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Bupivacaine hydrochloride

Cat. No. M3418
Bupivacaine hydrochloride Structure
Size Price Availability Quantity
Free Sample (1-2 mg)  USD 0 In stock
100mg USD 40  USD40 In stock
500mg USD 70  USD70 In stock
1g USD 100  USD100 In stock
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Quality Control & Documentation
Biological Activity

Bupivacaine hydrochloride is a NMDA receptor inhibitor.Bupivacaine can block sodium, L-calcium, and potassium channels.Bupivacaine potently blocks SCN5A channels with the IC50 of 69.5 μM. Bupivacaine hydrochloride can be used for the research of chronic pain. Bupivacaine hydrochloride reversibly inhibits the SK2 channel in a dose-dependent manner with the IC 50 of 16.5 µM.

Chemical Information
Molecular Weight 324.89
Formula C18H28N2O.HCl
CAS Number 18010-40-7
Solubility (25°C) DMSO 25 mg/mL
Water 12 mg/mL
Storage 2-8°C, dry, sealed, protect from light
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Hanns-Christian Dinges, et al. The analgesic efficacy of liposomal bupivacaine compared with bupivacaine hydrochloride for the prevention of postoperative pain: a systematic review and meta-analysis with trial sequential analysis

[2] Alaa Abd-Elsayed. Liposomal bupivacaine versus bupivacaine hydrochloride: are we changing the outcomes?

[3] Srdjan S Nedeljkovic, et al. Transversus Abdominis Plane Block With Liposomal Bupivacaine for Pain After Cesarean Delivery in a Multicenter, Randomized, Double-Blind, Controlled Trial

[4] Anh L Ngo, et al. Postherpetic Neuralgia: Current Evidence on the Topical Film-Forming Spray with Bupivacaine Hydrochloride and a Review of Available Treatment Strategies

[5] Andrea Casati, et al. Bupivacaine, levobupivacaine and ropivacaine: are they clinically different?

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