| Targets |
The FP receptor (Prostaglandin F2alpha receptor), which is a G-protein coupled receptor.
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| ln Vitro |
This entry is not available. A general in vitro activity for FP agonists is to reduce intraocular pressure by increasing uveoscleral outflow.
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| ln Vivo |
This entry is not available. In vivo, the deuterated form is expected to have a similar activity profile to Bimatoprost, which effectively reduces intraocular pressure.
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| Enzyme Assay |
A general protocol for assessing FP receptor binding involves a radioligand binding assay. Membrane homogenates from cells expressing the human FP receptor are incubated with [3H]-Prostaglandin F2alpha (PGF2alpha) in a buffer (50 mM Tris-HCl, pH 7.4, 10 mM MgCl2, 1 mM EDTA) at 25degC for 60 minutes. Non-specific binding is determined by adding 10 microM unlabeled PGF2alpha. The reaction is terminated by filtration, and radioactivity is measured using a scintillation counter. Ki values are calculated by performing the assay in the presence of various concentrations of the test compound, such as Bimatoprost-d5.
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| Cell Assay |
A general protocol for assessing FP receptor activation involves seeding HEK293 cells stably expressing the human FP receptor into a 96-well plate. After 24 hours, the cells are loaded with a fluorescent calcium indicator dye (e.g., Fluo-4-AM) for 45 minutes at 37degC. The cells are then washed and incubated with a range of concentrations of the test compound (e.g., Bimatoprost-d5). Intracellular calcium release, which is a downstream signal of FP receptor activation, is monitored in real-time using a fluorescence plate reader. The EC50 value is calculated by plotting the fluorescence change against the logarithm of the compound concentration.
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| Animal Protocol |
A general in vivo protocol involves using normotensive or glaucomatous animal models, such as rabbits or non-human primates. The intraocular pressure (IOP) is measured using a tonometer at baseline (0 hours). Bimatoprost-d5 is administered as a single topical ocular dose (e.g., 0.03% solution) in the test eye, while the contralateral eye receives a vehicle control. IOP is then measured at multiple time points post-dose (e.g., 1, 2, 4, 6, and 24 hours). The IOP-lowering effect is calculated as the reduction in IOP from baseline. Bimatoprost is used as a positive control for comparison.
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| ADME/Pharmacokinetics |
This entry is not available. The parent compound, Bimatoprost, is known to be metabolized primarily via oxidation, reduction, and glucuronidation. The deuterium substitution in Bimatoprost-d5 can alter the rate of metabolism, potentially leading to a longer half-life and a more stable pharmacokinetic profile compared to the non-deuterated form.
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| References | |
| Additional Infomation |
Bimatoprost-d5 is primarily used as an internal standard in analytical chemistry for the quantification of Bimatoprost in biological samples by LC-MS or LC-MS/MS. Its structure contains five deuterium atoms, giving it a distinct mass from the non-deuterated molecule, which makes it ideal for use as a tracer in drug development and pharmacokinetic studies. Bimatoprost (non-deuterated) is used topically as eye drops to control the progression of glaucoma and in the management of ocular hypertension.
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| Appearance |
Solid powder
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|---|---|
| Synonyms |
AGN 192024 d5
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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) |
DMSO : ≥ 100 mg/mL (237.76 mM)
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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.) |
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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