SLL-022CCP
SLL-022CCP is a KOR-selective, high affinity and extremely potent agonist with an EC50 of 9.1 nM and a Ki of 2.0 nM. SLL-022CCP inhibits cAMP production with an EC50 of 0.002 nM, and exhibits high receptor subtype selectivity over the μ-opioid receptor (MOR, EC50 = 1.6 nM) and δ-opioid receptor (DOR, EC50 = 30.0 nM). SLL-022CCP exhibits robust antinociceptive and antipruritic effects with low central side effects.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- CAS. Nr.: 2084834-44-4
- Formel: C31H34N2O4
- Molecular Weight:498.61
-
Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biologische Aktivität
-
Chemical Information
- Reinheit & Dokumentation
- Verweise
-
Help & FAQs
Alle Opioid Receptor Isoform-spezifische Produkte anzeigen
More
Biologische Aktivität
Beschreibung
IC50 & Target
|
κ Opioid Receptor/KOR 2.0 nM (Ki) |
κ Opioid Receptor/KOR 9.1 nM (EC50) |
μ Opioid Receptor/MOR 18.7 nM (EC50) |
δ Opioid Receptor/DOR 186.0 nM (EC50) |
In Vitro
SLL-022CCP shows highest affinity toward KOR (Ki = 2.0 nM) and the highest selectivity (MOR/KOR = 30.1, DOR/KOR = 128)[1].
SLL-022CCP shows EC50 values of 9.1, 18.7, and 186.0 nM against KOR, MOR, and DOR, respectively, in the GTPγS binding assay using CHO cells[1].
SLL-022CCP demonstrates potent and selective agonism at the KOR, inhibiting cAMP production with an EC50 of 0.002 nM in HEK293 cell, which represents >770-fold and >14,000-fold selectivity over the MOR (EC50 = 1.6 nM) and DOR (EC50 = 30.0 nM)[1].
SLL-022CCP induces cAMP inhibition which reaches 76.5%, 77.7%, and 119.2% of the maximal stimulation obtained with U69593, DAMGO, and DPDPE in HEK293 cell[1].
SLL-022CCP does not exhibit KOR or MOR antagonist activity respectively in HEK293 cell[1].
SLL-022CCP recruits β-arrestin at the KOR with an EC50 of 15.5 nM and at the MOR with an EC50 of 668.0 nM in HTLA cells transfected with MOR or KOR Tango plasmid[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
SLL-022CCP (0.0625-0.25 mg/kg; i.p.; single dose) produces significant antipruritic effects in the histamine-induced itch test (ED50 = 0.079 mg/kg) and the Complete Freund’s adjuvant (CFA) (HY-153808) -induced itch test (ED50 = 0.105 mg/kg) in mice[1].
SLL-022CCP (0.1-3.2 mg/kg; i.p.; single dose) shows a dose-dependently trend toward increasing nesting behaviors in male ICR mice in lactic acid-induced depression of nesting behavior[1].
SLL-022CCP (1-8 mg/kg; i.p.; single dose) does not impair motor coordination at effective dose but exerts this effect at higher doses in male Kunming mice in the rotarod test[1].
SLL-022CCP (1.8-8 mg/kg; i.p.; single dose) causes transient sedation at its effective dose in male Kunming mice in locomotor activity test[1].
SLL-022CCP (i.p.; once a day; 5 days) does not cause aversion at the antinociceptive dose in male ICR mice in the the conditioned place aversion (CPA) experiment[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Male ICR mice in Acetic Acid-induced writhing test[1].
-
Dosage:0.0625 mg/kg, 0.125 mg/kg, 0.25 mg/kg, 0.5 mg/kg
-
Administration:i.p.; single dose
-
Result:Reduced scratching behaviors in a dose-dependent manner, exhibiting an ED50 of 0.113 mg/kg.
-
Animal Model:Kunming mice were pretreated with the KOR antagonist Nor-Binaltorphimine (Nor-BNI) (HY-117040) (−24 h, i.p.) or the MOR antagonist CTAP (HY-P1335) (−1 h, i.p.) and then intraperitoneally injected with the compound (−3 h) or vehicle (−3 h) in hot plate test[1].
-
Dosage:8 mg/kg
-
Administration:i.p.; single dose
-
Result:Attenuated antinociception with Nor-BNI pretreatment significantly but had no significant effect with CTAP pretreatment.
-
Animal Model:Kunming mice in hot plate test[1].
-
Dosage:1 mg/kg, 3 mg/kg, 5 mg/kg, 8 mg/kg
-
Administration:i.p.; single dose
-
Result:Induced antinociception at 3 h and gradually declined and returned to the basal level within 6 h.
-
Animal Model:Male ICR mice were pretreated i.p. with the Nor-BNI (−24 h), CTAP (−1 h), or vehicle, then injected i.p. with SLL-022CCP (0.25 mg/kg) or vehicle in Acetic Acid-induced writhing test[1].
-
Dosage:0.25 mg/kg
-
Administration:i.p.; single dose
-
Result:Attenuated antinociception with Nor-BNI pretreatment significantly but had no significant effect with CTAP pretreatment.
-
Animal Model:Male ICR mice were injected intradermally 100 μL of the Histamine (10 mg/mL in 1% DMSO) or 50 μL of the Complete Freund’s adjuvant into the nape of the neck in pruritogen-induced scratching test[1].
-
Dosage:0.0625 mg/kg, 0.125 mg/kg, 0.25 mg/kg
-
Administration:i.p.; single dose
-
Result:Reduced scratching behaviors in a dose-dependent manner and the ED50 was 0.079 mg/kg in the histamine-induced itch and 0.105 mg/kg in the CFA-induced itch.
Chemical Information
-
CAS. Nr. 2084834-44-4
-
Molecular Weight 498.61
-
Formel C31H34N2O4
-
SMILES
O=C(C1=C(N)C=CC=C1)[C@@H]2[C@@](C=C3)(OC)[C@H]4[C@]5(CC6)C7=C(O4)C(OC)=CC=C7CC(N6CC8CC8)[C@@]53C2
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
SLL-022CCP Related Classifications
HY-184476 Related Classifications
Powered by Bioz