| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Prostaglandin F2alpha (PGF2alpha) receptor (FP receptor). The parent drug bimatoprost and its active metabolite, 15-Keto Bimatoprost, are prostaglandin F2alpha (PGF2alpha) analogs. They are potent agonists of the FP receptor. Activation of FP receptors in the eye increases uveoscleral outflow of aqueous humor, which reduces intraocular pressure (IOP). This is the therapeutic mechanism for treating glaucoma.
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| ln Vitro |
Drug compounds have included stable heavy isotopes of carbon, hydrogen, and other elements, mostly as tracers for quantification throughout the drug development process. Due to its potential to alter the pharmacokinetic and metabolic characteristics of medications, deuteration has drawn attention[1].
A standard LC-MS/MS protocol is used: a known amount of the d5-labeled internal standard is spiked into biological samples (e.g., plasma, aqueous humor). After protein precipitation and solid-phase extraction, the sample is injected onto a C18 column. The analyte and internal standard are detected in MRM mode, and the peak area ratio is used for precise quantification. |
| Cell Assay |
The labeled internal standard is not used directly in cells. It is added to cell culture media (e.g., from primary human trabecular meshwork cells) as a standard for LC-MS/MS analysis. It measures the concentration of prostaglandin analogs produced by the cells, allowing researchers to study prostaglandin metabolism and FP receptor signaling in vitro.
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| Animal Protocol |
The internal standard is not administered to animals; it is spiked into collected samples. In an animal model of ocular hypertension (e.g., laser-induced ocular hypertension model in rabbits or monkeys), blood or aqueous humor samples are collected. The d5-internal standard is added to these samples to accurately measure the concentration of the dosed bimatoprost or its metabolites.
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| ADME/Pharmacokinetics |
15-Keto Bimatoprost-d5 has a molecular weight of 418.58 and a formula C25H30D5NO4. As an internal standard, it is chemically stable and co-elutes with the non-labeled analyte in LC, while being distinguishable by mass spectrometry. For storage, it should be kept at -20degC, protected from light and moisture. It is soluble in DMSO and ethanol.
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| Toxicity/Toxicokinetics |
The deuterated compound is non-toxic at the trace concentrations used for analytical purposes. The parent compound, Bimatoprost, is a clinically approved drug with a well-established safety profile for ocular use. The product is "For research use only" and not for human therapeutic or diagnostic use.
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| References | |
| Additional Infomation |
15-Keto Bimatoprost-d5 is a research-grade stable isotope-labeled chemical (Internal Standard) used for LC-MS/MS quantitation. It is not a drug and has no FDA approval for therapeutic use. The unlabeled parent compound, Bimatoprost, is an FDA-approved drug (Lumigan®) for reducing intraocular pressure in patients with open-angle glaucoma or ocular hypertension. This labeled standard is used for research and method validation.
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| Molecular Formula |
C25H30D5NO4
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|---|---|
| Molecular Weight |
418.58
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| Appearance |
Off-white to light yellow solid powder
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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 | 2.3890 mL | 11.9451 mL | 23.8903 mL | |
| 5 mM | 0.4778 mL | 2.3890 mL | 4.7781 mL | |
| 10 mM | 0.2389 mL | 1.1945 mL | 2.3890 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
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