2. GPCR/G Protein Neuronal Signaling
  3. Opioid Receptor
  4. KOR agonist-9

KOR agonist-9 is a selective kappa opioid receptor (KOR) agonist with an EC50 of 1.41 nM. KOR agonist-9 exhibits >125-fold selectivity over μ/δ-opioid receptors. KOR agonist-9 antinociceptive and antipruritic effects in mice. KOR agonist-9 can be used for the research of pain, pruritus.

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

KOR agonist-9

KOR agonist-9 Chemical Structure

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KOR agonist-9 Related Antibodies

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μ Opioid Receptor/MOR κ Opioid Receptor/KOR δ Opioid Receptor/DOR NOP Receptor/ORL1

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Description

KOR agonist-9 is a selective kappa opioid receptor (KOR) agonist with an EC50 of 1.41 nM. KOR agonist-9 exhibits >125-fold selectivity over μ/δ-opioid receptors. KOR agonist-9 antinociceptive and antipruritic effects in mice. KOR agonist-9 can be used for the research of pain, pruritus[1].

IC50 & Target[1]

κ Opioid Receptor/KOR

0.0016 nM (Ki)

κ Opioid Receptor/KOR

1.41 nM (EC50)

μ Opioid Receptor/MOR

0.20 nM (Ki)

δ Opioid Receptor/DOR

15.15 nM (Ki)

In Vitro

KOR agonist-9 (17 h) shows significantly lower potency for β-arrestin recruitment in HTLA-KOR Tango cells (EC50 = 4912 nM) compared to cAMP inhibition, indicating G-protein biased signaling[1].

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

KOR agonist-9 Related Antibodies
In Vivo

KOR agonist-9 (compound 10e) (2-20 mg/kg; i.p.; single dose; 4 hours pretreatment) induces dose-dependent antinociception in the mouse acetic acid-induced writhing visceral nociception model[1].
KOR agonist-9 (5-10 mg/kg; i.p.; single dose; 4 hours pretreatment) induces dose-dependent antipruritic effects in the mouse histamine-induced pruritus model[1].

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

Animal Model: ICR mice (male, 18~22 g)[1]
Dosage: 2; 5; 10; 15; 20 mg/kg
Administration: i.p.; single dose; 4 hours pretreatment
Result: Produced dose-dependent antinociceptive effects.
Showed significant antinociception observed at the 15 mg/kg dose.
Animal Model: ICR mice (male, 18~22 g)[1]
Dosage: 5; 10 mg/kg
Administration: i.p.; single dose; 4 hours pretreatment
Result: Elicited dose-dependent antipruritic activity.
Showed a significant reduction in scratching bouts observed at the 10 mg/kg dose.
Molecular Weight

583.76

Formula

C36H45N3O4
SMILES

COC1=C(O2)C([C@]([C@@H]2[C@]3(OC)[C@@H](N4CCN(C(CC5=CC=CC=C5)=O)CC4)C6)(CC7)[C@@]6(CC3)C(N7CC8CC8)C9)=C9C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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KOR agonist-9 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    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:

KOR agonist-9KOR agonist9KOR agonist 9Opioid Receptorkappa opioid receptorpruritusHTLA-KOR Tango cellsHEK293-hKOR-GloSensor cellspainCHO cell membranesμ-opioid receptorsδ-opioid receptorsmouse hot-plate testsmouse acetic acid-induced writhing visceral nociception modelInhibitorinhibitorinhibit

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