2. Immunology/Inflammation
  3. COX
  4. COX-1/2-IN-12

COX-1/2-IN-12 is an orally active dual inhibitor of COX-1 and COX-2, with an IC50 of 41.6 nM against human COX-1 and an IC50 of 31.1 nM against human COX-2. COX-1/2-IN-12 induces antinociceptive activity and inhibits edema in in vivo experiments. COX-1/2-IN-12 can be used in research related to inflammation and pain.

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COX-1/2-IN-12

COX-1/2-IN-12 Chemical Structure

CAS No. : 3068797-68-9

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COX-1/2-IN-12 Related Antibodies

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Description

COX-1/2-IN-12 is an orally active dual inhibitor of COX-1 and COX-2, with an IC50 of 41.6 nM against human COX-1 and an IC50 of 31.1 nM against human COX-2. COX-1/2-IN-12 induces antinociceptive activity and inhibits edema in in vivo experiments. COX-1/2-IN-12 can be used in research related to inflammation and pain[1].

IC50 & Target[1]

Human COX-1

41.6 nM (IC50)

Human COX-2

31.1 nM (IC50)

In Vitro

COX-1/2-IN-12 (Compound 73) (1-100 μM) carries an inherently low risk of hERG-mediated cardiotoxicity, with an hERG IC50 greater than 3 μM and complete solubility at a concentration of 3 μM[1].

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

COX-1/2-IN-12 Related Antibodies
Parmacokinetics
Species Dose Route T1/2 Cmax AUC0-∞ CL Bioavailability
Rat[1] 1 mg/kg i.v. 5.0 h 574 ng/mL 1444 ng·h/mL 11.6 mL/min/kg /
Rat[1] 10 mg/kg p.o. 4.5 h 186 ng/mL 1794 ng·h/mL 93.3 mL/min/kg 12.4 %
In Vivo

COX-1/2-IN-12 (10 mg/kg; p.o.; single administration) exhibits potent analgesic activity in the acetic acid-induced writhing model in mice, significantly reducing the number of writhing episodes and prolonging the latency period[1].
COX-1/2-IN-12 (10 mg/kg; p.o.; single administration) exhibits potent and long-lasting anti-inflammatory activity in a carrageenan-induced rat paw edema model, reducing the degree of edema[1].

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

Animal Model: Mice (SPF-grade)[1]
Dosage: 10 mg/kg
Administration: p.o.; single dose
Result: Reduced the number of writhing events to 10 times (compared to vehicle control's 37.5 times).
Prolonged the latency period to 7 minutes (compared to vehicle control's 3.3 min).
Achieved statistically significant efficacy.
Animal Model: Rat (SPF-grade)[1]
Dosage: 10 mg/kg
Administration: p.o.; single dose
Result: Reduced paw swelling volume to 0.377 mL at 1 h, 0.276 mL at 2 h, 0.202 mL at 4 h, and 0.158 mL at 8 h, compared to model control's 0.536 mL at 1 h, 0.432 mL at 2 h, 0.376 mL at 4 h, and 0.303 mL at 8 h.
Molecular Weight

446.45

Formula

C21H17F3N4O2S
CAS No.
SMILES

CC(C1=C(C=C(N=C21)C(C=C3)=CC=C3S(N)(=O)=O)C(F)(F)F)=NN2CC4=CC=CC=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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COX-1/2-IN-12 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

COX-1/2-IN-123068797-68-9COXCyclooxygenaseratsCOX-1COX-2hERGSprague-Dawley ratsantinociceptive activitycyclooxygenase-2anti-inflammatory activitycyclooxygenase-1mouse liver microsomesInhibitorinhibitorinhibit

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