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Ropivacaine mesylate

MCE China：Ropivacaine mesylate

Brand：MedChemExpress (MCE)

Cat. No.HY-B0563C

CAS：854056-07-8

Purity：99.51%

Storage：4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Ropivacaine mesylate is a long-acting amide local anaesthetic agent for a spinal block and effectively blocks neuropathic pain. Ropivacaine blocks impulse conduction via reversible inhibition of?sodium ion influx?in nerve fibressup>[1]. Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel)?TREK-1?with an IC50?of 402.7 μM in COS-7 cell's membrane.

In Vivo：Epidural administration of Ropivacaine mesylate effectively blocks neuropathic pain (both mechanical allodynia and heat hyperalgesia) without induction of analgesic tolerance and significantly delays the development of neuropathic pain produced by peripheral nerve injury[1]. Ropivacaine mesylate inhibits pressure-induced increases in filtration coefficient (Kf) without affecting pulmonary artery pressure (Ppa), pulmonary capillary pressures (Ppc), and zonal characteristics (ZC)[2]. Ropivacaine mesylate prevents pressure-induced lung edema and associated hyperpermeability as evidence by maintaining PaO2, lung wet-to-dry ratio and plasma volume in levels similar to sham rats[2]. Ropivacaine mesylate inhibits pressure-induced NO production as evidenced by decreased lung nitro-tyrosine content when compared to hypertensive lungs[2].

IC50 & Target：IC50: sodium ion influx[1]IC50: 402.7 μM (TREK-1 in COS-7 cell's membrane)[3] In Vivo Epidural administration of Ropivacaine mesylate effectively blocks neuropathic pain (both mechanical allodynia and heat hyperalgesia) without induction of analgesic tolerance and significantly delays the development of neuropathic pain produced by peripheral nerve injury[1]. Ropivacaine mesylate inhibits pressure-induced increases in filtration coefficient (Kf) without affecting pulmonary artery pressure (Ppa), pulmonary capillary pressures (Ppc), and zonal characteristics (ZC)[2]. Ropivacaine mesylate prevents pressure-induced lung edema and associated hyperpermeability as evidence by maintaining PaO2, lung wet-to-dry ratio and plasma volume in levels similar to sham rats[2]. Ropivacaine mesylate inhibits pressure-induced NO production as evidenced by decreased lung nitro-tyrosine content when compared to hypertensive lungs[2]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Adult Sprague-Dawley rats (300-400g)[2]

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References：

[1]. Li TF, et al. Epidural sustained release ropivacaine prolongs anti-allodynia and anti-hyperalgesia in developing and established neuropathic pain. PLoS One. 2015 Jan 24;10(1):e0117321.  [Content Brief]

[2]. Milan Patel, et al. Ropivacaine Inhibits Pressure-Induced Lung Endothelial Hyperpermeability in Models of Acute Hypertension. Life Sci. 2019 Apr 1;222:22-28.  [Content Brief]

[3]. Dene Simpson, et al. Ropivacaine: a review of its use in regional anaesthesia and acute pain management. Drugs. 2005;65(18):2675-717.  [Content Brief]

[4]. Hye Won Shin, et al. The inhibitory effects of bupivacaine, levobupivacaine, and ropivacaine on K2P (two-pore domain potassium) channel TREK-1. J Anesth. 2014 Feb;28(1):81-6.  [Content Brief]