Salvinorin A

Reagent Authentication Certificate:

Chemical Probes Portal Salvinorin A.pdf

Protein target name:

OPRK1

Mechanism of action:

Agonist

Recommended Concentration for use in cells:

Up to 10 nM

Probe Availability

Tocris (83729-01-5)

MilliporeSigma (83729-01-5)

Cayman (83729-01-5)

Abcam (83729-01-5)

Probe Information

Target and Probe Information

Target Details

Target class:

GPCR

Subclass:

Opioid receptor

HUGO ID:

HGNC:8154

Entrez gene ID:

4986

UNIPROT ID:

P41145

Target alias:

K-OR-1, KOR, KOR-1, OPRK

Probe Details

Chemical Probes Portal ID:

CPP36

Probe alias:

Divinorin A

PubChem CID:

128563

ChEMBL ID:

CHEMBL445332

SMILES string:

CC(=O)O[C@H]1C[C@H]([C@@]2(CC[C@H]3C(=O)O[C@@H](C[C@@]3([C@H]2C1=O)C)C4=COC=C4)C)C(=O)OC

InChi Key:

OBSYBRPAKCASQB-AGQYDFLVSA-N

Orthogonal probe:

ICI-199441

PAINs evaluation:

PAINs free

Physico-chemical properties

Solubility - preferred solvent:

DMSO

Solubility - concentration:

2 mg/mL

Storage Recommendations

Storage (dry powder):

shelf

Storage (solution):

-20 oC

Validation in Cells and Model Organisms

In vitro validation

On target activity

Potency:

16 nM

Off target activity

Potency (off target):

Off target protein and potency:

Mu opioid receptor >10,000 nMDelta opioid receptor >10,000 nM

Probe Selectivity in Vitro:

In a screen of GPCRs (50), 10 uM of Salvinorin A was active only against OPRK1.

In cell validation

On target activity in cells

Potency in cells:

EC50

235 nM

Potency assay (cells):

Agonism for guinea pig KOR. In 293 cells, Salvinorin A inhibited adenylate cyclase with EC50 = 1.05 nM.

Primary Reference

Reference (doi):

10.1073/pnas.182234399

Reference (PMID):

12192085

Endorsed probe

The Chemical Probes Portal endorses this compound as chemical probe for use in cells and in model organisms.

SAB Rating

Rating for use in Cells

3 review(s)

Rating for use in Model Organisms

3 review(s)

SAB Members

SAB Comments

The compound is a diester and, additionally, a lactone. It is highly lipophilic. The potential for intracellular esterase inactivation of the probe is high. Since the probe is for KOR, there are many other more suitable ligands to choose from which are available, selective and stable.

Jun 16 2016 - 5:28pm

This is an extremely potent and selective probe. It has activity at the CB1 receptor at 200 nM, but this should not interfere with interpretations of biological activity when the probe is used at the recommended doses/concentrations.

Jun 16 2016 - 5:28pm

This is a structurally unique probe for kappa opioid receptors. It is highly selective, poorly soluble, and rapidly metabolized. Literature suggests it has clear differences from other kappa opioid receptor ligands.

Jun 23 2016 - 7:40pm

Salvinorin A

Probe Availability

Probe Information

Target Details

K-OR-1, KOR, KOR-1, OPRK

Probe Details

Physico-chemical properties

In vitro validation

In cell validation

Primary Reference

Supporting Organizations

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Salvinorin A

Probe Availability

Probe Information

Target Details

K-OR-1, KOR, KOR-1, OPRK

Probe Details

Physico-chemical properties

In vitro validation

In cell validation

Primary Reference

Supporting Organizations

Interested in supporting the portal?