| Size | Price | Stock | Qty |
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| 5mg |
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| Other Sizes |
| Targets |
PF-03882845 targets the mineralocorticoid receptor (MR). It is a potent non-steroidal MR antagonist. By blocking the MR, it prevents the effects of aldosterone and other mineralocorticoids, which are involved in sodium retention, potassium excretion, and inflammation. This leads to blood pressure lowering, reduced urine albumin, and kidney protection. PF-03882845 has an IC₅₀ of 2.7 nM for MR binding.
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| ln Vitro |
In vitro, PF-03882845 is a potent MR antagonist with an IC₅₀ of 0.755 nM. It has an MR binding IC₅₀ of 2.7 nM. It shows high affinity and selectivity for the MR. It is a remarkably high affinity selective MR antagonist. Its activity has been characterized in various cell-based assays.
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| ln Vivo |
In Dahl SS rats, PF-3882845 lowers blood pressure, lowers urine albumin, and safeguards the kidneys [1]. Oral administration of PF-3882845 at a dose of 2 mg/kg results in a moderate oral bioavailability (F 86%) in male Sprague-Dawley rats [1]. Due to high plasma clearance (CL 9.8 mL/min/kg) and a wide volume of distribution (Vdss 1.4 mL/kg, respectively) after intravenous administration (2 mg)/kg in male Sprague-Dawley rats, PF-3882845 demonstrates a terminal elimination half-life (T1/2 1.7 h) [1].
In vivo, PF-03882845 lowers blood pressure, lowers urine albumin, and safeguards the kidneys in Dahl SS rats. Oral administration at a dose of 2 mg/kg results in a moderate oral bioavailability (F 86%) in male Sprague-Dawley rats. It has the potential for the treatment of hypertension and kidney disease. It prevents kidney injury and reduces the risk of hyperkalemia in animal models of kidney disease. |
| Enzyme Assay |
The activity of PF-03882845 can be assessed using cell-based receptor binding assays. Cells expressing the mineralocorticoid receptor are incubated with a radiolabeled MR ligand (e.g., [³H]aldosterone) and varying concentrations of PF-03882845. The displacement of the radioligand is measured to determine the binding affinity (IC₅₀). Functional assays measuring MR-mediated gene expression can also be used.
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| Cell Assay |
To evaluate the cellular effects of PF-03882845, cells expressing the MR are treated with the compound. The inhibition of aldosterone-induced gene expression (e.g., ENaC, SGK1) is measured by qRT-PCR. The effects on cell proliferation, migration, and inflammatory responses are assessed. The compound's effects on cell viability are also evaluated using standard assays.
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| Animal Protocol |
Animal/Disease Models: Male Dahl salt-sensitive (SS) rat [1]
Doses: 10, 40, and 100 mg/kg Route of Administration: po (oral gavage); twice (two times) daily; 21 days Experimental Results: Blood pressure observed at 10 mg/kg Dramatically diminished. Most notably, rats dosed at 40 and 100 mg/kg experienced negligible increases in blood pressure over 21 days in the presence of high salt. In vivo studies with PF-03882845 typically involve administration to animal models via oral routes. In models of hypertension (e.g., Dahl SS rats), the compound's effects on blood pressure are assessed. Its renoprotective effects are evaluated by measuring urine albumin, creatinine, and renal histology. Pharmacokinetic parameters, such as oral bioavailability and half-life, are also characterized. |
| ADME/Pharmacokinetics |
PF-03882845 has a molecular formula and weight that are not specified in the available literature. Its CAS number is 1023650-66-9. It is a potent non-steroidal mineralocorticoid receptor antagonist. It is soluble in DMSO and other organic solvents. The purity is typically >98%. It should be stored according to the manufacturer's instructions.
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| Toxicity/Toxicokinetics |
Specific toxicology data for PF-03882845 are not extensively detailed in the available literature. However, its use in animal models at effective doses suggests a degree of tolerability. As with all research compounds, standard safety precautions should be taken when handling PF-03882845. It is intended for research use only and is not for human consumption.
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| References | |
| Additional Infomation |
PF-03882845 has been used in trials investigating the basic science of type 2 diabetes and type 2 diabetic nephropathy.
PF-03882845 (PF-3882845) is a potent, non-steroidal mineralocorticoid receptor antagonist. It has an IC₅₀ of 0.755 nM for MR antagonism. PF-03882845 lowers blood pressure, reduces urine albumin, and protects the kidneys in preclinical models. It is a research tool for studying mineralocorticoid receptor function, hypertension, and nephropathy. |
| Molecular Formula |
C24H22CLN3O2
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|---|---|
| Molecular Weight |
419.903384685516
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| Exact Mass |
419.14
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| CAS # |
1023650-66-9
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| PubChem CID |
46871935
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
4.755
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
30
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| Complexity |
755
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C1CCC(C1)[C@H]2[C@H]3CCC4=C(C3=NN2C5=CC(=C(C=C5)C#N)Cl)C=CC(=C4)C(=O)O
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| InChi Key |
XNULRSOGWPFPBL-REWPJTCUSA-N
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| InChi Code |
InChI=1S/C24H22ClN3O2/c25-21-12-18(8-5-17(21)13-26)28-23(14-3-1-2-4-14)20-10-6-15-11-16(24(29)30)7-9-19(15)22(20)27-28/h5,7-9,11-12,14,20,23H,1-4,6,10H2,(H,29,30)/t20-,23-/m0/s1
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| Chemical Name |
(3S,3aR)-2-(3-chloro-4-cyanophenyl)-3-cyclopentyl-3,3a,4,5-tetrahydrobenzo[g]indazole-7-carboxylic acid
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.3815 mL | 11.9076 mL | 23.8152 mL | |
| 5 mM | 0.4763 mL | 2.3815 mL | 4.7630 mL | |
| 10 mM | 0.2382 mL | 1.1908 mL | 2.3815 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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