| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Prostaglandin F2α receptor (PGF2α receptor). Tiaprost is a PGF2α analogue that acts on the PGF2α receptor to induce luteolysis.
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|---|---|
| ln Vitro |
In vitro, Tiaprost is characterized as a synthetic PGF2α analogue. Its biological activity is primarily assessed through its effects on progesterone levels in vivo rather than through direct in vitro assays.
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| ln Vivo |
After starting prostatin treatment, plasma progesterone levels drop precipitously after 12 hours and peak at 3.18 nM (1 ng/mL) in 24 hours. Progesterone levels stayed marginally above (cows 1, 3, 5, and 6) or below (cow 2) 3.18 nM over the course of the following several days. The level in cow 4 dropped below 3.18 nM after remaining above it for 17 days. All cows had the lowest progesterone levels ever measured (1 to 2 nM) at term. Individual progesterone levels were unaffected by repeated luteolytic therapy with progestin (cows 1 and 2) or estradiol benzoate 1 (cow 3). Plasma progesterone levels are not markedly raised by intravaginal progesterone-releasing device (PRID) treatment. The amount of total estrogen in plasma doesn't alter much [1].
In vivo, Tiaprost causes a sharp decrease in plasma progesterone levels within 12 hours of initial treatment, reaching approximately 3.18 nM (1 ng/mL) within 24 hours. Progesterone levels remain either slightly above or below this threshold in the following days. At term, all treated cows show the lowest recorded progesterone levels (1 to 2 nM). Repeated luteolytic treatments with Tiaprost have no further influence on individual progesterone levels. Total estrogens in plasma remain generally unchanged. |
| Enzyme Assay |
Non-cell receptor binding assays for Tiaprost are performed using membrane preparations from cells expressing the prostaglandin F2α receptor. Radioligand binding studies are conducted using [³H]PGF2α as a tracer. Membranes are incubated with the radioligand and varying concentrations of Tiaprost (0.001-100 μM). Nonspecific binding is determined with excess unlabeled PGF2α. After incubation at 25°C for 60-90 minutes, bound and free ligand are separated by filtration through glass fiber filters, and radioactivity is measured by scintillation counting. IC₅₀ and Ki values are calculated from competition curves.
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| Cell Assay |
Cellular assays for Tiaprost are performed using cell lines expressing the PGF2α receptor, such as luteal cells or transfected HEK-293 cells. Cells are treated with Tiaprost at concentrations ranging from 0.01-100 μM. Receptor activation is measured by intracellular calcium mobilization using fluorescent indicators (e.g., Fluo-4). Inhibition of forskolin-stimulated cAMP accumulation is also measured as a functional readout of PGF2α receptor activation. EC₅₀ values are calculated from dose-response curves.
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| Animal Protocol |
In vivo animal studies are conducted in dairy cows. Cows pregnant for 190 to 266 days are treated initially with 0.75 mg of Tiaprost subcutaneously (day 0). Animals are examined clinically, rectally, and vaginally at two- to six-day intervals. Plasma progesterone and total estrogen levels are measured to assess the luteolytic effect. The efficacy of Tiaprost in terminating third-trimester gestations and inducing parturition is evaluated.
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| ADME/Pharmacokinetics |
Tiaprost has a molecular weight of 396.5 and a molecular formula of C20H28O6S. It is a synthetic PGF2α analogue used in veterinary medicine. The compound is typically stored as a powder at -20°C for up to 3 years or in solvent at -80°C for up to 6 months.
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| Toxicity/Toxicokinetics |
Comprehensive toxicology data for Tiaprost are limited to veterinary use. In cattle, Tiaprost is generally well tolerated at the recommended doses. Potential adverse effects may include local reactions at the injection site. Standard safety pharmacology studies would be required for therapeutic development in other species.
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| References | |
| Additional Infomation |
Thiaprost is a prostaglandin drug.
Tiaprost is a synthetic analogue of prostaglandin F2α (PGF2α) used in veterinary medicine. It is used as an estrus-synchronizing agent, to treat endometritis, and to induce parturition. Tiaprost induces luteolysis by acting on the PGF2α receptor. It is not approved for human use and is available for research purposes only. |
| Molecular Formula |
C20H28O6S
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|---|---|
| Molecular Weight |
396.49772
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| Exact Mass |
396.16
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| CAS # |
71116-82-0
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| Related CAS # |
71116-82-0;71116-83-1 (trometamol);
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| PubChem CID |
6441899
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| Appearance |
Colorless to light yellow liquid
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
613.4±55.0 °C at 760 mmHg
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| Flash Point |
324.8±31.5 °C
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| Vapour Pressure |
0.0±1.9 mmHg at 25°C
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| Index of Refraction |
1.633
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| LogP |
1.16
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
27
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| Complexity |
509
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| Defined Atom Stereocenter Count |
4
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| SMILES |
O=C(O)CCC/C=C/CC1C(/C=C/C(O)COC2=CSC=C2)C(O)CC1O
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| InChi Key |
FYBFDIIAPRHIQS-JRSBLEPXSA-N
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| InChi Code |
InChI=1S/C20H28O6S/c21-14(12-26-15-9-10-27-13-15)7-8-17-16(18(22)11-19(17)23)5-3-1-2-4-6-20(24)25/h1,3,7-10,13-14,16-19,21-23H,2,4-6,11-12H2,(H,24,25)/b3-1-,8-7+/t14?,16-,17-,18+,19-/m1/s1
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| Chemical Name |
(Z)-7-[(1R,2R,3R,5S)-3,5-dihydroxy-2-[(E)-3-hydroxy-4-thiophen-3-yloxybut-1-enyl]cyclopentyl]hept-5-enoic 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 | 2.5221 mL | 12.6103 mL | 25.2207 mL | |
| 5 mM | 0.5044 mL | 2.5221 mL | 5.0441 mL | |
| 10 mM | 0.2522 mL | 1.2610 mL | 2.5221 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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