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PF-915275 

Cat. No.: HY-18056 Purity: 96.31%
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
Estimated Time of Arrival: December 31
5 mg USD 108 In-stock
Estimated Time of Arrival: December 31
10 mg USD 144 In-stock
Estimated Time of Arrival: December 31
50 mg USD 576 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1020 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

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]

Solvent & Solubility
In Vitro: 

DMSO : ≥ 31 mg/mL (88.47 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8540 mL 14.2698 mL 28.5396 mL
5 mM 0.5708 mL 2.8540 mL 5.7079 mL
10 mM 0.2854 mL 1.4270 mL 2.8540 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

350.39

Formula

C₁₈H₁₄N₄O₂S

CAS No.

857290-04-1

SMILES

N#CC1=CC=C(C2=CC=C(S(NC3=NC(N)=CC=C3)(=O)=O)C=C2)C=C1

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

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

PF-915275

Cat. No.: HY-18056