Cat. No.: HY-100845

Salvinorin A

(Synonyms: Divinorin A)

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Salvinorin A is a potent, unique and short-acting high efficacy kappa-opioid receptor (KOPr) agonist with K_i value of 4.3 nm. Salvinorin A is a non-nitrogenous neoclerodane isolated from Salvia divinorum.

For research use only. We do not sell to patients.

Purity: 98.99%
CAS No.: 83729-01-5
Formula: C₂₃H₂₈O₈
Molecular Weight:432.46

Storage:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

Salvinorin A Chemical Structure

CAS No.: 83729-01-5

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

Ki:4.3 nm (kappa-opioid receptor)^[1]

All Opioid Receptor Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	40 nM Compound: 1	Stimulation of [35S]GTP-gamma-S, binding to Opioid receptor kappa1 expressed in CHO cells Stimulation of [35S]GTP-gamma-S, binding to Opioid receptor kappa1 expressed in CHO cells	[PMID: 16033256]
CHO	EC₅₀	0.81 nM Compound: 1, Salvinorin A	Agonist activity at human kappa opioid receptor-Galpha-16 fusion protein expressed in CHO cells by calcium flux assay Agonist activity at human kappa opioid receptor-Galpha-16 fusion protein expressed in CHO cells by calcium flux assay	[PMID: 16441078]
CHO	EC₅₀	45 nM Compound: 1, Salvinorin A	Agonist activity at human kappa opioid receptor expressed in CHO cells by [35S]GTPgammaS binding Agonist activity at human kappa opioid receptor expressed in CHO cells by [35S]GTPgammaS binding	[PMID: 16441078]
CHO	EC₅₀	4.5 nM Compound: Sal-A	Binding potency at human kappa opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay Binding potency at human kappa opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	[PMID: 16945525]
CHO	EC₅₀	45 nM Compound: 1a	Antagonist activity at human kappa opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay Antagonist activity at human kappa opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay	[PMID: 17580847]
CHO	EC₅₀	1.8 nM Compound: 1	Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	[PMID: 17981041]
CHO	EC₅₀	40 nM Compound: 1a	Agonist activity at human recombinant kappa opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay Agonist activity at human recombinant kappa opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay	[PMID: 18380425]
CHO	EC₅₀	2.1 nM Compound: 1	Agonist activity at human KOPR expressed in CHO cells assessed as enhancement of [35S]GTPgammaS binding Agonist activity at human KOPR expressed in CHO cells assessed as enhancement of [35S]GTPgammaS binding	[PMID: 19147366]
CHO	EC₅₀	7.5 nM Compound: 1	Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as increase of [35S]GTPgammaS binding Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as increase of [35S]GTPgammaS binding	[PMID: 20801035]
CHO	EC₅₀	6.9 nM Compound: salvA	Agonist activity at human KOPR expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by liquid scintillation counting Agonist activity at human KOPR expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by liquid scintillation counting	[PMID: 22204910]
CHO	EC₅₀	40 nM Compound: 1, Salvinorin A	Agonist activity at human recombinant kappa opioid receptor expressed in CHO cells assessed as [35S]GTP-gamma-S binding after 3 hrs by liquid scintillation counting Agonist activity at human recombinant kappa opioid receptor expressed in CHO cells assessed as [35S]GTP-gamma-S binding after 3 hrs by liquid scintillation counting	[PMID: 22464684]
CHO	EC₅₀	6.11 nM Compound: 1, Salvinorin A	Agonist activity at human recombinant kappa opioid receptor expressed in CHO cells assessed as calcium mobilization after 1 hrs by fluorescence analysis Agonist activity at human recombinant kappa opioid receptor expressed in CHO cells assessed as calcium mobilization after 1 hrs by fluorescence analysis	[PMID: 22464684]
CHO	EC₅₀	1.7 nM Compound: Salvinorin A	Agonist activity at human kappa opioid receptor expressed CHO cells co-expressing Galphaq16 assessed as calcium mobilization by fluorescence assay Agonist activity at human kappa opioid receptor expressed CHO cells co-expressing Galphaq16 assessed as calcium mobilization by fluorescence assay	[PMID: 25075762]
CHO	EC₅₀	0.03 nM Compound: 1	Agonist activity at human KOR expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by luminescence assay Agonist activity at human KOR expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by luminescence assay	[PMID: 25426797]
CHO	EC₅₀	≥10 μM Compound: 1	Agonist activity at human MOR expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by luminescence assay Agonist activity at human MOR expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by luminescence assay	[PMID: 25426797]
CHO	EC₅₀	4.5 nM Compound: 1	Agonist activity at human kappa opioid receptor expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding Agonist activity at human kappa opioid receptor expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding	[PMID: 26330078]
HEK293	EC₅₀	0.2 nM Compound: 1, SA	Agonist activity at kappa opioid receptor expressed in HEK293 cells by [35S]GTPgammaS binding assay Agonist activity at kappa opioid receptor expressed in HEK293 cells by [35S]GTPgammaS binding assay	[PMID: 21115248]
HEK293	EC₅₀	5 nM Compound: 1	Agonist activity at kappa opioid receptor in human HEK293 cells assessed as stimulation of Galphai signaling by cAMP assay Agonist activity at kappa opioid receptor in human HEK293 cells assessed as stimulation of Galphai signaling by cAMP assay	[PMID: 23587424]
HEK-293T	EC₅₀	0.36 nM Compound: 1	Inhibition of human kappa opioid receptor expressed in HEK293T cells assessed as inhibition of cAMP production after 30 mins Inhibition of human kappa opioid receptor expressed in HEK293T cells assessed as inhibition of cAMP production after 30 mins	[PMID: 25193297]
MCF7	IC₅₀	>100 μM Compound: Salvinorin A	Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTS/PMS assay Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTS/PMS assay	[PMID: 25075762]
U2OS	EC₅₀	31 nM Compound: salvA	Agonist activity at human KOPR expressed in U2OS cells assessed as beta-arrestin2 recruitment after 90 mins by DiscoveRx PathHunter assay Agonist activity at human KOPR expressed in U2OS cells assessed as beta-arrestin2 recruitment after 90 mins by DiscoveRx PathHunter assay	[PMID: 22204910]

In Vitro

Salvinorin A (Divinorin A)(0.01-10 pM; pre-30 minues; 24 hours) does not affect the membrane function after 24-h exposure in macrophages^[1].
Salvinorin A (Divinorin A) (0.01-10 pM; pre-30 minues; 18 hours) before LPS stimulation causes a significant and concentrationdependent manner reduction of LPS-stimulated nitrite levels, the IC50 (95% CL) of salvinorin A inhibitory effect was 6.5×10⁻¹³M^[1].
Salvinorin A (Divinorin A) (0.01-10 pM; pre-30 minues; 18 hours) incubates 30 min before LPS stimulation, reduces in concentration-dependent manner the LPSinduced iNOS, but not COX-2, hyperexpression, reaching a statistical significance at the 10 pM concentration^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Salvinorin A (intraperitoneal injection; 0.5-2 mg/kg; pre-treatment 30 minutes) at the 0.5 mg/kg dose is the most effective one, at the dose of 0.5 mg/kg, significantly inhibits oedema during the first 6 h; at the dose of 1 mg/kg, salvinorin A significantly reduces the oedema only 4 h after carrageenan injection; at the highest doses tested (2 mg/kg), salvinorin A fails to evoke significant changes on the carrageenan-induced paw oedema^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 83729-01-5
Appearance Solid
Molecular Weight 432.46
Formula C₂₃H₂₈O₈
Color White to off-white
SMILES

C[C@@]12[C@]3([H])[C@]([C@@H](C[C@@H](C3=O)OC(C)=O)C(OC)=O)(CC[C@@]1([H])C(O[C@H](C4=COC=C4)C2)=O)C
Synonyms

Divinorin A
Structure Classification
- Terpenoids
- Diterpenoids
Initial Source
- Plants
- Labiatae
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (605 KB)
- English - EN (605 KB)
- Français - FR (605 KB)
- Deutsch - DE (605 KB)
- Norwegian - NO (605 KB)
- Español - ES (605 KB)
- Swedish - SV (605 KB)
- Italian - IT (605 KB)
- Korean - KR (605 KB)
- Portuguese - PT (605 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Butelman ER, et al. Salvinorin A, a kappa-opioid receptor agonist hallucinogen: pharmacology and potential template for novel pharmacotherapeutic agents in neuropsychiatric disorders. Front Pharmacol. 2015 Sep 8;6:190. [Content Brief]

[2]. John TF, et al. The antinociceptive effect of salvinorin A in mice.Eur J Pharmacol. 2006 Sep 18;545(2-3):129-33. Epub 2006 Jul 4. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Salvinorin A

All Opioid Receptor Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

Salvinorin A Related Classifications

HY-100845 Related Classifications