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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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1g |
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5g |
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Other Sizes |
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Ropivacaine HCl hydrate is a novel and potent sodium channel blocker used as an anaesthetic agent, blocking neuropathic pain. It 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.
ln Vivo |
Epidural injection of ropivacaine hydrochloride monohydrate efficiently suppresses neuropathic pain (mechanical allodynia and thermal hyperalgesia) without inducing analgesic tolerance and greatly delays nerve degeneration resulting from peripheral nerve injury. Development of sexual pain [1]. Ropivacaine hydrochloride monohydrate reduces the pressure-induced increase in filtration coefficient (Kf) without changing pulmonary artery pressure (Ppa), pulmonary capillary pressure (Ppc) and zonal characteristics (ZC) [2]. Evidence suggests that ropivacaine hydrochloride monohydrate maintains PaO2, lung wet-to-dry ratio, and plasma volume at values similar to those in sham-operated rats, hence reducing pressure-induced pulmonary edema and associated hyperosmotic risk [2] . Ropivacaine hydrochloride monohydrate reduces pressure-induced NO generation compared with hypertensive lung, as shown by lower lung nitrotyrosine levels [2].
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Animal Protocol |
Animal/Disease Models: Adult SD (SD (Sprague-Dawley)) rat (300–400g) [2]
Doses: 1 μM Route of Administration: Infusion (added to perfusate reservoir) Experimental Results: Attenuated pressure-dependent increase in filtration coefficient (Kf) . |
References |
[1]. Dene Simpson, et al. Ropivacaine: a review of its use in regional anaesthesia and acute pain management. Drugs. 2005;65(18):2675-717.
[2]. 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. [3]. 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. [4]. Milan Patel, et al. Ropivacaine Inhibits Pressure-Induced Lung Endothelial Hyperpermeability in Models of Acute Hypertension. Life Sci. 2019 Apr 1;222:22-28. |
Molecular Formula |
C17H27CLN2O
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Molecular Weight |
310.8621
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CAS # |
132112-35-7
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Related CAS # |
Ropivacaine;84057-95-4;Ropivacaine hydrochloride;98717-15-8;Ropivacaine-d7 hydrochloride;1217667-10-1;Ropivacaine mesylate;854056-07-8;Ropivacaine-d7;684647-62-9;(Rac)-Ropivacaine-d7;1392208-04-6
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SMILES |
Cl[H].O=C([C@]1([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])N1C([H])([H])C([H])([H])C([H])([H])[H])N([H])C1C(C([H])([H])[H])=C([H])C([H])=C([H])C=1C([H])([H])[H]
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ~100 mg/mL (~304.06 mM)
H2O : ~50 mg/mL (~152.03 mM) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.60 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.60 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.60 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.2169 mL | 16.0844 mL | 32.1688 mL | |
5 mM | 0.6434 mL | 3.2169 mL | 6.4338 mL | |
10 mM | 0.3217 mL | 1.6084 mL | 3.2169 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.