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Professional Design 4-Methylaminophenol Sulfate - Carbetocin to Prevent Uterine Contraction and Postpartum Hemorrhage – Gentolex

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Professional Design 4-Methylaminophenol Sulfate - Carbetocin to Prevent Uterine Contraction and Postpartum Hemorrhage – Gentolex Detail:

Product Detail

Name  CARBETOCIN
CAS number  37025-55-1
Molecular formula  C45H69N11O12S
Molecular weight  988.17
EINECS Number  253-312-6
Specific rotation  D -69.0° (c = 0.25 in 1M acetic acid)
Boiling point  1477.9±65.0 °C (Predicted)
Density  1.218±0.06 g/cm3(Predicted)
Storage conditions  -15°C
Form  powder

Synonyms

BUTYRYL-TYR(ME)-ILE-GLN-ASN-CYS-PRO-LEU-GLY-NH2, (SULFIDEBONDBETWEENBUTYRYL-4-YLANDCYS); BUTYRYL-TYR(ME)-ILE-GLN-ASN-CYS-PRO-LEU-GLY-NH2TRIFLUOROACETATESALT; (BUTYRYL1, TYR(ME)2)-1-CARBAOXYTOC INTRIFLUOROACETATESALT; (BUTYRYL1, TYR(ME)2)-OXYTOCIN; (BUTYRYL1,TYR(ME)2)-OXYTOCINTRIFLUOROACETATESALT; CARBETOCIN; CARBETOCINTRIFLUOROACETATESALT; (2-O-METHYLTYROSINE)-DE-AMINO-1-CARBAOXYTOCIN

Biological activity

Carbetocin, an oxytocin (OT) analog, is an oxytocin receptor agonist with a Ki of 7.1 nM. Carbetocin has a high affinity (Ki=1.17 μM) for the chimeric N-terminus of the oxytocin receptor. Carbetocin has potential for postpartum hemorrhage research. Carbetocin can penetrate the blood-brain barrier and has antidepressant-like activity by activating oxytocin receptors in the CNS.

Function

Carbetocin is a synthetic long-acting oxytocin 8-peptide analog with agonist properties, and its clinical and pharmacological properties are similar to those of naturally occurring oxytocin. Like oxytocin, carbetocin binds to the hormone receptors of uterine smooth muscle, causing rhythmic contractions of the uterus, increasing its frequency and increasing uterine tone on the basis of the contractions of the original. Oxytocin receptor levels in the uterus are low in the non-pregnant state, increase during pregnancy, and peak during labor. Therefore, carbetocin has no effect on the non-pregnant uterus, but has a potent uterine contractile effect on the pregnant uterus and the newly produced uterus.

Change Controls

Changes are controlled according to the procedure. Based on the impact and risk and severity, changes are classified as Major, Minor and Site. Site changes have slight impact on safety and quality of product, and therefore do not need approval and notification to the customer; Minor changes have moderate impact on safety and quality of product, and need to notify the customer; Major changes have higher impact on safety and quality of product, and need approval by the customer.

According to the procedure, change control is started with change application in which change details and rational for the change are described. The evaluation is then performed following the application, which is done by change control relevant departments. Meanwhile, the change control is classified into Major level, General level and Minor level. After appropriate evaluation as well as the classification, all level change control should be approved by QA Manager. The change control is executed after approval according to the action plan. The change control is finally closed after QA confirms the change control has been appropriately implemented. If involving client notification, the client should be notified timely after change control approved


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Professional Design 4-Methylaminophenol Sulfate - Carbetocin to Prevent Uterine Contraction and Postpartum Hemorrhage  – Gentolex detail pictures


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