Salvinorin A (Synonyms: Divinorin A)

Name: Salvinorin A
Brand: MedChemExpress
SKU: HY-100845
Rating: 4.5 (0 reviews)

Cat. No.: HY-100845 Purity: 98.99%: Data Sheet
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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.

Salvinorin A Chemical Structure

CAS No. : 83729-01-5

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1 mg	In-stock	Estimated Time of Arrival: December 31
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μ Opioid Receptor/MOR κ Opioid Receptor/KOR δ Opioid Receptor/DOR NOP Receptor/ORL1

Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target

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

Cellular Effect

Cell Line	Type	Value	Description	References
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	>=10000 nM 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	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	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	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	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	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	2.2 nM Compound: 1a'	Enhancement of [35S]GTP-gamma-S binding to human KOR expressed in CHO cells Enhancement of [35S]GTP-gamma-S binding to human KOR expressed in CHO cells	[PMID: 16777411]
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]
CHO	EC₅₀	4.5 nM Compound: 1a	Enhancement of [35S]GTP-gamma-S binding to human KOR expressed in CHO cells Enhancement of [35S]GTP-gamma-S binding to human KOR expressed in CHO cells	[PMID: 16777411]
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	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	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	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	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	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	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	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	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]
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	2.82 nM Compound: 1	Activity at human kappa opioid receptor expressed in HEK293 cells as intracellular calcium mobilization Activity at human kappa opioid receptor expressed in HEK293 cells as intracellular calcium mobilization	[PMID: 17303418]
HEK293	EC₅₀	4.77 nM Compound: 6	Activity at human kappa opioid receptor expressed in HEK293 cells as intracellular calcium mobilization Activity at human kappa opioid receptor expressed in HEK293 cells as intracellular calcium mobilization	[PMID: 17303418]
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

Molecular Weight

432.46

Formula

C₂₃H₂₈O₈

CAS No.

83729-01-5

Appearance

Solid

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

Structure Classification

Initial Source

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

Purity: 98.99%

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Data Sheet (276 KB) SDS (605 KB)

COA (257 KB) HNMR (386 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]

Salvinorin A Related Classifications

Cardiovascular Disease

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Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Salvinorin A83729-01-5Divinorin AOpioid ReceptorhallucinogenKOPrpawoedemaInhibitorinhibitorinhibit

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Salvinorin A (Synonyms: Divinorin A)

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