PECAVAPTAN

PECAVAPTAN : Antagonist of AVPR1A and AVPR2

Structure

Information

  • AVPR1A
  • AVPR2
  • Antagonist
  • 100 nM

In Vitro Validations

Uniprot ID: P37288
Target Class: GPCR
Target SubClass: Vasorepressin receptor
Potency: Ki
Potency Value: 0.5 nM
Potency Assay: Binding assay
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Vasopressin V1a receptor, AVPR1, AVPR1A, V1AR_HUMA ...

DOI Reference: 10.1097/FJC.0000000000000677

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Selectivity within target family: Binding assay: ADRA1B (Ki > 10 µM), OXTR (Oxytocin receptor, Ki = 5.1 nM). An oxytocin antagonist (Ki 4.6 nM, selectivity vs AVPR1A and AVPR2 > 695) is available L-371,257. Selectivity outside target familyEurofins Panlabs safety screen of >120 targets at 10 µM: clean. Eurofins kinase panel (378 kinases) at 10 µM: Closest off-target NEK3 (61% inh.)
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SERP ratings and comments


SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

- the probe displays weak off target activity/inhibition at 10µM against a number of kinases and GPCRs, but this should be marginal at a concentration of 100 nM - the prove has strong inhibition & binding to Oxytocin receptor (Ki ~ 5.1 nM) which is in the range of the compound primary cellular activity. Thus Oxytocin receptor mediated off targets effects must be carefully considered when interpreting experimental results

(last updated: 3 Apr 2024 )

SERP Ratings

In Cell Rating
In Model Organisms

(last updated: 16 Apr 2024 )

SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

This is a high quality probe for studying the effects of AVPR1A and AVPR2 antagonism in vitro and in vivo. The only reason I hesitate to say it is 4 stars in model organisms is the presence of oxytocin activity as it is not clear if this would be phenotypically relevant, or if it would confound on-target effects.

(last updated: 30 Apr 2024 )