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DPN

Cat. No. M4835
DPN Structure
Synonym:

Diarylpropionitrile

Size Price Availability Quantity
10mg USD 135  USD150 In stock
50mg USD 540  USD600 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

DPN increased GluR2 expression in the other lamina of the CA1.DPN acts as an agonist on both ER subtypes, but has a 70-fold higher relative binding affinity and 170-fold higher relative potency in transcription assays with ERbeta than with ERalpha. DPN displayed subtype-selective agonism, being ca. 30-fold more potent through ERbeta.Both PPT and DPN can acutely relax isolated mesenteric arteries with the relative potency of PPT>17beta-oestrogen>DPN.

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 239.27
Formula C15H13NO2
CAS Number 1428-67-7
Purity >98%
Solubility DMSO
Storage at -20°C
References

Estrogen receptor alpha and beta specific agonists regulate expression of synaptic proteins in rat hippocampus.
Waters EM, et al. Brain Res. 2009 Sep 22;1290:1-11. PMID: 19596275.

Activities of estrogen receptor alpha- and beta-selective ligands at diverse estrogen responsive gene sites mediating transactivation or transrepression.
Harrington WR, et al. Mol Cell Endocrinol. 2003 Aug 29;206(1-2):13-22. PMID: 12943986.

Acute effects of oestrogen receptor subtype-specific agonists on vascular contractility.
Montgomery S, et al. Br J Pharmacol. 2003 Aug;139(7):1249-53. PMID: 12890703.

Estrogen receptor-beta potency-selective ligands: structure-activity relationship studies of diarylpropionitriles and their acetylene and polar analogues.
Meyers MJ, et al. J Med Chem. 2001 Nov 22;44(24):4230-51. PMID: 11708925.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: DPN, Diarylpropionitrile supplier, Estrogen Receptor, inhibitors

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