Cart summary

You have no items in your shopping cart.

Crisaborole

SKU: orb1302987

Description

Crisaborole

Research Area

Metabolism Research

Images & Validation

Key Properties

CAS Number906673-24-3
MW251.05
Purity99.70%
FormulaC14H10BNO3
SMILESOB1OCc2cc(Oc3ccc(cc3)C#N)ccc12
TargetPDE
Solubility10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (7.97 mM);DMSO:250 mg/mL (995.82 mM)

Bioactivity

Target IC50
PDE4:0.49 μM
In Vivo
AN-2728 is well tolerated and significantly impacts efficacy markers, showing comparable results to positive controls in clinical trials. It effectively inhibits ear edema induced by phorbol ester with a dosing of 1 mg/ear×2 (78% and 68%, respectively), mirroring the efficacy of dexamethasone. This suggests AN-2728 possesses notable anti-inflammatory properties and skin penetration capabilities.
In Vitro
AN-2728 inhibits PDE isozymes PDE1A3, PDE3Cat , PDE4Cat and PDE7A1 with IC50 values of 6.1, 6.4, 0.11 and 0.73 μM. AN-2728 inhibits PDE4, TNF-α, IL-2, IFN-γ, IL-5 and IL-10 with IC50 values of 0.49, 0.54, 0.61, 0.83, 2.4 and 5.3 μM. AN-2728 shows the most potent activity against PDE4 catalytic domain, but it also shows inhibition against PDE1A3, PDE3Cat, and PDE7A1. Crystallography reveals that interaction of benzoxaboroles with the hydrophobic pocket in the PDE4 catalytic domain increase their affinity for PDE4. These benzoxaboroles strongly suppresses the secretion of cytokines associated with Ps and AD.

Storage & Handling

StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

Crisaborole, AN 2728, AN2728, AN-2728, Inhibitor, inhibit, PDE4, phosphodiesterase, Phosphodiesterase (PDE), PF 06930164, PF06930164, PF-06930164

Similar Products

  • Crisaborole-d4 [orb2299762]

    255.07

    C14H6D4BNO3

    5 mg, 1 mg
  • AN7602 [orb3143736]

    2803552-55-6

    241.24

    C14H11NO3

    10 mg, 50 mg
  • AN-2728 [orb1223689]

    >98% (HPLC)

    906673-24-3

    251.0451

    C14H10BNO3

    1 g, 500 mg, 10 mg, 50 mg, 200 mg, 100 mg
Quality Guarantee

Quality Guarantee

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at support@biorbyt.com.

Key Properties

No computed properties available.

Documents Download

Datasheet
Product Information
Download

Request a Document

Protocol Information

Crisaborole (orb1302987)

  • Star
  • Star
  • Star
  • Star
  • Star
  • 0.0
Based on 0 reviews

Participating in our Biorbyt product reviews program enables you to support fellow scientists by sharing your firsthand experience with our products.

Login to Submit a Review

No reviews yet

Step 1: Enter information below

(Recommended: An additional animal making an allowance for loss during the experiment)

Step 2: Enter the in vivo formulation

(This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO +
%+
% Tween 80 +
%

Available Sizes

Select a size below

10 mg
$ 80.00
1 ml x 10 mM (in DMSO)
$ 90.00
50 mg
$ 90.00
100 mg
$ 130.00
200 mg
$ 160.00
DispatchUsually dispatched within 3-5 working days
Bulk Enquiry