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Pregnenolone 16α-carbonitrile

Cat. No. M21085
Pregnenolone 16α-carbonitrile  Structure
Synonym:

PCN

Size Price Availability Quantity
5mg USD 78  USD78 In stock
10mg USD 122  USD122 In stock
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Quality Control & Documentation
Biological Activity

Pregnenolone 16α-carbonitrile is a derivative of pregnendione that functions as an agonist of the rodent pregnane X receptor (PXR). pregnenolone 16α-carbonitrile is a synthetic steroid that induces expression of cytochrome P450 3A. Pregnenolone 16α-carbonitrile exhibits greater tolerance to subsequent stress injury.

Chemical Information
Molecular Weight 341.49
Formula C22H31NO2
CAS Number 1434-54-4
Solubility (25°C) DMSO : 33.33 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] Peihua Liu, et al. Acta Pharm Sin B. PXR activation impairs hepatic glucose metabolism partly via inhibiting the HNF4 α-GLUT2 pathway

[2] Zhilin Luan, et al. Biochim Biophys Acta Mol Basis Dis. Pregnane X receptor (PXR) protects against cisplatin-induced acute kidney injury in mice

[3] Chuanzhu Lv, et al. Acta Pharm Sin B. Xenobiotic receptors in mediating the effect of sepsis on drug metabolism

[4] Yuki Yamasaki, et al. Biol Pharm Bull. Effect of Pregnenolone 16α-Carbonitrile on the Expression of P-Glycoprotein in the Intestine, Brain and Liver of Mice

[5] Susumu Kodama, et al. Toxicol Lett. Pregnenolone 16α-carbonitrile ameliorates concanavalin A-induced liver injury in mice independent of the nuclear receptor PXR activation

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Keywords: Pregnenolone 16α-carbonitrile , PCN supplier, Cytochrome P450 (e.g. CYP17), inhibitors, activators


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