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(R)-(-)-Rolipram

Cat. No. M14499
(R)-(-)-Rolipram Structure
Synonym:

(R)-Rolipram; (-)-Rolipram

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10mg USD 120  USD120 In stock
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Quality Control & Documentation
Biological Activity

(R)-(-)-Rolipram is the R-enantiomer of Rolipram. Rolipram is a selective inhibitor of phosphodiesterases PDE4 with IC50 of 3 nM, 130 nM and 240 nM for PDE4A, PDE4B, and PDE4D, respectively.

Chemical Information
Molecular Weight 275.34
CAS Number 85416-75-7
Solubility (25°C) DMSO 90 mg/mL
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] Maarten Ooms, et al. [ 11 C]( R)-Rolipram positron emission tomography detects DISC1 inhibition of phosphodiesterase type 4 in live Disc1 locus-impaired mice

[2] Miran Kenk, et al. PET measurements of cAMP-mediated phosphodiesterase-4 with (R)-[11C]rolipram

[3] Mireille Lortie, et al. Analysis of (R)- and (S)-[(11)C]rolipram kinetics in canine myocardium for the evaluation of phosphodiesterase-4 with PET

[4] Kam Leung. 4-(3-Cyclopentoxy-4-[ 11 C]methoxy-phenyl)pyrrolidin-2-one

[5] Christine A Parker, et al. Behaviour of [11C]R(-)- and [11C]S(+)-rolipram in vitro and in vivo, and their use as PET radiotracers for the quantificative assay of PDE4

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  Catalog
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Keywords: (R)-(-)-Rolipram, (R)-Rolipram; (-)-Rolipram supplier, PDE, inhibitors, activators

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