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Art. -Nr.: HY-B0161C

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(R)-Duloxetine

Name: (R)-Duloxetine
Brand: MedChemExpress
SKU: HY-B0161C
Price: 215.00 USD
Availability: PreOrder

(Synonyms: (R)-LY248686)

(R)-Duloxetine ((R)-LY248686) is a neuronal voltage-gated sodium channel blocker with analgesic activity. (R)-Duloxetine blocks Na⁺ currents with higher affinity for the inactivated state than for the resting state. (R)-Duloxetine alleviates postoperative mechanical allodynia and hyperalgesia. (R)-Duloxetine exerts its effects through a local peripheral mechanism of action. (R)-Duloxetine can be used for research on postoperative (post-incisional) pain.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 116539-60-7
Formel: C₁₈H₁₉NOS
Molecular Weight:297.41

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (276 KB)

(R)-Duloxetine Chemical Structure

CAS. Nr.: 116539-60-7

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

HY-B0161CR
(R)-Duloxetine (Standard)

Reference Standard

Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle Sodium Channel Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
GH3	IC50	33.78 μM	Resting-state block of voltage-gated Na+ currents in rat pituitary GH3 cells measured by whole-cell patch-clamp assay with Na+ currents evoked by a test pulse to +50 mV from a holding potential of −140 mV. Resting-state block of voltage-gated Na+ currents in rat pituitary GH3 cells measured by whole-cell patch-clamp assay with Na+ currents evoked by a test pulse to +50 mV from a holding potential of −140 mV.	26646348
GH3	IC50	5.82 μM	Inactivated-state block of voltage-gated Na+ currents in rat pituitary GH3 cells measured by whole-cell patch-clamp assay with a 10-second conditioning pulse to −70 mV applied prior to the test pulse to promote channel inactivation. Inactivated-state block of voltage-gated Na+ currents in rat pituitary GH3 cells measured by whole-cell patch-clamp assay with a 10-second conditioning pulse to −70 mV applied prior to the test pulse to promote channel inactivation.	26646348

In Vitro

(R)-duloxetine (10 μM; 15-20 min) blocks voltage-gated Na⁺ channels in a state-dependent manner in rat GH3 cells, with approximately 5.8-fold higher potency for inactivated channels (IC₅₀ 5.82 μM) than for resting channels (IC₅₀ 33.8 μM), and produces significant use-dependent block (75% block after 60 pulses at 5 Hz)^[1].

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

In Vivo

(R)-Duloxetine (2-10 mg; s.c./i.p.; single injection; 1 h before surgery) produces significant local analgesic effects in a rat model of postoperative pain. After a single s.c. injection of 2 mg, mechanical allodynia and hyperalgesia around the incision are reduced by approximately 89%-99% within 5 days, whereas systemic i.p. administration of 10 mg reduces these endpoints by approximately 53%-69%^[1].

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

Animal Model:

Sprague-Dawley (male; weight 250-300 g; skin incision plus extension model on dorsothoracic skin)^[1]
Dosage:

2 mg (ipsilateral s.c.); 10 mg (i.p.); 10 mg (contralateral s.c.)
Administration:

s.c. (ipsilateral to incision; single injection; 1 hour prior to surgery); i.p. (single injection; 1 hour prior to surgery); s.c. (contralateral to incision; single injection; 1 hour prior to surgery)
Result:

Reduced 4 g von Frey allodynia 5-day AUC to 11% of control at 0.5 cm, 27% of control at 1.0 cm, 41% of control at 2.0 cm, and 46% of control at the contralateral site following 2 mg ipsilateral subcutaneous administration.
Reduced 15 g von Frey hyperalgesia 5-day AUC to 1% of control at 0.5 cm, 11% of control at 1.0 cm, and 65% of control at the contralateral site following 2 mg ipsilateral subcutaneous administration.
Produced analgesic effects on allodynia from time 0 through 5 days at all ipsilateral sites, with contralateral allodynia relief lasting 1 day post-injection after 2 mg ipsilateral subcutaneous administration.
Produced antihyperalgesic effects persisting for 5 days at ipsilateral sites, with responses below baseline at 0.5-1 cm from day 0 to day 3 after 2 mg ipsilateral subcutaneous administration.
Reduced 4 g allodynia 5-day AUC to 31% of control at 0.5 cm, 37% of control at 1.0 cm, 54% of control at 2.0 cm, and 72% of control at the contralateral site following 10 mg intraperitoneal administration.
Reduced 15 g hyperalgesia 5-day AUC to 35% of control at 0.5 cm, 40% of control at 1.0 cm, 48% of control at 2.0 cm, and 52% of control at the contralateral site following 10 mg intraperitoneal administration.
Produced immediate systemic allodynia reduction post-injection following 10 mg intraperitoneal administration.
Produced minimal analgesic effects on allodynia and hyperalgesia at the ipsilateral incision side, with 4 g allodynia AUC values at 89%-105% of control and 15 g hyperalgesia AUC values at 84%-92% of control across 0.5-2.0 cm ipsilateral sites following 10 mg contralateral subcutaneous administration.

Chemical Information

CAS. Nr. 116539-60-7
Molecular Weight 297.41
Formel C₁₈H₁₉NOS
SMILES

CNCC[C@@H](OC1=CC=CC2=C1C=CC=C2)C3=CC=CS3
Synonyms

(R)-LY248686
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

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 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)

Verweise

[1]. Wang CF, et al. R-Duloxetine and N-Methyl Duloxetine as Novel Analgesics Against Experimental Postincisional Pain. Anesthesia and analgesia. 2016 Mar;122(3):719-729. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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.

Bioz

Keywords

MOQ

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100 mg

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