Carbetocin
Based on 3 publication(s) in Google Scholar
Carbetocin, an oxytocin (OT) analogue, is an oxytocin receptor agonist with a Ki of 7.1 nM. Carbetocin has high affinity to chimeric N-terminus (E1) of the oxytocin receptor (Ki=1.17 μM). Carbetocin has the potential for postpartum hemorrhage research. Carbetocin can crosse the blood-brain barrier and produces antidepressant-like activity via activation of oxytocin receptors in the CNS.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté : 99.91%
- CAS No.: 37025-55-1
- Formule: C45H69N11O12S
- Masse moléculaire:988.16
-
Stockage:
Sealed storage, away from moisture and light, under nitrogen.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Activité biologique
-
Chemical Information
-
Solvant et solubilité
- Pureté et documentation
- Références
-
Help & FAQs
-
HY-17571
OxytocinHypothalamic Peptide -
HY-17572
AtosibanOxytocin/Vasopressin Receptor Antagonist -
HY-14778
RetosibanOxytocin Receptor Antagonist -
HY-15023
CligosibanOxytocin Receptor Antagonist -
HY-124733A
LIT-001Oxytocin Receptor Agonist -
HY-B1811
VasopressinCyclic Nonapeptide -
HY-16562
IrinotecanTopoisomerase I Inhibitor -
HY-13704
SN-38Topoisomerase I Inhibitor -
HY-10071
Y-27632ROCK Inhibitor -
HY-10431
SB-431542TGF-β Receptor Kinase Inhibitor -
HY-108677
L-368,899 hydrochlorideOxytocin Antagonist -
HY-17000
TolvaptanV2R Antagonist
Publications Citing Use of MedChemExpress (MCE) Carbetocin
More
Activité biologique
Description
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO-K1 | EC50 |
0.7 nM
Compound: 2
|
Agonist activity at human oxytocin receptor expressed in CHO-K1 cells after 5 hrs by firefly luciferase reporter gene assay
Agonist activity at human oxytocin receptor expressed in CHO-K1 cells after 5 hrs by firefly luciferase reporter gene assay
|
[PMID: 24874785] |
| HEK293 | EC50 |
170 nM
Compound: 2
|
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
|
[PMID: 24874785] |
| HEK293 | EC50 |
41 nM
Compound: 2
|
Agonist activity at human vasopressin V1a expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
Agonist activity at human vasopressin V1a expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
|
[PMID: 24874785] |
| HEK293 | EC50 |
>10000 nM
Compound: 2
|
Agonist activity at human vasopressin V1b expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
Agonist activity at human vasopressin V1b expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
|
[PMID: 24874785] |
| HEK293 | IC50 |
>10000 nM
Compound: 2
|
Antagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
Antagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
|
[PMID: 24874785] |
| HEK293 | EC50 |
0.01 nM
Compound: Carbetocin
|
Agonist activity at recombinant human OTR expressed in HEK293 cells assessed as increase in intracellular calcium level measured at 3 secs interval for 5 mins by fura-2/AM dye based micro spectrofluorometric method
Agonist activity at recombinant human OTR expressed in HEK293 cells assessed as increase in intracellular calcium level measured at 3 secs interval for 5 mins by fura-2/AM dye based micro spectrofluorometric method
|
[PMID: 30896946] |
| HEK293 | EC50 |
2.3 nM
Compound: Carbetocin
|
Agonist activity at recombinant human V1a receptor expressed in HEK293 cells assessed as increase in intracellular calcium level measured at 3 secs interval for 5 mins by fura-2/AM dye based micro spectrofluorometric method
Agonist activity at recombinant human V1a receptor expressed in HEK293 cells assessed as increase in intracellular calcium level measured at 3 secs interval for 5 mins by fura-2/AM dye based micro spectrofluorometric method
|
[PMID: 30896946] |
| HEK293 | EC50 |
4.8 nM
Compound: Carbetocin
|
Agonist activity at recombinant human V1b receptor expressed in HEK293 cells assessed as increase in intracellular calcium level measured at 3 secs interval for 5 mins by fura-2/AM dye based micro spectrofluorometric method
Agonist activity at recombinant human V1b receptor expressed in HEK293 cells assessed as increase in intracellular calcium level measured at 3 secs interval for 5 mins by fura-2/AM dye based micro spectrofluorometric method
|
[PMID: 30896946] |
In Vitro
Carbetocin is an agonist with about 10-fold lower affinity for the oxytocin receptor but with significantly higher stability and a longer duration of action. Carbetocin has higher affinity to the chimeric E1 receptor and especially to each of the combinations of E1 with the other extracellular domains, i.e. chimeric receptors E13 (Ki=13 nM), E123 (Ki=56 nM), and E1234 (Ki=37 nM)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Carbetocin (1, 10,100 μg/rat, i.c.v.) reveals a dose-dependent increase in the percent time spent swimming and a corresponding reduction in immobility following acute administration of 100 μg/rat[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Male Sprague-Dawley rats weighing between 300 and 500 g[1]
-
Dosage:2, 6.4, 20 mg/kg
-
Administration:IP; single dose
-
Result:Increased climbing with 6.4 mg/kg and resulted in a significantly greater proportion of time spent swimming with 20 mg/kg.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 37025-55-1
-
Appearance Solid
-
Masse moléculaire 988.16
-
Formule C45H69N11O12S
-
Color White to off-white
-
Sequence
{Butyric acid}-Tyr(OMe)-Ile-Gln-Asn-Cys-Pro-Leu-Gly-NH2 (carba sulfide bridge:Butyric acid1-Cys6)
-
Sequence Shortening
{Butyric acid}-Tyr(OMe)-IIQNCPLG-NH2 (carba sulfide bridge:Butyric acid1-Cys6)
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Sealed storage, away from moisture and light, under nitrogen
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)
Publications (3)
-
Journal Impact Factor
-
Most Recent
-
-
Neuropharmacology
2023 Sep 1:235:109576. PMID: 37164226 -
Andrology
The Oxytocin Receptor in Spermatozoa May Originate From Both Spermatogenesis and Epididymal Maturation, and Regulates Capacitation. [Abstract]2025 Sep 27. PMID: 41014065
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (101.20 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : ≥ 33.33 mg/mL (33.73 mM)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (2.53 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (2.53 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Pureté et documentation
-
Fiche technique (301 KB)
-
SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Korean - KR (419 KB)
- Portuguese - PT (419 KB)
-
Instruction de manipulation (2659 KB)
Références
[1]. Stella Chaviaras, et al. Assessing the antidepressant-like effects of carbetocin, an oxytocin agonist, using a modification of the forced swimming test. Psychopharmacology (Berl). 2010 May;210(1):35-43. [Content Brief]
[2]. Gerald Gimpl, et al. Binding domains of the oxytocin receptor for the selective oxytocin receptor antagonist barusiban in comparison to the agonists oxytocin and carbetocin. Eur J Pharmacol. 2005 Mar 7;510(1-2):9-16. [Content Brief]
[3]. David Feifel, et al. The effects of oxytocin and its analog, carbetocin, on genetic deficits in sensorimotor gating. Eur Neuropsychopharmacol. 2012 May;22(5):374-8. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 1.0120 mL | 5.0599 mL | 10.1198 mL | 25.2995 mL |
| 5 mM | 0.2024 mL | 1.0120 mL | 2.0240 mL | 5.0599 mL | |
| 10 mM | 0.1012 mL | 0.5060 mL | 1.0120 mL | 2.5300 mL | |
| 15 mM | 0.0675 mL | 0.3373 mL | 0.6747 mL | 1.6866 mL | |
| 20 mM | 0.0506 mL | 0.2530 mL | 0.5060 mL | 1.2650 mL | |
| 25 mM | 0.0405 mL | 0.2024 mL | 0.4048 mL | 1.0120 mL | |
| 30 mM | 0.0337 mL | 0.1687 mL | 0.3373 mL | 0.8433 mL | |
| DMSO | 40 mM | 0.0253 mL | 0.1265 mL | 0.2530 mL | 0.6325 mL |
| 50 mM | 0.0202 mL | 0.1012 mL | 0.2024 mL | 0.5060 mL | |
| 60 mM | 0.0169 mL | 0.0843 mL | 0.1687 mL | 0.4217 mL | |
| 80 mM | 0.0126 mL | 0.0632 mL | 0.1265 mL | 0.3162 mL | |
| 100 mM | 0.0101 mL | 0.0506 mL | 0.1012 mL | 0.2530 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Carbetocin Related Classifications
HY-17573 Related Classifications
Powered by Bioz