| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Oxytocin receptor. Carbetocin acetate is a synthetic peptide analog of oxytocin and a long-acting oxytocin receptor agonist. It binds to oxytocin receptors on uterine smooth muscle cells, activating G protein-coupled receptor signaling that leads to increased intracellular calcium and rhythmic uterine contractions. These contractions compress uterine blood vessels and reduce postpartum hemorrhage. Carbetocin has a longer duration of action than oxytocin.
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| ln Vitro |
An agonist with a ten-fold decrease in affinity for the oxytocin receptor, carbetocin acetate exhibits a notable increase in stability and a prolonged duration of activity. Higher affinity for chimeric E1 receptors is exhibited by carbetocin acetate, particularly when it comes to E1 binding to additional extracellular domains, such as chimeric receptors E13 (Ki=13 nM), E123 (Ki=56 nM), and E1234 (Ki=37 nM)[2].
Carbetocin acetate binds to oxytocin receptors with high affinity and activates receptor-mediated signaling. As a long-acting oxytocin receptor agonist, it induces rhythmic uterine contractions in vitro. Its activity is characterized by its ability to stimulate uterine smooth muscle contraction through oxytocin receptor activation. The compound's longer duration of action compared to oxytocin is attributed to its resistance to enzymatic degradation. |
| ln Vivo |
Treatment effects of carbetocin acetate (2–20 mg/kg; i.p.) on climbing, swimming, and percentage of immobility are noteworthy[1]. After acute 100 μg/rat dosing, there is a dose-dependent increase in % swimming time observed with carbetocin acetate (1, 10, 100 μg/rat, icv)[1].
In vivo, Carbetocin acetate is used clinically for the prevention of postpartum hemorrhage (PPH) following delivery. It induces sustained uterine contractions that help to control bleeding after childbirth. The compound is administered via intravenous or intramuscular injection, and its effects on uterine tone and bleeding are monitored. Carbetocin has a longer duration of action than oxytocin, allowing for single-dose administration for PPH prevention. |
| Enzyme Assay |
In vitro receptor binding assays for Carbetocin acetate are used to characterize its affinity for the oxytocin receptor. Radioligand binding assays are performed using membranes from cells expressing the oxytocin receptor, and the compound's ability to displace a labeled oxytocin ligand is measured to determine its binding affinity. Functional assays measuring receptor activation (e.g., calcium mobilization) confirm its agonistic activity.
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| Cell Assay |
Cellular assays for Carbetocin acetate involve treating oxytocin receptor-expressing cells (such as uterine smooth muscle cells) with the compound and measuring receptor activation. Functional readouts include intracellular calcium mobilization, which is a key downstream signal following oxytocin receptor activation. These assays confirm the compound's agonistic activity and potency at the oxytocin receptor.
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| Animal Protocol |
Animal/Disease Models: Male SD (Sprague-Dawley) rats weighing between 300 and 500 g[1]
Doses: 2, 6.4, 20 mg/kg Route of Administration: IP; single dose Experimental Results: Increased climbing with 6.4 mg/kg and resulted in a Dramatically greater proportion of time spent swimming with 20 mg/kg. In vivo efficacy of Carbetocin acetate has been evaluated in clinical studies for the prevention of postpartum hemorrhage. The compound is administered via intravenous or intramuscular injection following delivery. Efficacy endpoints include the need for additional uterotonic agents, the incidence of postpartum hemorrhage, and blood loss measurements. Carbetocin has been shown to be effective in reducing the risk of postpartum hemorrhage with a longer duration of action compared to oxytocin. |
| ADME/Pharmacokinetics |
Carbetocin acetate is a synthetic peptide analog of oxytocin. As a peptide, its pharmacokinetic properties are characterized by a short half-life, though carbetocin has a longer duration of action than oxytocin due to its resistance to enzymatic degradation. The compound is administered via intravenous or intramuscular injection. It is supplied as a sterile solution for injection and should be stored under recommended conditions.
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| Toxicity/Toxicokinetics |
Carbetocin acetate is generally well-tolerated at therapeutic doses. Common adverse effects include nausea, abdominal pain, headache, and flushing. As an oxytocin receptor agonist, it may cause uterine hyperstimulation. The compound should be used with caution in patients with cardiovascular disease, hypertension, or renal impairment.
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| References |
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| Additional Infomation |
Carbetocin acetate (CAS#: 1631754-28-3) is a synthetic analog of oxytocin and a long-acting oxytocin receptor agonist used for the prevention of postpartum hemorrhage. As a peptide analog, it induces sustained uterine contractions and has a longer duration of action than oxytocin. It is administered via intravenous or intramuscular injection and is approved for clinical use in many countries for the prevention of postpartum hemorrhage.
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| Molecular Formula |
C47H73N11O14S
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|---|---|
| Molecular Weight |
1048.21
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| Exact Mass |
1047.505
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| CAS # |
1631754-28-3
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| Related CAS # |
Carbetocin;37025-55-1
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| PubChem CID |
129319308
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
11
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| Hydrogen Bond Acceptor Count |
15
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| Rotatable Bond Count |
18
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| Heavy Atom Count |
73
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| Complexity |
1880
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| Defined Atom Stereocenter Count |
8
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| SMILES |
CC[C@H](C)[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CSCCCC(=O)N[C@H](C(=O)N1)CC2=CC=C(C=C2)OC)C(=O)N3CCC[C@H]3C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N)CC(=O)N)CCC(=O)N.CC(=O)O
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| InChi Key |
AWSBRHKQUFVWPU-AJDWMHSWSA-N
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| InChi Code |
InChI=1S/C45H69N11O12S.C2H4O2/c1-6-25(4)38-44(66)51-28(15-16-34(46)57)40(62)52-31(21-35(47)58)41(63)54-32(23-69-18-8-10-37(60)50-30(42(64)55-38)20-26-11-13-27(68-5)14-12-26)45(67)56-17-7-9-33(56)43(65)53-29(19-24(2)3)39(61)49-22-36(48)59;1-2(3)4/h11-14,24-25,28-33,38H,6-10,15-23H2,1-5H3,(H2,46,57)(H2,47,58)(H2,48,59)(H,49,61)(H,50,60)(H,51,66)(H,52,62)(H,53,65)(H,54,63)(H,55,64);1H3,(H,3,4)/t25-,28-,29-,30-,31-,32-,33-,38-;/m0./s1
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| Chemical Name |
acetic acid;(2S)-N-[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]-1-[(3R,6S,9S,12S,15S)-6-(2-amino-2-oxoethyl)-9-(3-amino-3-oxopropyl)-12-[(2S)-butan-2-yl]-15-[(4-methoxyphenyl)methyl]-5,8,11,14,17-pentaoxo-1-thia-4,7,10,13,16-pentazacycloicosane-3-carbonyl]pyrrolidine-2-carboxamide
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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: 125 mg/mL (119.25 mM)
H2O: 10 mg/mL (9.54 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (1.98 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (1.98 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (1.98 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.9540 mL | 4.7700 mL | 9.5401 mL | |
| 5 mM | 0.1908 mL | 0.9540 mL | 1.9080 mL | |
| 10 mM | 0.0954 mL | 0.4770 mL | 0.9540 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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