d[Cha4]-AVP TFA
d[Cha4]-AVP TFA is a potent and selective vasopressin (AVP) V1b receptor agonist with a Ki of 1.2 nM for human V1b receptor. d[Cha4]-AVP TFA shows more selective for V1b receptor than human V1a receptor, V2 receptor, and oxytocin receptors.
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- Fòrmula: C50H71N13O11S2
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
![d[Cha4]-AVP TFA Chemical Structure](https://file.medchemexpress.com/product_pic/hy-p1390a.gif "Click to View d[Cha4]-AVP TFA Chemical Structure")
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Actividad biológica
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Chemical Information
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Actividad biológica
Descripciòn
IC50 & Target
Ki: 1.2 nM (vasopressin V1B receptor), 151 nM (vasopressin V1A receptor), 240 nM (Oxytocin receptor), 750 nM (vasopressin V2 receptor)
In Vitro
d[Cha4]-AVP binds to hV1b receptors and human oxytocin receptors with pKi values of 9.68 and 7.68, respectively[2].
d[Cha4]-AVP stimulates [Ca2+]i increase in hV1b-CHO cells with a pEC50 value of 10.05. d[Cha4]-AVP shows pEC50 values of 6.53 and 5.92 at hV1a and hV2 receptors, respectively, and behaved as a weak antagonist at hOT receptors (pKB=6.31)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Fòrmula C50H71N13O11S2
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Sequence
{Mpa}-Tyr-Phe-{Cha}-Asn-Cys-Pro-Arg-Gly-NH2 (Disulfide bridge:Mpa1-Cys6)
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Sequence Shortening
{Mpa}YF{Cha}NCPRG-NH2 (Disulfide bridge:Mpa1-Cys6)
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[1]. Ling Ling Cheng, et al. Design of potent and selective agonists for the human vasopressin V1b receptor based on modifications of [deamino-cys1]arginine vasopressin at position 4. J Med Chem. 2004 Apr 22;47(9):2375-88. [Content Brief]
[2]. Cristiana Griffante, et al. Selectivity of d[Cha4]AVP and SSR149415 at human vasopressin and oxytocin receptors: evidence that SSR149415 is a mixed vasopressin V1b/oxytocin receptor antagonist. Br J Pharmacol. 2005 Nov;146(5):744-51. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
d[Cha4]-AVP TFA Related Classifications
HY-P1390A Related Classifications
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