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PF-915275 

Cat. No.: HY-18056
Handling Instructions

PF-915275 is a potent and selective inhibitor of human 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) (Ki < 1 nM) with good preclinical pharmacokinetic properties.

For research use only. We do not sell to patients.
PF-915275 Chemical Structure

PF-915275 Chemical Structure

CAS No. : 857290-04-1

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 119 In-stock
5 mg USD 108 In-stock
10 mg USD 144 In-stock
50 mg USD 576 In-stock
100 mg USD 1020 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Description

PF-915275 is a potent and selective inhibitor of human 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) (Ki < 1 nM) with good preclinical pharmacokinetic properties. IC50 value: < 1 nM (Ki)[2] Target: 11βHSD1 in vitro: PF-915275 maintains potency in our cellular assay against human 11βHSD1 (HEK293, EC50 = 5 nM) and is selective against human 11βHSD2 (HEK293, 1.5% inhibition 10 μM). PF-915275 displays only weak affinity for the rodent choline transporter (Ki = 9.6 μM) and the hamster melatonin MT3 receptor (Ki = 9.6 μM) in the Cerep Bioprint screening panel. PF-915275 has good in vitro pharmacokinetic properties. In particular, PF-915275 is categorized as a low clearance compound (liver microsome assays) with high permeability (Caco2 assay). [2] in vivo: As a prelude to in vivo studies with PF-915275, the rat pharmacokinetic properties of this compound were determined. PF-915275 has an excellent pharmacokinetic profile characterized by low clearance, long half-life and good oral bioavailability. [2]

References
Molecular Weight

350.39

Formula

C₁₈H₁₄N₄O₂S

CAS No.

857290-04-1

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 31 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
PF-915275
Cat. No.:
HY-18056
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