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NP118809

Cat. No. M3613
NP118809 Structure
Synonym:

39-1B4, NP-118809

Size Price Availability Quantity
10mg USD 160 In stock
50mg USD 480 In stock
100mg USD 720 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

NP-118809 (39-1B4) is a potent N-type calcium channel blockers (IC50= 0.11 uM) which has good selectivity over L-type calcium channels. NP-118809 exhibites increased N-type channel blockade (IC50=0.11 uM) and is 111-fold more selective for N-type channels (L-type calcium channel IC50=12.2 uM). NP118809 further exhibits a number of favorable preclinical characteristics as they relate to overall pharmacokinetics and minimal off-target activity including the hERG potassium channel.

Customer Product Validations & Biological Datas
Source Bioorg Med Chem Lett (2010). Figure 3. NP118809
Method i.p.
Cell Lines rat
Concentrations 25 mg/kg
Incubation Time -
Results Figure 2 shows that up on intraperitoneal (ip) administration both NP118809 and NP078585 (25 mg/kg) both exhibited significant analgesic activity in the phase IIA portions of the rat formalin model.
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 460.61
Formula C32H32N2O
CAS Number 41332-24-5
Purity >98%
Solubility DMSO
Storage at -20°C
References

Scaffold-based design and synthesis of potent N-type calcium channel blockers.
Zamponi GW, et al. Bioorg Med Chem Lett. 2009 Nov 15;19(22):6467-72. PMID: 19815411.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: NP118809, 39-1B4, NP-118809 supplier, Calcium Channel, inhibitors

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