2. GPCR/G Protein Immunology/Inflammation
  3. CCR
  4. PF-04634817 succinate

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.

For research use only. We do not sell to patients.

PF-04634817 succinate Chemical Structure

PF-04634817 succinate Chemical Structure

CAS No. : 2140301-98-8

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5 mg USD 345 In-stock
10 mg USD 550 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of PF-04634817 succinate:

PF-04634817 succinate Related Antibodies

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CCR1 CCR2 CCR3 CCR4 CCR5 CCR6 CCR7 CCR8 CCR9

  • Biological Activity

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Description

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].

IC50 & Target[1]

Rat CCR2

20.8 nM (IC50)

CCR5

470 nM (IC50)

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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
Clinical Trial
Molecular Weight

629.67

Formula

C29H42F3N5O7
CAS No.
Appearance

Solid

Color

White to off-white

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.OC(CCC(O)=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 14.48 mg/mL (23.00 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5881 mL 7.9407 mL 15.8813 mL
5 mM 0.3176 mL 1.5881 mL 3.1763 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.50%

SDS (252 KB)

COA (256 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.5881 mL 7.9407 mL 15.8813 mL 39.7033 mL
5 mM 0.3176 mL 1.5881 mL 3.1763 mL 7.9407 mL
10 mM 0.1588 mL 0.7941 mL 1.5881 mL 3.9703 mL
15 mM 0.1059 mL 0.5294 mL 1.0588 mL 2.6469 mL
20 mM 0.0794 mL 0.3970 mL 0.7941 mL 1.9852 mL
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PF-04634817 succinate Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PF-046348172140301-98-8PF04634817PF 04634817CCRCC chemokine receptorDiabeticMacularEdemaOvertNephropathynon-alcoholicsteatohepatitisNASH,fibrosis,interventionagentInhibitorinhibitorinhibit

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