purity:98% Package:5mg；10mg；20mg；50mg；100mg；200mg
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PF-04634817 succinate manufacturers
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| | PF-04634817 succinate Basic information |
| | PF-04634817 succinate Chemical Properties |
| storage temp. | room temp | | solubility | DMSO: 2mg/mL, clear | | form | Solid | | color | White to off-white | | InChIKey | MCRWZBYTLVCCJJ-DKALBXGISA-N | | SMILES | CO[C@H]1[C@@H](N[C@@H]2CC[C@@](C(N3C[C@@]4([H])N(C5=NC=NC(C(F)(F)F)=C5)C[C@]3([H])C4)=O)(C(C)C)C2)CCOC1 |
| WGK Germany | WGK 3 | | Storage Class | 11 - Combustible Solids |
| | PF-04634817 succinate Usage And Synthesis |
| Uses | PF-0463481 succinate is a potent and orally active dual CCR2/CCR5 antagonist with comparable human and rodent CCR2 potency (rat IC50=20.8 nM), and displays 10-20 fold less rodent CCR5 potency (rat IC50=470 nM). PF-0463481 succinate is safe and well-tolerated and has the potential for the study of diabetic nephropathy[3]. | | Biological Activity | Orally available, potent and selective CCR2/5 receptor antagonist | | in vivo | PF-04634817 succinate (oral administration; 30 mg/kg; once daily; 31 days intervention (weeks 2-15 after Streptozotocin )) intervention at the onset of diabetes (week 2) has no impact on the fasting blood glucose levels in diabetic Nos3-/- 221 mice. The development of diabetes results in a marked increase in the levels of glycated haemoglobin (HbA1c) in Nos3-/- mice. Early intervention with PF-04634817 induces an additional increase in glycated hemoglobin (HbA1c) levels[1]. | Animal Model: | Nos3-/- mice on the C57BL/6 background[1] | | Dosage: | 30 mg/kg | | Administration: | Oral administration; once daily; 31 days intervention (weeks 2-15) after Streptozotocin | | Result: | Had no impact on the fasting blood glucose levels, but induced an additional increase in HbA1c levels
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| | IC 50 | Rat CCR2: 20.8 nM (IC50); CCR5: 470 nM (IC50) | | References | [1] Tesch GH, et al. Combined inhibition of CCR2 and ACE provides added protection against progression of diabetic nephropathy inNos3-deficient mice.Am J Physiol Renal Physiol.2019 Dec 1;317(6):F1439-F1449. DOI:10.1152/ajprenal.00340.2019
[2] 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. DOI:10.1167/iovs.17-22731
[3] 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. DOI:10.1016/j.ekir.2018.07.010 |
| | PF-04634817 succinate Preparation Products And Raw materials |
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