1. Membrane Transporter/Ion Channel
  2. Potassium Channel
  3. Ropivacaine hydrochloride

Ropivacaine hydrochloride 

Cat. No.: HY-B0563B Purity: 99.97%
Handling Instructions

Ropivacaine hydrochloride is an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM.

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

Ropivacaine hydrochloride Chemical Structure

Ropivacaine hydrochloride Chemical Structure

CAS No. : 98717-15-8

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Description

Ropivacaine hydrochloride is an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM.

IC50 & Target

IC50: 402.7 μM (K2P TREK-1)[1]

In Vitro

Ropivacaine hydrochloride shows reversible inhibition of TREK-1 channels in a concentration-dependent manner. The half-maximal inhibitory concentrations (IC50) of Ropivacaine hydrochloride is 402.7±31.8 μM.. Hill coefficient is 0.89 for Ropivacaine hydrochloride[1].

In Vivo

Epidural injections of Ropivacaine hydrochloride (60, 180 and 600 μg) produce immediate and reversible motor paralysis. The motor blockade effect is dose-dependent, with paralysis duration of 4.6, 14.6 and 29.5 mins, respectively. Epidural Ropivacaine hydrochloride sustained release suspension also produces significant blockade of mechanical allodynia and thermal hyperalgesia by 59.5% and 70.9%, respectively (P<0.05). Ropivacaine hydrochloride sustained release suspension also produces a mild antinociception (response to heat stimulus) but longer anti-allodynic and anti-hyperalgesic effects, with biological half-lives of 6.4±2.5 hrs and 6.8±2.9 hrs, respectively (P<0.05). Multiple daily epidural administration of Ropivacaine hydrochloride sustained release suspension prolongs the preemptive effects (P<0.05)[2].

Clinical Trial
Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
References
Cell Assay
[1]

COS-7 cells are cultured in a 5 % CO2 humidified incubator at 37°C in Dulbecco’s Modified Eagle’s Medium containing 10 % heat-inactivated fetal bovine serum, and 1 % penicillin/streptomycin (100 U/mL and 100 μg/mL). The effect of Ropivacaine hydrochloride (10, 50, 100, 200, and 400 μM) on TREK-1 channels are investigated in COS-7 cells by using the whole cell patch clamp technique with a voltage ramp protocol ranging from -100 to 100 mV for 200 ms from a holding potential of -70 mV[1].

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

Animal Administration
[2]

Adult male Wistar rats (240±20 g body weight) are used in this study. Animals are housed four per cage with thick sawdust bedding at standard room temperature, under a 12/12 hrs reversed light-dark cycle (7:00 a.m. to 7:00 p.m.) at a constant temperature of 22±2°C. All rats receive food and water ad libitum. For epidural administration of Ropivacaine hydrochloride, a polyethylene catheter is implanted into the epidural space. One hundred microliters of 0.2% Ropivacaine hydrochloride injection, 0.2% Ropivacaine hydrochloride sustained release suspension or saline is slowly injected for 30 secs through the epidural catheter, followed by 10 μL of sterile saline[2].

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

References
Molecular Weight

310.86

Formula

C₁₇H₂₇ClN₂O

CAS No.

98717-15-8

SMILES

[H]Cl.O=C([[email protected]]1N(CCC)CCCC1)NC2=C(C)C=CC=C2C

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Ropivacaine hydrochloride
Cat. No.:
HY-B0563B
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Ropivacaine hydrochloride

Cat. No.: HY-B0563B