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MDR-652

Cat. No. M10493
MDR-652 Structure
Synonym:

MDR652

Size Price Availability Quantity
5mg USD 300  USD300 In stock
25mg USD 880  USD880 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

MDR-652 is a potent and specific transient receptor potential vanilloid 1 (TRPV1) agonist with Ki of 11.4 nM and 23.8 nM for hTRPV1 and rTRPV1, respectively. MDR-652 (5-10 mg/kg; i.p. and s.c.) blocks the neuropathic pain completely, indicating 100% maximum possible effect (MPE). MDR-652 has a promising topical pharmacokinetic profile.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 447.95
Formula C22H23ClFN3O2S
CAS Number 1933528-96-1
Purity >98%
Solubility DMSO 90 mg/mL
Storage at -20°C
References

[1] Jihyae Ann, et al. J Med Chem. Discovery of Nonpungent Transient Receptor Potential Vanilloid 1 (TRPV1) Agonist as Strong Topical Analgesic

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: MDR-652, MDR652 supplier, TRP Channel, inhibitors

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