1. Immunology/Inflammation
  2. COX
  3. Firocoxib

Firocoxib (Synonyms: ML 1785713)

Cat. No.: HY-14670 Purity: 98.42%
Handling Instructions

Firocoxib (ML 1785713) is a potent, selective and orally active COX-2 inhibitor with an IC50 of 0.13 μM. Firocoxib shows 58-fold more selective for COX-2 than COX-1 (IC50 of 7.5 μM). Firocoxib has anti-inflammatory effects.

For research use only. We do not sell to patients.

Firocoxib Chemical Structure

Firocoxib Chemical Structure

CAS No. : 189954-96-9

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10 mM * 1  mL in DMSO USD 158 In-stock
Estimated Time of Arrival: December 31
5 mg USD 144 In-stock
Estimated Time of Arrival: December 31
10 mg USD 192 In-stock
Estimated Time of Arrival: December 31
50 mg USD 688 In-stock
Estimated Time of Arrival: December 31
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Description

Firocoxib (ML 1785713) is a potent, selective and orally active COX-2 inhibitor with an IC50 of 0.13 μM. Firocoxib shows 58-fold more selective for COX-2 than COX-1 (IC50 of 7.5 μM). Firocoxib has anti-inflammatory effects[1].

IC50 & Target[1]

COX-2

0.13 μM (IC50)

COX-1

7.5 μM (IC50)

In Vitro

The COX-1:COX-2 selectivity ratios generally are established by comparing the IC50 for COX-1 to the IC50 for COX-2. The IC80 value more closely resembles the steady-state plasma drug concentration than does the IC50 value[1].
The selectivity ratio for Firocoxib based on the IC80 values is 121 (IC80 of 0.36 μM and 43.6 μM for COX-2 and COX-1, respectively), indicating that selectivity for COX-2 is not reduced at concentrations higher than the IC50. Notably, Firocoxib concentrations that yield 80% to 95% inhibition of COX-2 produce < 20% inhibition of COX-1[1].

In Vivo

Firocoxib (0.75-1.5mg/kg; oral gavage; female domestic shorthair cats) treatment efficacious in attenuating fever when administered to cats 1 or 14 hours before LPS challenge[1].
Pharmacokinetic properties of Firocoxib are determined after i.v. (2 mg/kg) and oral (3 mg/kg) administration in male cats. Firocoxib has moderate to high oral bioavailability (54% to 70%), low plasma clearance (4.7 to 5.8 mL/min/kg), and an elimination half-life of 8.7 to 12.2 hours[1].

Animal Model: 14 healthy female domestic shorthair cats (11-15 months old, 2.9-3.9 kg) with lipopolysaccharide (LPS)[1]
Dosage: 0.75 mg/kg, 1.5 mg/kg
Administration: Oral gavage
Result: Was efficacious in attenuating fever when administered to cats 1 or 14 hours before LPS challenge.
Molecular Weight

336.40

Formula

C₁₇H₂₀O₅S

CAS No.

189954-96-9

SMILES

O=C1OC(C)(C)C(C2=CC=C(S(=O)(C)=O)C=C2)=C1OCC3CC3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 52 mg/mL (154.58 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9727 mL 14.8633 mL 29.7265 mL
5 mM 0.5945 mL 2.9727 mL 5.9453 mL
10 mM 0.2973 mL 1.4863 mL 2.9727 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

FirocoxibML 1785713ML1785713ML-1785713COXCyclooxygenaseCOX-2anti-inflammatoryorallyLPSfeversafetyIC80Inhibitorinhibitorinhibit

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Firocoxib
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HY-14670
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