| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| Other Sizes |
| Targets |
The primary target of the parent drug (Cilostazol) is phosphodiesterase 3 (PDE3). 4'-trans-Hydroxy Cilostazol retains some PDE3 inhibitory activity, though it is less potent than the parent compound. It also contributes to the overall pharmacological effect of Cilostazol.
|
|---|---|
| ln Vitro |
In vitro, the metabolite inhibits PDE3 with an IC50 approximately 2-5 fold higher (less potent) than Cilostazol. It also shows weak inhibition of other PDE isoforms. Like the parent, it increases intracellular cAMP levels in platelets and vascular smooth muscle cells.
|
| ln Vivo |
In vivo, this metabolite circulates at concentrations roughly 20-50% of the parent drug after Cilostazol administration. It contributes to the antiplatelet and vasodilatory effects. Animal studies show that the trans-hydroxy metabolite has a longer elimination half-life than Cilostazol.
|
| Enzyme Assay |
Standard protocol: PDE3 inhibition assays use recombinant human PDE3 enzyme. The compound is incubated with [3H]cAMP or a non-radioactive cAMP substrate. The reaction is stopped by boiling, and the product (AMP) is converted to adenosine and quantified by scintillation or by using a PDE-Glo assay.
|
| Cell Assay |
Standard cellular assays: Human platelets or vascular smooth muscle cells are incubated with the compound. Intracellular cAMP levels are measured by ELISA or radioimmunoassay. Antiplatelet activity is assessed by aggregometry using platelet-rich plasma and aggregating agents like ADP or collagen.
|
| Animal Protocol |
In vivo pharmacokinetic studies: Rats or dogs are administered Cilostazol orally. Blood samples are collected over 24-48 hours, and plasma concentrations of 4'-trans-Hydroxy Cilostazol are determined by LC-MS/MS to assess metabolite formation and elimination.
|
| ADME/Pharmacokinetics |
Metabolism / Metabolites
OPC-13217 is a known human metabolite of cilostazol. This metabolite has an elimination half-life of approximately 6-8 hours in humans, longer than the parent drug (3-4 hours). It is highly protein-bound (>95%) and is primarily eliminated via glucuronidation and further oxidation before renal excretion. |
| Toxicity/Toxicokinetics |
As a metabolite of an approved drug, toxicity is well-characterized through the parent drug's safety profile. Cilostazol and its metabolites are generally well tolerated but may cause headaches, diarrhea, and palpitations. This specific impurity is controlled in pharmaceutical formulations.
|
| References |
[1]. Weng Q, et, al. Effect of Baicalein on the Pharmacokinetics of Cilostazol and Its Two Metabolites in Rat Plasma Using UPLC-MS/MS Method. Front Pharmacol. 2022 Apr 27;13:888054.
|
| Additional Infomation |
This compound is an analytical reference standard, not a drug. It is used for impurity profiling and pharmacokinetic studies of Cilostazol. Cilostazol is approved for intermittent claudication. The trans-hydroxy metabolite is less active than the cis isomer and the parent.
|
| Molecular Formula |
C20H27N5O3
|
|---|---|
| Molecular Weight |
385.46
|
| Exact Mass |
385.211
|
| CAS # |
87153-04-6
|
| Related CAS # |
4'-trans-Hydroxy Cilostazol-d5;4-cis-Hydroxy Cilostazol-d5
|
| PubChem CID |
10022985
|
| Appearance |
White to off-white solid powder
|
| Density |
1.42g/cm3
|
| Boiling Point |
710.5ºC at 760 mmHg
|
| Melting Point |
200-202ºC
|
| Flash Point |
383.5ºC
|
| Index of Refraction |
1.691
|
| LogP |
2.573
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
28
|
| Complexity |
514
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C(C1=NN=NN1[C@@H]1CC[C@@H](O)CC1)CCCOC1C=CC2NC(CCC=2C=1)=O
|
| InChi Key |
KFXNZXLUGHLDBB-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C20H27N5O3/c26-16-7-5-15(6-8-16)25-19(22-23-24-25)3-1-2-12-28-17-9-10-18-14(13-17)4-11-20(27)21-18/h9-10,13,15-16,26H,1-8,11-12H2,(H,21,27)
|
| Chemical Name |
6-[4-[1-(4-hydroxycyclohexyl)tetrazol-5-yl]butoxy]-3,4-dihydro-1H-quinolin-2-one
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 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
|
|---|---|
| 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 | 2.5943 mL | 12.9715 mL | 25.9430 mL | |
| 5 mM | 0.5189 mL | 2.5943 mL | 5.1886 mL | |
| 10 mM | 0.2594 mL | 1.2972 mL | 2.5943 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
