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Pravadoline

Cat. No. M3264
Pravadoline Structure
Synonym:

WIN 48098

Size Price Availability Quantity
5mg USD 415  USD415 In stock
10mg USD 615  USD615 In stock
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Quality Control & Documentation
Biological Activity

Pravadoline (WIN 48098) is an antiinflammatory and analgesic compound with an IC50 of 4.9 uM for inhibition of the synthesis of prostaglandins (PGs) in mouse brain. Pravadoline (WIN 48098) is related in structure to non-steroidal antinflammtory agents such as indometacin. Pravadoline (WIN 48098) was developed in the 1980s as a new antiinflammatory and prostaglandin synthesis inhibitor, acting through inhibition of the enzyme cyclooxygenase (COX).

Product Citations
Customer Product Validations & Biological Datas
Source Org Lett (2016). Scheme 1. WIN 48098 (Abmole Bioscience Inc.)
Method Short Synthesis
Cell Lines
Concentrations
Incubation Time
Results This new synthetic method provides a short synthesis of pravadoline 7a (WIN 48098) that acts as a potent antiinflammatory and analgesic drug (IC50 4.9 μM, Ki 2511 nM at CB1).
Chemical Information
Molecular Weight 378.46
Formula C23H26N2O3
CAS Number 92623-83-1
Solubility (25°C) DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
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] Allyn C Howlett, et al. The Spicy Story of Cannabimimetic Indoles

[2] R M Everett, et al. Nephrotoxicity of pravadoline maleate (WIN 48098-6) in dogs: evidence of maleic acid-induced acute tubular necrosis

[3] S J Ward, et al. Pravadoline and aminoalkylindole (AAI) analogues: actions which suggest a receptor interaction

[4] D R Haubrich, et al. Pharmacology of pravadoline: a new analgesic agent

[5] S J Ward, et al. Pravadoline: profile in isolated tissue preparations

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  Catalog
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Keywords: Pravadoline, WIN 48098 supplier, COX, inhibitors, activators


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