1. Immunology/Inflammation
  2. COX

Timegadine (Synonyms: SR1368)

Cat. No.: HY-100125
Handling Instructions

Timegadine, a new antiinflammatory agent, is found to be a potent, competitive inhibitor of cyclo-oxygenase (COX) and lipo-oxygenase, with IC50s ranging from 5 nM (washed rabbit platelets) to 20 μM (rat brain) for COX and 100 μM for lipo-oxygenase both in the cytosol fraction of horse platelet homogenates, and in washed rabbit platelets.

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

Timegadine Chemical Structure

Timegadine Chemical Structure

CAS No. : 71079-19-1

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Description

Timegadine, a new antiinflammatory agent, is found to be a potent, competitive inhibitor of cyclo-oxygenase (COX) and lipo-oxygenase, with IC50s ranging from 5 nM (washed rabbit platelets) to 20 μM (rat brain) for COX and 100 μM for lipo-oxygenase both in the cytosol fraction of horse platelet homogenates, and in washed rabbit platelets.

IC50 & Target

COX

5 nM (IC50, in rabbit platelets)

COX

20 μM (IC50, in rat brain)

lipo-oxygenase

100 μM (IC50, in horse and washed rabbit platelets)

In Vitro

Timegadine, a new antiinflammatory agent, is found to be a potent, competitive inhibitor of of COX and lipo-oxygenase, with IC50s ranging from 5 nM (washed rabbit platelets) to 20 μM (rat brain) for COX and 100 μM for lipo-oxygenase both in the cytosol fraction of horse platelet homogenates, and in washed rabbit platelets[2].

In Vivo

Timegadine, a new antiinflammatory agent, is found to be a potent, competitive inhibitor of prostaglandin synthetase which also inhibits cyclo-oxygenase (COX) and lipoxygenase. Daily oral doses of 10 to 30 mg/kg of Timegadine significantly inhibit both the primary and secondary lesions of adjuvant arthritis when the treatment is initiated on the day of the disease induction and continues for 28 days. Timegadine is able specifically to prevent the development of the swelling of the non-injected paw until 28 days after the adjuvant injection when administered for 5 days prior to and 5 days after the induction of the disease, in analogy with the effect of cyclophosphamide[1].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7360 mL 13.6799 mL 27.3598 mL
5 mM 0.5472 mL 2.7360 mL 5.4720 mL
10 mM 0.2736 mL 1.3680 mL 2.7360 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[1]

Female inbred Lewis rats (body weight ~150 g) are used in adjuvant arthritis and experimental allergic encephalomyelitis experiments. Paw volume is determined by mercury displacement plethismometer. Timegadine is administered orally in a volume of 1 mL/kg body weight, suspended in 0.5% carboxymethylcellulose[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

365.50

Formula

C₂₀H₂₃N₅S

CAS No.

71079-19-1

SMILES

CC1=NC2=CC=CC=C2C(/N=C(NC3CCCCC3)/NC4=NC=CS4)=C1

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Timegadine
Cat. No.:
HY-100125
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Timegadine

Cat. No.: HY-100125