| Size | Price | Stock | Qty |
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| 1mg |
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| 2mg | |||
| Other Sizes |
| Targets |
Prostacyclin (IP) receptor; also PPARdelta (peroxisome proliferator‑activated receptor delta).
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| ln Vitro |
Carbacyclin is a prostacyclin (PGI2) receptor agonist[1]. In vitro, carbacyclin inhibits platelet aggregation brought on by collagen or ADP[2]. Analogous to PGI2, carbacyclin stimulates the production of CPT-1 mRNA via PPARδ, without requiring the IP receptor signaling cascade. H-89, a PKA inhibitor, blocks carbacyclin's (0.02 μM to 20 μM) ability to activate the IP receptor signaling pathway through PKA. In cardiomyocytes, carbacyclin (0.02-80 μM) boosts PPRE promoter activity via PPARδ without affecting the IP receptor signaling pathway[3].
In vitro, carbacyclin binds to the IP receptor with high affinity and stimulates cAMP production in platelets and vascular smooth muscle cells. It potently inhibits platelet aggregation induced by ADP, collagen, or thrombin with IC₅0 values in the low nanomolar range. The compound also activates PPARdelta, leading to increased expression of CPT‑1, a key enzyme in fatty acid oxidation. This effect is independent of the IP receptor and can be observed in cells lacking IP. Carbacyclin has vasodilatory effects on isolated arteries, relaxing pre‑constricted vessels in a dose‑dependent manner. |
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| ln Vivo |
When it comes to preventing platelet aggregation in human, canine, or rabbit plasma, carbacyclin is 0.03 times more effective than prostacyclin[2]. In the mouse heart, carbacyclin (100 μg, ip) stimulates the expression of CPT-1 mRNA[3].
In vivo, carbacyclin exhibits vasodilation and inhibition of platelet aggregation when administered intravenously. It has been used in animal models to study the role of prostacyclin in cardiovascular homeostasis. However, due to its rapid metabolism (though slower than PGI2), its in vivo half‑life is still relatively short, limiting systemic use. It is not clinically developed but serves as a reference compound for comparing other stable PGI2 analogs (e.g., iloprost, treprostinil). In some studies, it has shown protective effects against ischemia‑reperfusion injury. |
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| Enzyme Assay |
IP receptor binding assays are performed using platelet membranes or membranes from cells expressing recombinant human IP receptor. Membranes are incubated with 1-2 nM [3H]‑iloprost (or [3H]‑PGI2) and increasing concentrations of carbacyclin (0.01-1000 nM) in binding buffer (50 mM Tris‑HCl, pH 7.4, 10 mM MgCl2, 1 mM EDTA, 0.1% BSA) for 60 min at 25 degC. Non‑specific binding is determined with 10 microM unlabeled iloprost. Bound radioligand is separated by filtration through GF/B filters and counted. Ki values are derived from competition curves. For PPARdelta activation, a reporter gene assay is used: cells transfected with a PPARdelta‑luciferase construct are treated with carbacyclin (0.1-10 microM) and luciferase activity is measured after 24 h.
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| Cell Assay |
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| Animal Protocol |
In vivo studies are performed in rodents, typically rats or mice. Carbacyclin is administered intravenously (bolus or infusion) at doses of 0.1-10 microg/kg/min. Blood pressure is measured via carotid artery catheter, and platelet aggregation is assessed ex vivo by collecting blood samples before and after infusion. For ischemia‑reperfusion models, the compound may be given prior to or during the ischemic period. Due to its short half‑life, continuous infusion is often required. Pharmacokinetic sampling involves blood collection at multiple time points for LC‑MS/MS analysis of carbacyclin concentrations.
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| ADME/Pharmacokinetics |
Carbacyclin has molecular formula C21H30O4 and molecular weight 350.49. It is soluble in ethanol, DMSO, and other organic solvents. The compound is stable in solution for several hours at room temperature, but it is recommended to store stock solutions at -20 degC. Its half‑life in blood is longer than that of PGI2 (minutes vs. seconds) but still relatively short (about 10-30 min in vivo). It is primarily metabolized by oxidation and conjugation. The compound is not orally bioavailable and must be administered parenterally.
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| Toxicity/Toxicokinetics |
No significant toxicity has been reported for carbacyclin at pharmacological doses. As a prostacyclin analog, it can cause vasodilation and hypotension at high doses, as well as headache and flushing. In animal studies, the compound is generally well‑tolerated. It is not approved for clinical use and is intended for research only. Standard safety precautions for handling bioactive lipids should be followed.
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| References |
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| Additional Infomation |
Carboprostacyclin is a prostaglandin.
Carbacyclin is a stable prostacyclin analog that acts as an IP receptor agonist and a PPARdelta activator. It is widely used as a research tool to study the physiological roles of prostacyclin, platelet function, vascular tone, and lipid metabolism. Its ability to induce CPT‑1 expression via PPARdelta provides a unique mechanism distinct from other prostacyclin mimetics. The compound is not a drug; it is supplied as a high‑purity reagent for in vitro and in vivo experiments. Researchers often use it as a positive control for IP receptor‑mediated effects and as a reference for comparing the stability and potency of newer PGI2 analogs. |
| Molecular Formula |
C21H34O4
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| Molecular Weight |
350.49226
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| Exact Mass |
350.245
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| CAS # |
69552-46-1
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| PubChem CID |
6436393
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
514.8±50.0 °C at 760 mmHg
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| Melting Point |
65-67 °C
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| Flash Point |
279.2±26.6 °C
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| Vapour Pressure |
0.0±3.0 mmHg at 25°C
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| Index of Refraction |
1.611
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| LogP |
3.65
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
25
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| Complexity |
482
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| Defined Atom Stereocenter Count |
5
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| SMILES |
CCCCC[C@@H](/C=C/[C@H]1[C@@H](C[C@H]2[C@@H]1C/C(=C/CCCC(=O)O)/C2)O)O
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| InChi Key |
XZFRIPGNUQRGPI-WBQKLGIQSA-N
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| InChi Code |
InChI=1S/C21H34O4/c1-2-3-4-8-17(22)10-11-18-19-13-15(7-5-6-9-21(24)25)12-16(19)14-20(18)23/h7,10-11,16-20,22-23H,2-6,8-9,12-14H2,1H3,(H,24,25)/b11-10+,15-7+/t16-,17-,18+,19-,20+/m0/s1
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| Chemical Name |
(5E)-5-[(3aS,4R,5R,6aS)-5-hydroxy-4-[(E,3S)-3-hydroxyoct-1-enyl]-3,3a,4,5,6,6a-hexahydro-1H-pentalen-2-ylidene]pentanoic 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 | 2.8531 mL | 14.2657 mL | 28.5315 mL | |
| 5 mM | 0.5706 mL | 2.8531 mL | 5.7063 mL | |
| 10 mM | 0.2853 mL | 1.4266 mL | 2.8531 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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